NCI Drug Dictionary

417 results found for: L

L-arginine/Korean ginseng/ Gingko biloba/damiana-based supplement: An amino acid and herbal supplement with libido-enhancing activity. L-arginine/korean ginseng/Ginkgo biloba/damiana-based supplement contains a blend of the amino acid L-arginine and the herbs Korean ginseng, Ginkgo biloba, and damiana (Turnera aphrodisiaca) in addition to 14 other vitamins and minerals. The semi-essential amino acid L-arginine is a precursor for nitric oxide (NO); Korean ginseng may enhance the conversion of L-arginine into NO by NO synthase; and Ginkgo biloba may promote microvascular circulation. This agent may increase NO production, resulting in vasodilatation and an enhanced circulation critical to sexual function and arousal. The damiana component may exert an anxiolytic effect and stimulate sexual behavior.
L-Asnase: (Other name for: asparaginase)
L-Carnipure L-Carnitine L-Tartrate: (Other name for: L-carnitine L-tartrate)
L-carnitine L-tartrate: A dietary supplement containing the levo-enantiomers of carnitine and tartrate with potential chemoprotective and antioxidant activities. L-carnitine L-tartrate increases fatty acid oxidation and reduces purine catabolism and free radical formation, which may prevent exercise fatigue, muscle weakness, chemotherapy-induced peripheral neuropathy, and hyperlipoproteinemia. L-carnitine, the biologically active form of carnitine, is a carrier molecule that transports activated long-chain fatty acids (LCFAs)from the cytosol to mitochondria where fatty acids are oxidized, resulting in ATP production,. L-tartrate, a salt of tartaric acid, is a potent antioxidant.
L-gossypol: The levo-enantiomer of an orally bioavailable polyphenolic aldehyde, derived primarily from unrefined cottonseed oil, with potential antineoplastic activity. Mimicking the inhibitory BH3 (Bcl-2 homology 3) domain of endogenous antagonists of Bcl-2, L-gossypol binds to and inhibits various anti-apoptotic Bcl-2 proteins, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. This agent has greater affinity for Bcl-2 proteins than racemic gossypol.
L-leucyl-L-leucine methyl ester: A 2-amino acid compound with immunomodulatory activity. L-leucyl-L-leucine methyl ester (LLME) is a lysosomotropic agent entering cells via receptor-mediated endocytosis. LLME undergoes a condensation process catalyzed by dipeptidyl peptidase I (DPPI) in lysosomes. Condensation of LLME leads to lysosomal rupture and DNA fragmentation in DPPI-expressing immune cells such as cytotoxic T-cells and natural killer cells. Therefore, this agent may be able to decrease the incidence of graft versus host disease (GVHD) via cytotoxic T-cell depletion. Furthermore, LLME has the potential for augmenting antibody production when used in pretreatment of peripheral blood mononuclear cells (PBMCs), possibly by interfering with gene expression of inflammatory factors.
L-lysine: A nutritional supplement containing the biologically active L-isomer of the essential amino acid lysine, with potential anti-mucositis activity. Upon oral intake, L-lysine promotes healthy tissue function, growth and healing and improves the immune system. L-Lysine promotes calcium uptake, is essential for carnitine production and collagen formation. As collagen is essential for connective tissue maintenance, this agent may also help heal mucosal wounds. This may help decrease and prevent mucositis induced by radiation or chemotherapy.
L-lysine/L-arginine-containing amino acid solution: An intravenous (IV) amino acid (AA) solution containing the cationic amino acids L-lysine and L-arginine, with radioprotective activity. Upon IV administration of the AA solution, L-lysine and L-arginine are specifically taken up by the kidneys. This protects the kidneys from toxicity by certain co-administered radio-labeled peptides as they compete with radio-labeled peptides for renal uptake. This reduces uptake of the radio-labeled peptides by the kidneys and decreases their renal retention. It also increases the target-to-kidney ratio of the radio-labeled peptides, thereby reducing radiation exposure to the kidneys and preventing nephrotoxicity.
L-menthol preparation NPO-11: A preparation containing L-menthol with potential anti-peristaltic activity. Upon spraying directly onto the gastric mucosa, L-menthol preparation NPO-11 may relax gastrointestinal smooth muscle. This may result in a suppression of gastric peristalsis and may be beneficial during upper GI endoscopic procedures.
L-methylfolate: A nutritional supplement containing the biologically active form of the B9 vitamin folate, 5-methyltetrahydrofolate (L-methylfolate), with potential antineoplastic activity. Upon administration, L-methylfolate is able to provide methyl groups allowing an increase in the level of DNA methylation in the promoter regions of certain tumor-promoting genes, thereby reversing the DNA hypomethylation of these genes and inactivating them. This may result in a decrease of both tumor cell proliferation and tumor progression. In addition, administration of L-methylfolate may sensitize tumor cells to the cytotoxic effects of other chemotherapeutic agents. Unlike folic acid, L-methylfolate is able to cross the blood brain barrier and could be beneficial in the treatment of brain tumors. DNA hypomethylation of certain genes leads to chromosome instability and contributes to tumor development.
L-selenomethionine: The amino acid methionine with selenium substituting for the sulphur moiety. Methionine is an essential amino acid in humans, whereas selenium is a free-radical scavenging anti-oxidant, essential for the protection of various tissues from the damages of lipid peroxidation. As a trace mineral that is toxic in high doses, selenium is a cofactor for glutathione peroxidase, an anti-oxidant enzyme that neutralizes hydrogen peroxide. L-selenomethionine is considered a safe, efficacious form of selenium and is readily bioavailable. Selenium may be chemoprotective for certain cancers, particularly prostate cancer.
labetuzumab-SN-38 immunoconjugate IMMU-130: An antibody-drug conjugate (ADC) containing labetuzumab, a mildly reduced, anti-CEACAM5 humanized monoclonal antibody, conjugated to the potent topoisomerase I inhibitor SN-38, with antineoplastic activity. The monoclonal antibody moiety of antibody-drug conjugate IMMU-130 selectively binds to carcinoembryonic cell adhesion molecule 5 (CEACAM5), which is abundantly expressed on the surface of a majority of solid tumors. Upon internalization and proteolytic cleavage, SN-38, the active metabolite of irinotecan, inhibits the activity of topoisomerase I in the tumor cells, eventually inhibiting both DNA replication and transcription and leading to tumor cell apoptosis.
LaBID: (Other name for: theophylline)
labyrinthin peptide vaccine LabVax 3(22)-23: A synthetic peptide vaccine composed of four synthetic peptide epitopes of the tumor-associated antigen (TAA) labyrinthin, with potential immunomodulating and antineoplastic activities. Upon vaccination with labyrinthin peptide vaccine LabVax 3(22)-23, the labyrinthin peptides may stimulate the immune system to mount B-cell and cytotoxic T-lymphocyte (CTL) responses against labryrinthin-expressing tumor cells. Labyrinthin is expressed on the surface of essentially all adenocarcinomas, but is not expressed in normal, healthy cells.
lacosamide: A functionalized amino acid compound specifically synthesized as an anticonvulsive drug to use as add-on therapy for partial-onset seizures with antinociceptive and neuroprotective activities. Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels without affecting fast inactivation, thereby stabilizing hyperexcitabe neuronal membranes. Furthermore, this agent binds to collapsin response mediator protein 2 (CRMP2; DPYSL2), a cytosolic phosphoprotein expressed in most tissues. In the nervous system, CRMP2 acts as a mediator of growth cone collapse as well as modifies axon number, length, and neuronal polarity.
Lactobacillus acidophilus/estriol vaginal tablet: A vaginal tablet containing a low dose of the estrogen hormone estriol and lyophilized Lactobacillus acidophilus, with hormone replacement and vaginal flora restoring activity. Upon vaginal application, estriol may restore estrogen levels locally and may relieve symptoms caused by estrogen deficiency; the Lactobacillus acidophilus may be able to restore the vaginal Lactobacillus flora.
Lactobacillus acidophilus/Streptococcus thermophilus/Bifidobacterium lactis/L. rhamnosus/B. longum/B. bifidum-based probiotic supplement: A nutritional supplement containing probiotic cultures of Lactobacillus acidophilus (L. acidophilus), L. rhamnosus Streptococcus thermophilus, Bifidobacterium lactis, (B. lactis), B. longum and B. bifidum, with gastrointestinal (GI) protective and immunomodulating activities. Upon oral administration, the bacteria in this probiotic supplement help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier that helps maintain the integrity of the epithelial barrier. This will interfere with the attachment of pathogenic bacteria and other harmful substances, prevent inflammation and improve GI function.
Lactobacillus brevis CD2 lozenge: A lozenge containing an extract from the Lactobacillus brevis (L. brevis) with potential anti-inflammatory activity. As L. brevis CD2 contains high levels of arginine deiminase, which catalyzes the conversion of arginine to citrulline and ammonia, administration of this lozenge leads to hydrolysis of arginine in the oral cavity. The growth of bacteria, which depends on arginine, is halted, polyamine biosynthesis is reduced and the production of nitric oxide (NO) is reduced. The reduction in NO generation may further prevent inflammation in the oral cavity. Therefore, this agent may be able to reduce chemo- and radiotherapy-induced mucositis.
Lactobacillus bulgaricus,/Bifidobacterium longum/Streptococcus thermophilus-based probiotic mixture: A nutritional supplement containing probiotic cultures of Lactobacillus bulgaricus, Bifidobacterium longum, and Streptococcus thermophilus, with gastrointestinal (GI) protective and immunomodulating activities. Upon oral administration, the bacteria in this probiotic supplement help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier that helps maintain the integrity of the epithelial barrier. This will interfere with the attachment of pathogenic bacteria and other harmful substances, prevent inflammation and improve GI function.
Lactobacillus crispatus M247 supplement: A supplement containing the probiotic strain Lactobacillus crispatus M247, with potential protective activity. Upon oral administration of L. crispatus M247 supplement, the bacteria in this probiotic supplement colonize the vaginal tract and help to maintain as well as restore the composition of the normal, healthy vaginal flora. The bacteria also produce lactic acid and maintain a more acidic vaginal pH level, which may prevent the colonization and proliferation of pathogenic microorganisms, thereby protecting against genitourinary infections.
lactobacillus fermented extract: A proprietary dietary supplement. Lactobacillus fermented extract is made from soymilk fermented by several strains of lactobacillus and yeast via a symbiotic co-culturing technology. The composition of the agent includes amino acids, vitamins, minerals, fatty acids, isoflavones, and saponins. Lactobacillus fermented extract may support healthy intestinal function.
Lactobacillus fermentum strain HEM 1036: A nutritional supplement containing a probiotic strain of the Gram-positive bacterium Lactobacillus (L.) fermentum, with gastrointestinal (GI) protective and immunomodulating activities. Upon oral administration of L. fermentum strain HEM 1036, the bacteria in this probiotic supplement help maintain adequate colonization of the GI tract, modulate the composition of the normal microflora., and promote the production of beneficial short-chain fatty acids while inhibiting the production of harmful short-chain fatty acids, which further improves the intestinal environment. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier that helps maintain the integrity of the epithelial barrier. This will interfere with the attachment of pathogenic bacteria and other harmful substances, prevent inflammation and improve GI function.
Lactobacillus plantarum 299v/Lactobacillus acidophilus/Bifidobacterium lactis probiotic supplement: A powder-based, probiotic supplement drink containing the non-pathogenic microorganisms Lactobacillus plantarum 299v, Lactobacillus acidophilus, and Bifidobacterium lactis, with potential immunomodulating and protective activities. Upon oral ingestion, the naturally-occurring bacterial components in this dietary supplement may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization in the GI tract, the bacteria may form a protective intestinal barrier which may prevent damage to the mucosal epithelia caused by toxins and attachment of potential pathogens, thereby protecting against infections. In addition, this agent may reduce the secretion of proinflammatory cytokines and may potentiate natural and acquired immunity.
Lactobacillus plantarum strain 299: A nutritional supplement containing the probiotic bacterium Lactobacillus plantarum 299 (Lp 299) with potential antimicrobial, immune-boosting, and anti-inflammatory activities. Upon oral ingestion, Lp 299 adheres to the intestinal mucosa, modulates the composition of the normal microflora, helps maintain adequate colonization of the gastrointestinal (GI) tract and improves digestion and metabolism. Upon colonization of the GI tract, the probiotic may form a protective barrier, thereby preventing attachment of pathogens, protecting against infections and boosting the immune system. In addition, Lp 299 stimulates the secretion of protective mucin and produces lactic acid and hydrogen peroxide as well as other substances, thereby creating an acidic environment which prevents growth of pathogens.
Lactobacillus plantarum strain 299v: A nutritional supplement containing a strain of the probiotic bacterium Lactobacillus plantarum 299v (Lp 299v) with potential antimicrobial, immune-boosting, and anti-inflammatory activities. Upon oral ingestion, L. plantarum strain 299v adheres to the intestinal mucosa, modulates the composition of the normal microflora, helps maintain adequate colonization of the gastrointestinal (GI) tract and improves digestion and metabolism. Upon colonization of the GI tract, the probiotic may form a protective barrier, thereby preventing attachment of pathogens, protecting against infections and boosting the immune system. In addition, Lp 299v stimulates the secretion of protective mucin and produces lactic acid and hydrogen peroxide as well as other substances, thereby creating an acidic environment which prevents growth of pathogens.
Lactobacillus probiotic BSL_PS6: A probiotic composed of a strain of the Gram-positive, naturally-occurring bacterium Lactobacillus, with potential antimicrobial, immunomodulatory and protective activities. Upon oral administration of the Lactobacillus probiotic BSL_PS6, the Lactobacillus strain may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization of the GI tract, this bacterium adheres to human intestinal epithelial cells, and activates intestinal epithelial proliferation. This promotes the formation and maintenance of a protective barrier, thereby preventing the attachment of harmful pathogens. The Lactobacillus produces an acidic environment that is unfavorable for pathogens, thereby further protecting the intestinal mucosa against pathogen-induced damage and a loss of integrity of the intestinal mucosal barrier. Dietary supplementation with this bacterium may decrease intestinal inflammation and enhance intestinal immune responses.
Lactobacillus reuteri probiotic lozenge: An oral lozenge containing the DSM 17938 and ATCC PTA 5289 strains of the probiotic Gram-positive, naturally occurring bacterium Lactobacillus reuteri (L. reuteri), with potential antimicrobial, immunomodulatory and protective activities. Upon oral administration of L. reuteri probiotic lozenge, the Lactobacillus strain may modulate the composition of the oral biofilm, which may inhibit the colonization and recolonization of pathogens. It may also downregulate proinflammatory cytokines and reduce inflammation.
Lactobacillus reuteri probiotic tablet: A tablet containing a strain of the probiotic Gram-positive, naturally-occurring bacterium Lactobacillus reuteri (L. reuteri), with potential antimicrobial, immunomodulatory and protective activities. Upon oral administration of the L. reuteri probiotic tablet, the Lactobacillus strain may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization of the GI tract, this bacterium adheres to human intestinal epithelial cells, and activates intestinal epithelial proliferation; both of these processes promote the formation and maintenance of a protective barrier, thereby preventing the attachment of harmful pathogens. L. reuteri produces lactic acid and other substances during fermentation, and creates an acidic environment that is unfavorable for pathogens, thereby further protecting the intestinal mucosa against pathogen-induced damage and loss of integrity of the intestinal mucosal barrier. Dietary supplementation with this bacterium has been shown to decrease intestinal inflammation and enhance innate and acquired immunity. Lactobacillus reuteri is naturally found in the GI tract.
Lactobacillus rhamnosus GG: A live specific strain of the species, Lactobacillus rhamnosus (a subspecies of Lactobacillus casei) with probiotic activity. When administered orally, Lactobacillus rhamnosus GG adheres to the mucous membrane of the intestine and may help to restore the balance of the GI microflora; promote gut-barrier functions; diminish the production of carcinogenic compounds by other intestinal bacteria; and activate the innate immune response and enhance adaptive immunity, especially during infections.
Lactobacillus rhamnosus/L. acidophilus/L. plantarum/Enterococcus faecium aqueous probiotic supplement: A water-based multi-strain probiotic composed of an extract of germinated barley containing the four live, activated lactic acid bacteria strains Lactobacillus rhamnosus, L. acidophilus, L. plantarum, and Enterococcus faecium, with potential immunomodulatory and anti-inflammatory activities. Upon oral administration of Lactobacillus rhamnosus/L. acidophilus/L. plantarum/Enterococcus faecium aqueous probiotic supplement, these four live bacteria modulate the composition of the normal gastrointestinal (GI) microflora, by increasing the beneficial bacteria and decreasing the harmful bacteria, and helps maintain adequate colonization of the GI tract, thereby improving digestion and preventing GI disturbances. These bacteria and the butyric acid produced by them create an environment unfavorable to pathogens by adhering to human epithelial cells, protecting epithelium by maintaining the tight junction integrity and forming a protective mucosal barrier. This prevents attachment of pathogens and reduces the risk of infection, and potentially reduces the severity of mucositis. By restoring gut microbiota, these bacteria may restore or enhance intestinal immune responses.
Lactobacillus rhamnosus/L. jensenii/L. crispatus/L. gasseri oral supplement: A nutritional supplement containing the probiotic Lactobacillus strains L. rhamnosus, L. jensenii, L. crispatus and L. gasseri with protective and immunomodulating activities. The bacteria in this probiotic supplement colonize the vaginal tract and help to maintain as well as restore the composition of the normal, healthy vaginal flora. The four Lactobacillus species form a protective barrier that helps both to maintain the integrity of the vaginal tract and prevent the attachment of pathogenic bacteria and other harmful substances, thereby protecting against genitourinary infections.
Lactobacillus rhamnosus/Lactobacillus reuteri probiotic supplement: A probiotic supplement containing the bacteria Lactobacillus (L.) rhamnosus and L. reuteri, with potential restorative and protective activities. Upon oral administration of the L. rhamnosus and L. reuteri probiotic supplement, the bacteria may restore and provide balance to the microbiota in the breast tissue. This may reduce or prevent inflammation, and may protect against the invasion of harmful bacteria and infection in the breast. In addition, the bacteria may restore the natural balance of the vaginal flora. This may prevent the invasion of harmful bacteria and yeast, and may prevent bacterial and yeast infections. This supplement may also relieve symptoms such as vaginal itching, odor and discharge, and may improve vaginal discomfort.
Lactobacillus vaginalis-containing vaginal capsule: A vaginal capsule formulation containing the lactic acid-producing bacterium Lactobacillus vaginalis (L. vaginalis), with vaginal healing, soothing, protective and immunomodulating activities. Upon intravaginal application of the L. vaginalis-containing vaginal capsule, L. vaginalis provides the naturally occurring vaginal bacterium to a dysregulated vaginal microbiome, and thereby restores the vaginal Lactobacillus flora to an optimal vaginal lactobacillus-dominated microbiota. L. vaginalis produces efficient levels of lactic acid, which normalizes and restores a healthy vaginal pH. Altogether, this enhances epithelial barrier integrity and barrier protection, and may prevent or improve various vulvovaginal symptoms, such as vulvovaginal atrophy, vaginal dryness, difficulty with intercourse, genital skin irritation, itching, burning, vaginal pain, bleeding, increased vaginal discharge and an unpleasant odor. In addition, a healthy vaginal microbiome provides immunomodulation and may prevent inflammation and infection. L. vaginalis, normally proliferating in the anaerobic environment of a healthy vagina, produces various antimicrobial compounds such as lactic acid, hydrogen peroxide (H2O2) and bacteriocins and maintains vaginal health.
Lactobacillus-based probiotic capsule: A capsule containing a strain of the probiotic bacterium Lactobacillus with potential antimicrobial and immunomodulatory activities. As a dietary supplement, Lactobacillus, a naturally-occurring bacterium, may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. Because it produces lactic acid and hydrogen peroxide and other substances during fermentation, this bacterium creates an acidic environment that is unfavorable for pathogens. In addition, during colonization of the GI tract, this bacterium adheres to human epithelial cells and forms a protective barrier, thereby preventing the attachment of pathogens. Dietary supplementation with this bacterium has been shown to enhance innate and acquired immunity.
lacutamab: A humanized monoclonal antibody against the immune receptor human killer cell immunoglobulin-like receptor, three domains, long cytoplasmic tail, 2 (KIR3DL2), with potential immunomodulating and antineoplastic activities. Upon administration, lacutamab binds to KIR3DL2 expressed on certain tumor cells. This recruits natural killer (NK) cells and leads to lysis of KIR3DL2-expressing tumor cells. In addition, IPH4102 induces antibody-dependent cellular cytotoxicity (ADCC), thereby further eliminating tumor cells. KIR3DL2, a tumor-associated antigen (TAA) and inhibitory receptor of the KIR family, is specifically expressed in most subtypes of cutaneous T-cell lymphomas (CTCL) and expressed only on a fraction of normal NK cells.
ladarixin sodium: The sodium salt form of ladarixin, an orally bioavailable, small molecule, dual inhibitor of C-X-C motif chemokine receptors 1 (CXCR1) and 2 (CXCR2), with potential anti-inflammatory and antineoplastic activities. Upon oral administration, ladarixin selectively targets and allosterically binds to CXCR 1 and 2, thereby preventing CXCR1 and CXCR2 activation by their ligand and pro-inflammatory chemokine interleukin 8 (IL-8 or CXCL8). This inhibits CXCR1/2-mediated signaling, which inhibits inflammatory processes, reduces both the recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) and neutrophils in the tumor microenvironment (TME), and abrogates the immunosuppressive-induced nature of the TME. This allows effector cells, such as natural killer (NK) cells and cytotoxic T lymphocytes (CTLs), to kill and eliminate cancer cells, and inhibits tumor cell migration, metastasis, angiogenesis and tumor cell proliferation. CXCR1 and 2, G protein-coupled receptor proteins located on myeloid cells and certain tumor cells, play key roles in the immunosuppressive nature of the TME, tumor metastasis, resistance to chemotherapeutic agents and myeloid cell suppression. They also play a key role in inflammation and their expression is elevated in several inflammatory-driven diseases.
ladiratuzumab vedotin: An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed against the anti-solute carrier family 39 zinc transporter member 6 (SLC39A6; LIV-1; ZIP6) protein that is conjugated, via a protease-cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration and internalization by LIV-1-positive tumor cells, ladiratuzumab vedotin undergoes enzymatic cleavage to release MMAE into the cytosol. In turn, MMAE binds to and inhibits tubulin polymerization, which may result in G2/M phase cell cycle arrest and apoptosis in LIV-1-expressing tumor cells. LIV-1, a member of the zinc transporter family, is expressed in several types of solid tumors and plays a key role in tumor cell progression and metastasis. The linkage system in ladiratuzumab vedotin is highly stable in plasma, resulting in cytotoxic specificity against LIV-1-positive cells.
laetrile: Originally, the name laetrile was the contraction of laevo-mandelonitrile glucoside, a cyanogenic glycoside found naturally in some plants. Over the years the meaning of laetrile has changed. There are now preparations called Laetrile where amygdalin is the major constituent. Laetrile and amygdalin are often used interchangeably, but are different agents. Cyanide and benzaldehyde are metabolites of both laetrile and amygdalin. Both metabolites may possess antineoplastic properties. Laetrile has been used as an anticancer treatment in humans worldwide, but scientific evidence does not support its effectiveness. It is not approved for use in the United States.
LAIR-2 fusion protein NC410: A fusion protein of leukocyte-associated immunoglobulin (Ig)-like receptor (LAIR)-2, a high-affinity collagen receptor, with potential immunomodulatory and antineoplastic activities. Upon administration, LAIR-2 fusion protein NC410 binds to the ligand collagen of LAIR-1 (CD305), thereby blocking the binding of LAIR-1 to its ligand collagen and inhibiting LAIR-1-mediated immune suppression. This may result in enhanced T-cell and dendritic cell (DC) activities, and cytotoxic T-lymphocyte (CTL) and anti-tumor immune responses. LAIR-1, a collagen-receptor and an inhibitory immune receptor belonging to the Ig superfamily, is expressed on many peripheral blood mononuclear cells (PBMC) including T cells and DCs.
lamellar body mimetic mouth spray LMS-611: A suspension-based oral spray containing multilamellar lipid vesicles in which the lipids mimic the lipidic composition of endogenous extra-alveolar lamellar bodies, with muco-restorative and protective activity against radiotherapy (RT)-induced xerostomia (RIX). Upon sublingual administration of the lamellar body mimetic LMS-611 using a spray, the lipids in this agent mimic the natural secretions of endogenous lamellar bodies. This makes mucus more fluid and may prevent dryness of the mouth. This restores saliva functions and makes it easier to chew, swallow and talk, and also prevents xerostomia-induced infections, tooth decay and tooth enamel decay. RT decreases saliva secretion by causing the destruction of the parotid and submandibular serous salivary glands and lamellar bodies. This results in thicker and more visco-adhesive saliva, which causes various xerostomia-induced symptoms; intact lamellar bodies maintain the fluidity of mucus and lubricate the mouth.
Lamictal: (Other name for: lamotrigine)
lamivudine: A synthetic nucleoside analogue with activity against hepatitis B virus (HBV) and HIV. Intracellularly, lamivudine is phosphorylated to its active metabolites, lamiduvine triphosphate (L-TP) and lamiduvine monophosphate (L-MP). In HIV, L-TP inhibits HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleoside analogue into viral DNA. In HBV, incorporation of L-MP into viral DNA by HBV polymerase results in DNA chain termination. L-TP is a weak inhibitor of mammalian DNA polymerases alpha and beta, and mitochondrial DNA polymerase.
lamotrigine: A synthetic phenyltriazine with antiepileptic and analgesic properties. Lamotrigine enhances the action of gamma-aminobutyric acid, an inhibitory neurotransmitter, which may result in a reduction of pain-related transmission of signals along nerve fibers. This agent may also inhibit voltage-gated sodium channels, suppress glutamate release, and inhibit serotonin reuptake.
Lamprene: (Other name for: clofazimine)
landogrozumab: A monoclonal antibody against myostatin (MSTN) with potential anti-cachexia activity. Upon administration, landogrozumab binds to and neutralizes the MSTN protein, thereby blocking the MSTN signalling pathway. This may help decrease muscle protein breakdown and muscle weakness and may attenuate cancer cachexia. MSTN, a member of the transforming growth factor-beta (TGF-beta) superfamily, is a negative regulator of muscle growth and development.
Lanoxin: (Other name for: digoxin)
lanraplenib: An orally available inhibitor of spleen tyrosine kinase (Syk), with potential immunomodulating and antineoplastic activities. Upon oral administration, lanraplenib binds to and inhibits the activity of Syk. This inhibits B-cell receptor (BCR) signaling, which leads to the inhibition of B-cell activation, and prevents tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoietic malignancies; it plays a key role in B-cell receptor signaling.
lanreotide acetate: The acetate salt of a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide binds to somatostatin receptors (SSTR), specifically SSTR-2 and also to SSTR-5 with a lesser affinity. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland. Furthermore, lanreotide has an acute effect on decreasing circulating total and free insulin-like growth factor 1 (IGF-I). This agent is usually given as a prolonged-release microparticle or Autogel formulation for the treatment of acromegaly and to relieve the symptoms of neuroendocrine tumors.
lanreotide acetate copolymer microparticles: A prolonged-release depot suspension of microparticles containing the acetate salt of lanreotide, a synthetic peptide analog of the naturally occurring somatostatin, and copolymers. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent has a much longer duration of action than natural somatostatin and is selective towards the inhibition of growth hormone.
Lanreotide Autogel: (Other name for: lanreotide long-acting aqueous gel)
lanreotide long-acting aqueous gel: A long-acting aqueous gel preparation of lanreotide, a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit the release of various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent also decreases circulating total and free insulin-like growth factor 1 (IGF-I). Lanreotide exhibits a high binding affinity for somatostatin receptor 2 (SSTR-2) and a lesser binding affinity for SSTR-5. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland.
lapatinib ditosylate: The ditosylate salt of lapatinib, a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.
lapatinib/letrozole regimen: A regimen consisting of lapatinib and letrozole that is used as a treatment for breast cancer.
lapuleucel-T: A cell-based vaccine targets tumors expressing the HER2/neu marker. HER-2/neu is a growth factor receptor, and its overexpression has been associated with a number of cancers including breast, ovarian, colon and lung cancers. APC8024 comprise of autologous antigen-presenting peripheral blood mononuclear cells (APCs) that have been exposed to HER2/neu protein and can be administered to the patient. These cells may stimulate an antitumor T-cell response to cancer cells expressing HER2/neu.
Laradopa: (Other name for: levodopa)
largetrifoliolious bugbane rhizome supplement: A proprietary tablet formulation containing an extract from Largetrifoliolious Bugbane rhizome (Shengma), the dried root of Cimicifuga sp., with potential use for relieving menopausal symptoms. The Largetrifoliolious bugbane rhizome supplement contains total saponins, including phytoestrogens that can modulate estrogen receptor signaling. This supplement is used to reduce disease symptoms, such as sweating, toothache, headache, ulcers, and insomnia. In women, this supplement may be used to reduce symptoms related to menopause.
Larodopa: (Other name for: levodopa)
laromustine: A sulfonyl hydrazine prodrug with antineoplastic activity. Laromustine releases the DNA chloroethylating agent 90CE after entering the blood stream; 90CE chloroethylates alkylates the 06 position of guanine, resulting in DNA crosslinking, strand breaks, chromosomal aberrations, and disruption of DNA synthesis. Intracellular metabolism of this agent also releases methyl isocyanate which inhibits 06-alkyl-guanine transferase, an enzyme involved with DNA repair.
larotaxel: A semi-synthetic derivative of the taxane 10-deacetylbaccatin III with potential antineoplastic activities. Larotaxel binds to tubulin, promoting microtubule assembly and stabilization and preventing microtubule depolymerization, thereby inhibiting cell proliferation. As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors. Larotaxel penetrates the blood brain barrier.
larotinib mesylate: The mesylate salt form of larotinib, a reversible pan-ErbB inhibitor with potential antineoplastic activity. Upon administration, larotinib binds to and inhibits ErbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing ErbB. The ErbB protein family, also called the epidermal growth factor receptor (EGFR) family, plays major roles in tumor cell proliferation and tumor vascularization.
larotrectinib sulfate: An orally available, tropomyosin receptor kinase (Trk) inhibitor, with potential antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.
lartesertib: An orally bioavailable ATP-competitive inhibitor of ataxia telangiectasia mutated kinase (ATM), with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, lartesertib targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, by preventing DNA damage repair, M4076 sensitizes tumor cells to chemo- and radiotherapy and increases their anti-tumor activity. ATM, a serine/threonine protein kinase upregulated in a variety of cancer cell types, is activated in response to DNA damage and plays a key role in DNA-strand repair.
Lasix: (Other name for: furosemide)
lasmotinib: An orally bioavailable inhibitor of checkpoint kinase 2 (chk2), with potential antineoplastic and chemopotentiating activities. Upon oral administration, lasmotinib binds to and inhibits the activity of chk2, which may prevent the repair of DNA damage caused by DNA-damaging agents. This may result in tumor cell apoptosis and potentiate the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine-threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types.
lasofoxifene: A non-steroidal, naphthalene-derived, third-generation selective estrogen receptor modulator (SERM) with potential antineoplastic and anti-osteoporotic activities. Upon oral administration, lasofoxifene selectively binds to both estrogen receptor alpha (ERalpha; ESR1) and estrogen receptor beta (ERbeta; ESR2) with high affinity and mimics the effects of endogenous estradiol with varying agonist and antagonist effects in ER-expressing tissues. Blockade of ERalpha by lasofoxifene may potentially inhibit estrogen-dependent cancer cell proliferation in ER-expressing cancers. Lasofoxifene may also bind to the certain mutant forms of ERalpha, including the Y537S ESR1 mutant, making it potentially useful in the treatment of tumors that have acquired resistance to other ER-targeting agents.
Laudicon: (Other name for: hydromorphone hydrochloride)
lavender oil: The essential oil extracted from the flowers of several species of Lavandula. Lavender oil is used primarily for its aromatic properties in parfumery, aromatherapy, skincare products, and other consumer products.
laventatug tivedotin: An antibody-drug conjugate (ADC) composed of laventatug, a humanized monoclonal antibody directed against solute carrier family 39 zinc transporter member 6 (SLC39A6; LIV-1; ZIP6) that is conjugated, via a linker, to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration and binding to LIV-1-positive tumor cells, laventatug tivedotin enters the tumor cell lysosome through endocytosis, and releases MMAE. MMAE binds to and inhibits tubulin polymerization, which may result in G2/M phase cell cycle arrest and apoptosis in LIV-1-expressing tumor cells. LIV-1, a multi-pass transmembrane protein and zinc transporter, is expressed in several types of solid tumors and plays a key role in tumor cell progression, proliferation and metastasis. The conjugation method and linkage system prevent MMAE from separating from the antibody during circulation, thereby limiting off target toxicity.
Lazanda: (Other name for: fentanyl citrate pectin-based nasal spray)
Lazcluze: (Other name for: lazertinib mesylate hydrate)
lazertinib mesylate hydrate: The hydrated mesylate salt form of lazertinib, an orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon oral administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, specifically EGFR exon 19 deletions and exon 21 L858R substitution mutations. This prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. In addition, lazertinib penetrates the blood-brain barrier (BBB). As this agent shows minimal activity against wild-type EGFR (wtEGFR), systemic toxicity is minimal as compared to non-selective EGFR inhibitors. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
lead Pb 203 VMT-a-NET: A radioconjugate consisting of the human somatostatin receptor subtype 2 (SSTR2)-targeting peptide and Tyr3-octreotide (TOC) analog VMT-a-NET, in which the N-terminus of TOC is conjugated, via polyethylene glycol (PEG) linkers (PEG2), to the cyclen-based lead-specific chelator PSC and labeled with the gamma-emitting radioisotope lead Pb 203, with potential imaging activity of neuroendocrine tumors (NETs) using single photon emission computed tomography (SPECT)/computed tomography (CT). Upon administration of lead Pb 203 VMT-a-NET, the peptide moiety specifically targets and binds to SSTR2, which is present on the cell membranes of many types of NETs. This allows for visualization of SSTR2-positive cells upon SPECT/CT imaging. SSTR2 is overexpressed on NETs and their metastases while most other normal tissues express low levels of SSTR2.
lead Pb 203-VMT01: A radioconjugate composed of the melanocyte-stimulating hormone receptor (MSHR; melanocortin-1 receptor; MC1R; melanin-activating peptide receptor; melanotropin receptor)-targeting peptide, VMT01, labeled with the radioisotope lead Pb 203, with potential imaging activity using single photon emission computed tomography (SPECT)/computed tomography (CT). Upon administration of lead Pb 203-VMT01, VMT01 targets and binds to MC1R-expressing tumor cells. Upon SPECT/CT imaging, MC1R-expressing tumor cells can be detected. MC1R, a G protein-coupled receptor expressed by melanocytes that binds to melanocortins, is involved in regulating mammalian skin and hair color. It is upregulated on the surface of metastatic melanoma cells.
lead Pb 212 DOTAMTATE: A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated, through a bifunctional, macrocyclic chelating agent DOTAM (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic amide; TCMC), to the alpha-emitting radioisotope lead Pb 212, with potential antineoplastic activity. Upon administration, lead Pb 212 DOTAMTATE targets and binds to somatostatin receptors (SSTRs) present on the cell membranes of most types of neuroendocrine tumor (NET) cells. This allows for the specific delivery of a cytotoxic dose of alpha radiation to SSTR-positive cells. TATE is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NET and their metastases, while most other normal tissues express low levels of SSTRs.
lead Pb 212 pentixather: A radioconjugate composed of pentixather, a chemokine receptor C-X-C chemokine receptor type 4 (CXCR4)-targeting ligand, conjugated to the alpha-emitting radioisotope lead Pb 212, with potential antineoplastic activity. Upon administration, lead Pb 212 pentixather targets and binds to CXCR4-expressing cancer cells. This allows for the specific delivery of a cytotoxic dose of alpha radiation to CXCR4-expressing cancer cells. CXCR4, a marker of poorly differentiated cells, is overexpressed on various cancer cells, and plays a key role in tumor growth, progression, invasiveness and metastasis.
lead Pb 212 TCMC-trastuzumab: A radioimmunoconjugate containing the recombinant humanized monoclonal antibody trastuzumab conjugated with the bifunctional chelating agent TCMC ((1,4,7,10-Tetra-(2-Carbamoyl Methyl)-Cyclododecane), and radiolabeled with the alpha-emitting isotope lead Pb 212, with potential anti-tumor activity. Upon administration, the antibody moiety of lead Pb 212 TCMC-trastuzumab binds with high affinity to the extracellular domain of human epidermal growth factor receptor 2 (HER2); after internalization, the radioisotope moiety delivers a cytotoxic dose of alpha radiation to the HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed on the cell surface of a variety of cancer cell types.
lead Pb 212-DOTAM-GRPR1: A radioconjugate consisting of a gastrin-releasing peptide receptor (GRPR)-targeting antagonist conjugated, through a bifunctional, macrocyclic chelating agent DOTAM (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic amide; TCMC), to the alpha-emitting radioisotope lead Pb 212, with potential antineoplastic activity. Upon administration, lead Pb 212-DOTAM-GRPR1 targets and binds to GRPR-expressing tumor cells. This allows for the specific delivery of a cytotoxic dose of alpha radiation to GRPR-expressing tumor cells. GRPR, also called bombesin receptor 2 (BB2), is a G protein-coupled seven-transmembrane receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers.
lead Pb 212-VMT01: A radioconjugate composed of the melanocyte-stimulating hormone receptor (MSHR; melanocortin-1 receptor; MC1R; melanin-activating peptide receptor; melanotropin receptor)-targeting peptide, VMT01, conjugated to the alpha-emitting radioisotope lead Pb 212, with potential antineoplastic activity. Upon administration, lead Pb 212-VMT01 targets and binds to MC1R-expressing tumor cells. This allows for the specific delivery of a cytotoxic dose of alpha radiation to MC1R-expressing tumor cells. MC1R, a G protein-coupled receptor expressed by melanocytes that binds to melanocortins, is involved in regulating mammalian skin and hair color. It is upregulated on the surface of metastatic melanoma cells.
lebrikizumab: A humanized monoclonal antibody against interleukin 13 (IL-13) with immunosuppressive and anti-asthmatic activities. Lebrikizumab binds to IL-13 and inhibits IL-13-mediated pathways. IL-13, a cytokine mainly secreted by type 2 helper T cells, plays a key role in the induction of allergic inflammation.
ledipasvir: An orally available inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, with potential activity against HCV. Upon oral administration and after intracellular uptake, ledipasvir binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of hepatocellular carcinoma (HCC).
ledipasvir mixture with sofosbuvir: A tablet containing a fixed dose combination of ledipasvir, an inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, and the prodrug sofosbuvir, an inhibitor of HCV NS5B polymerase, with activity against HCV. Upon oral administration of ledipasvir/sofosbuvir and intracellular uptake, ledipasvir binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. Sofosbuvir is converted to its active triphosphate form, and competes with uridine triphosphate for incorporation into RNA, thereby inhibiting NS5B polymerase and preventing viral replication. This may eradicate HCV and prevent HCV-mediated tumorigenesis. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. The HCV NS5B protein, an RNA-dependent RNA polymerase, is essential for the replication of the viral HCV RNA genome. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of certain tumors.
leflunomide: A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation.
lemzoparlimab: A human monoclonal antibody targeting the human cell surface antigen CD47, with potential phagocytosis-inducing and antineoplastic activities. Upon administration, lemzoparlimab preferentially binds to a unique epitope of CD47 on tumor cells. This blocks the interaction of CD47 with signal regulatory protein alpha (SIRPalpha), an inhibitory protein expressed on macrophages and dendritic cells (DCs), which prevents CD47/SIRPalpha-mediated signaling and abrogates the CD47/SIRPalpha-mediated inhibition of phagocytosis. This induces pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related protein (LRP), expressed on macrophages, which results in macrophage activation and the specific phagocytosis of tumor cells. Additionally, blocking CD47 signaling activates an anti-tumor T-lymphocyte immune response and T-cell-mediated killing of CD47-expressing tumor cells. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic stem cells (HSCs) and overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRPalpha, leads to the inhibition of macrophage activation and protects cancer cells from phagocytosis, which allows cancer cells to proliferate. TJC4, compared to other anti-CD47 monoclonal antibodies, is designed to minimize inherent binding to normal red blood cells (RBCs), which may results in a more advantageous hematologic safety profile.
lenalidomide: A thalidomide analog with potential antineoplastic activity. Lenalidomide inhibits TNF-alpha production, stimulates T cells, reduces serum levels of the cytokines vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF), and inhibits angiogenesis. This agent also promotes G1 cell cycle arrest and apoptosis of malignant cells.
lenalidomide analog KPG-121: A lenalidomide analog with potential anti-angiogenic and immunomodulatory activities. Upon oral administration, lenalidomide analog KPG-121 may inhibit tumor necrosis factor alpha (TNF-alpha) production, stimulate T-lymphocytes, reduce serum levels of vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF; FGF2), and inhibit angiogenesis. Additionally, KPG-121 may promote G1 cell cycle arrest and induce apoptosis in malignant cells.
lenalidomide prolonged-release formulation NEX-20A: A prolonged-release formulation composed of a suspension of the thalidomide analog lenalidomide coated with slow-dissolving nontoxic inorganic oxides, with potential antineoplastic activity. Upon administration via subcutaneous injection, the coating dissolves and lenalidomide is released. Lenalidomide inhibits tumor necrosis factor alpha (TNF-alpha) production, stimulates T lymphocytes, reduces serum levels of vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF; FGF2), and inhibits angiogenesis. Additionally, lenalidomide promotes G1 cell cycle arrest and induces apoptosis in malignant cells.
lenapenem: A broad-spectrum, carbapenem antibiotic with bactericidal activity. Lenapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. This inhibition weakens the bacterial cell wall and leads to lytic cell death in a wide range of Gram-positive and Gram-negative aerobic and anaerobic pathogens.
lenograstim: A glycosylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions.
Lenti-D/ABCD1-transduced autologous hematopoietic stem cells: Autologous CD34+ hematopoietic stem cells transduced with Lenti-D lentiviral vector encoding the human ATP-binding cassette, sub-family D, member 1 (ABCD1) cDNA, for the potential treatment of childhood cerebral adrenoleukodystrophy (CCALD). Upon administration of the lenti-D/ABCD1-transduced autologous hematopoietic stem cells, the cells proliferate, and some travel to the brain and differentiate into microglial cells. The expressed ABCD1 restores the function of ALD protein (ALDP) and aids in the treatment of CCALD. In CCALD, the ABCD1 gene is mutated, leading to the inability of patients to metabolize very long chain fatty acids in cells of the brain.
LentiGlobin BB305 Drug Product: (Other name for: betibeglogene autotemcel)
LentiGlobin BB305 lentiviral vector-transduced autologous SCD CD34+ hemaptopoietic stem cells bb1111: A preparation of autologous, CD34-positive hematopoietic stem cells (HSCs), obtained from patients with sickle cell disease (SCD), transduced ex vivo with the BB305 recombinant replication-defective, self-inactivating lentiviral vector (LVV) encoding for an engineered, modified form of human beta-globin (hemoglobin-beta, HBB) gene, beta-A-T87Q (b-A-T87Q), in which the threonine (Thr; T) at position 87 has been substituted with glutamine (Gln; Q), with potential to restore beta-globin expression and function in SCD patients. Autologous CD34-positive stem cells are isolated from the patient's own bone marrow and the cells are transduced with the lentiviral vector. Upon re-infusion of autologous bb1111 back into the patient, these cells express the non-sickling b-A-globin protein b-A-T87Q-globin, thereby allowing the body to make anti-sickling hemoglobin, HbA-T87Q, and thus normal, healthy red blood cells (RBCs). Beta-globin, the beta-chain of the most common form of hemoglobin, is encoded by the HBB gene; mutations in this gene prevent normal beta-globin production and are associated with SCD. The b-A-T87Q form of beta-globin has increased anti-sickling activity compared to the wild type protein.
lentivirus vector CCR5 shRNA/TRIM5alpha/TAR decoy-transduced autologous CD34-positive hematopoietic progenitor cells: Autologous, CD34-positive hematopoietic progenitor cells (HPCs) transduced with a lentiviral vector encoding three anti-human immunodeficiency virus (HIV) genes: a short hairpin RNA (shRNA) that targets human chemokine receptor 5 (CCR5), a human/rhesus macaque chimeric tripartite motif-containing protein 5 alpha isoform (TRIM5alpha), and a TAT activation response (TAR) decoy, as well as a pre-selective cell-surface marker, which is a truncated and mutated form of human CD25, used to potentially provide resistance against human immunodeficiency virus (HIV) infection. Human autologous CD34-positive HPCs are isolated and transduced ex vivo with the lentiviral vector. Upon pre-selection, purification using CD25 immunomagnetic separation, and subsequent administration of effectively transduced HPCs, the HPCs display 3 separate mechanisms of action against HIV infection: CCR5 shRNA binds to CCR5 mRNA and inhibits the expression of CCR5, a HIV-1 co-receptor that mediates HIV attachment and host cell entry; TRIM5alpha prevents HIV genome integration upon cell entry; and the TAR decoy binds to the HIV TAT protein and prevents TAT-dependent viral gene transcription, thereby preventing HIV replication. Upon transfer of the lentivirus vector CCR5 shRNA/TRIM5alpha/TAR decoy-transduced autologous CD34-positive HPCs into the patient, the HPCs are resistant to HIV entry and replication and could provide long-term protection against both HIV infection and HIV-associated cancers.
lentivirus vector rHIV7-shI-TAR-CCR5RZ-transduced hematopoietic progenitor cells: Autologous, CD34-positive hematopoietic progenitor cells (HPCs) transduced with rHIV7-shI-TAR-CCR5RZ, a lentiviral vector encoding three anti-human immunodeficiency virus (HIV) RNA genes, with potential antineoplastic activity. The 3 RNA products produced by the lentilvirus are: a short hairpin RNA (shRNA) targeted to an exon of the HIV-1 genes tat/rev, designated as shI; a decoy for the HIV TAT reactive element, designated as TAR; a ribozyme targeting the host cells CCR5 chemokine receptor, designated as CCR5RZ. Upon administration, lentivirus vector rHIV7-shI-TAR-CCR5RZ-transduced hematopoietic progenitor cells expressing the 3 species of RNAs display 3 seperate mechanims of action: the shRNA blocks the transcription of tat/rev, the TAR decoy binds to the TAT protein that is essential for HIV replication, and CCR5RZ catalyzes CCR5 which is needed for viral attachment and entry into the host cells. Altogether, infusion of these HPCs may ultimately inhibit HIV replication and suppress HIV infection.
lenumlostat: An orally available, small-molecule, irreversible inhibitor of lysyl oxidase homolog 2 (lysyl oxidase-like protein 2; LOXL2) with potential antifibrotic activity. Upon oral administration, the aminomethyl pyridine moiety of lenumlostat interacts with the active site of LOXL2 to form a pseudo-irreversible inhibitory complex, thereby inhibiting the catalytic activity of LOXL2. LOXL2, a secreted glycoprotein, catalyzes the post-translational oxidative deamination of lysine residues on target proteins, including collagen and elastin, leading to the formation of deaminated lysine (allysine). Condensation with other allysines or lysines drives the formation of inter- and intramolecular cross-linkages that impact remodeling of the extracellular matrix (ECM), potentially leading to fibrosis. Inhibition of LOXL2, which is often upregulated in fibrotic tissue, may reduce fibrosis in certain chronic fibrotic diseases.
lenvatinib mesylate: A synthetic, orally available inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR/FLK-1) tyrosine kinase with potential antineoplastic activity. Lenvatinib mesylate blocks VEGFR2 activation by VEGF, resulting in inhibition of the VEGF receptor signal transduction pathway, decreased vascular endothelial cell migration and proliferation, and vascular endothelial cell apoptosis.
Lenvima: (Other name for: lenvatinib mesylate)
lenzilumab: A recombinant monoclonal antibody against the cytokine granulocyte macrophage colony-stimulating factor (GM-CSF), with potential immunomodulating activity. Upon administration, lenzilumab binds to and neutralizes GM-CSF. This prevents GM-CSF binding to the GM-CSF receptor, which is a heterodimeric protein expressed on myeloid progenitor cells, and prevents GM-CSF-mediated signaling. This may induce apoptosis in and inhibit proliferation of cancer cells that overproduce GM-CSF. GM-CSF plays a key role in the differentiation and proliferation of monocytes, macrophages and granulocytes; elevated levels of GM-CSF are associated with certain autoimmune diseases, inflammatory diseases, and cancers.
LEP-ETU: (Other name for: paclitaxel liposome)
lepirudin: A yeast cell-derived recombinant polypeptide related to the naturally occurring, leech-derived anticoagulant hirudin. Lepirudin directly binds to and inactivates thrombin, producing dose-dependent increases in the activated partial thromboplastin time (aPTT) and prothrombin time (PT). The mechanism of action of this agent is independent of antithrombin III and is not inhibited by platelet factor 4. Natural hirudin, a family of highly homologous isopolypeptides, is produced in trace amounts by the leech Hirudo medicinalis.
lerapolturev: A recombinant, live attenuated, nonpathogenic oncolytic virus containing the oral poliovirus Sabin type 1 in which the internal ribosomal entry site (IRES) is replaced with the IRES from human rhinovirus type 2 (HRV2), with potential antineoplastic activity. Upon administration of lerapolturev, the poliovirus is selectively taken up by and replicates in tumor cells expressing CD155 (poliovirus receptor, PVR or NECL5) eventually causing tumor cell lysis. Following the lysis of infected cells, the replicated virus is released and can infect adjacent cells, which both induces further tumor cell oncolysis and may activate, through the release of tumor-associated antigens (TAAs) and inflammatory mediators from the lysed tumor cells, the immune system to mount an anti-tumor immune response. This further kills tumor cells. This may also stimulate long-term anti-tumor immunity. Additionally, lerapolturev can induce a systemic anti-tumor immune response through engagement with antigen-presenting cells (APCs) upon CD155 binding thereby further killing tumor cells. CD155, an oncofetal cell adhesion molecule and tumor antigen, is ectopically expressed in certain cancers, such as glioblastoma multiforme (GMB), and plays an important role in tumor cell migration, invasion, and metastasis. Due to the heterologous HRV2 IRES in this recombinant virus, lerapolturev only propagates in susceptible CD155-expressing, nonneuronal neoplastic cells.
leridistim: A recombinant chimeric dual G-CSF and IL-3 receptor agonist. Leridistim binds with high affinity to both the interleukin-3 (IL-3) and granulocyte colony-stimulating factor (G-CSF) receptors, thereby stimulating the production and maturation of neutrophils, platelets, and lymphocytes after chemotherapy.
leriglitazone: An orally bioavailable, blood-brain-barrier (BBB) penetrable, selective peroxisome proliferator-activated receptor (PPAR) subtype gamma agonist, with potential neuroprotective activity that could be used for certain central nervous system (CNS) diseases, such as adrenomyeloneuropathy, cerebral adrenoleukodystrophy (cALD), Friedreich's ataxia, and certain other CNS diseases. Upon oral administration, leriglitazone selectively targets, binds to and activates PPARgamma, thereby regulating the expression of genes involved in mitochondrial biogenesis. This modulates pathways leading to the restoration of mitochondrial function in which dysfunction is caused by the accumulation of very long-chain fatty acids (VLCFAs), and increases energy production, decreases oxidative stress, decreases nuclear factor kappa B (NF-kB) levels, inhibits neuroinflammation, protects the BBB integrity, prevents demyelination and axonal degeneration, increases neuronal survival, increases myelination and oligodendrocyte survival and improves motor function. Mutations in the ABCD1 gene, which encodes the peroxisomal membrane adrenoleukodystrophy protein, cause a defective function of the ABCD1 transporter leading to an accumulation of VLCFA. VLCFA accumulation contributes to membrane destabilization of the myelin sheath, mitochondrial dysfunction, oxidative stress, neuroinflammation and compromised BBB integrity.
lerisetron: The hydrochloride salt of a 2-piperazinylbenzimidazole-derivative serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting.
lerociclib: An orally bioavailable inhibitor of cyclin-dependent kinase (CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon administration, lerociclib selectively inhibits CDK4 and CDK6, which inhibits the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase, prevents CDK-mediated G1-S phase transition and leads to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of both cell cycle progression from the G1-phase into the S-phase and tumor cell proliferation.
leronlimab: A humanized immunoglobulin (Ig) G4 monoclonal antibody against CC chemokine receptor 5 (CCR5; CD195), with potential activity as a human immunodeficiency virus (HIV) entry blocker and potential protective activity against graft-versus-host disease (GvHD). Upon administration, leronlimab targets and binds to CCR5 expressed on T cells. This blocks HIV cell entry, which prevents HIV infection and/or reduces HIV viral load. In addition, blocking CCR5 by PRO 140 decreases CCR5-mediated signaling and the CCR5-induced migration of donor cells into tissues after an allogeneic hematopoietic cell transplantation (HCT). Blocking CCR5 may therefore prevent or reduce GvHD. CCR5, a co-receptor needed for HIV cell entry, plays a key role in immunomodulation. Expressed on monocytes, activated T cells and dendritic cells (DCs), CCR5 can regulate chemotaxis. Lymphocyte trafficking via chemokine receptors, such as CCR5, and recruitment to target organs, plays a critical role in alloreactive responses.
Lescol: (Other name for: fluvastatin sodium)
Lessina: (Other name for: ethinyl estradiol/levonorgestrel)
lestaurtinib: An orally bioavailable indolocarbazole derivative with antineoplastic properties. Lestaurtinib inhibits autophosphorylation of FMS-like tyrosine kinase 3 (FLT3), resulting in inhibition of FLT3 activity and induction of apoptosis in tumor cells that overexpress FLT3.
letermovir: An orally bioavailable, non-nucleoside, 3,4-dihydroquinazolinyl acetic acid and inhibitor of the pUL56 subunit of the viral terminase complex of cytomegalovirus (CMV), with potential CMV-specific antiviral activity. Upon oral administration, letermovir binds to the pUL56 subunit of the viral terminase complex of CMV and prevents the cleavage of concatemeric DNA into monomeric genome length DNA. As this agent interferes with viral DNA processing and subsequent viral DNA packaging into procapsids, CMV replication is blocked and CMV infection is prevented.
letetresgene autoleucel: Human autologous T lymphocytes transduced with a lentiviral vector encoding a T-cell receptor (TCR) specific for the cancer-testis antigens (CTAs) NY-ESO-1 and L antigen family member 1 (LAGE-1; Cancer/Testis Antigen 2; CTAG2; CT2), with potential antineoplastic activity. Following leukapheresis, isolation of lymphocytes, expansion ex vivo, transduction, and reintroduction into the patient, letetresgene autoleucel specifically target and bind to NY-ESO-1/LAGE-1-overexpressing tumor cells. This may result in a cytotoxic T-lymphocyte (CTL)-mediated elimination of NY-ESO-1/LAGE-1-positive cancer cells. NY-ESO-1 and LAGE-1, members of the cancer-testis antigen (CTA) family, are overexpressed on the surface of various tumor cell types.
letrozole: A nonsteroidal inhibitor of estrogen synthesis with antineoplastic activity. As a third-generation aromatase inhibitor, letrozole selectively and reversibly inhibits aromatase, which may result in growth inhibition of estrogen-dependent breast cancer cells. Aromatase, a cytochrome P-450 enzyme localized to the endoplasmic reticulum of the cell and found in many tissues including those of the premenopausal ovary, liver, and breast, catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis.
letrozole/palbociclib regimen: A regimen consisting of letrozole and palbociclib that can be used in the treatment of breast cancer.
leucine-enhanced essential amino acid dietary supplement: An orally bioavailable leucine enriched essential amino acid dietary supplement with potential anti-cachexia activity. Leucine-enhanced essential amino acid nutritional supplement may stimulate the mammalian target of rapamycin (mTOR) signaling pathway, which may promote protein synthesis in muscle cells. Although the exact mechanism by which leucine and other essential amino acids stimulate mTOR has yet to be fully elucidated, leucine may stimulate mTOR by inhibiting adenosine monophosphate protein kinase (AMPK), which negatively controls mTOR signaling.
leucovorin calcium: An active metabolite of folic acid (also called folinic acid and citrovorum factor), which does not require metabolism by dihydrofolate reductase, the molecular target of folate antagonist-type chemotherapeutic drugs. Leucovorin calcium counteracts the toxic effects of these medications, 'rescuing' the patient while permitting the antitumor activity of the folate antagonist. This agent also potentiates the effects of fluorouracil and its derivatives by stabilizing the binding of the drug's metabolite to its target enzyme, thus prolonging drug activity.
leukemic apoptotic corpse-pulsed autologous dendritic cells: A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with corpses of apoptotic leukemic cells, with potential immunostimulatory and antineoplastic activities. Upon vaccination, autologous dendritic cells pulsed with leukemic apoptotic corpse may activate the immune system to mount an anti-tumoral cytotoxic T-lymphocyte (CTL) response against leukemic cells expressing leukemia-associated antigens, which may result in leukemic cell lysis and inhibition of tumor cell growth. Apoptotic tumor cell corpses contain an array of tumor associated antigens (TAAs).
Leukeran: (Other name for: chlorambucil)
Leukine: (Other name for: sargramostim)
leuprolide acetate: The acetate salt of a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors. Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. This agent reduces testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression.
leuprolide acetate for injectable suspension TOL2506: A subcutaneous injectable suspension formulation containing the acetate salt form of leuprolide, a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH), with potential antineoplastic activity. Upon subcutaneous administration of the leuprolide acetate for injectable suspension TOL2506, leuprolide binds to and activates the gonadotropin-releasing hormone receptor (GnRHR). The continuous stimulation of GnRHR by leuprolide results in both the desensitization of pituitary GnRHR and the inhibition of pituitary secretion of the gonadotropins follicle stimulating hormone (FSH) and luteinizing hormone (LH). In males, this results in a significant decline in testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression. In females, this decreases estradiol production and level, suppresses ovarian function and may inhibit proliferation of estrogen receptor (ER)-positive breast cancer.
leuprolide acetate sustained-release microspheres PT105: A sustained-release (SR) injectable microsphere formulation composed of the acetate salt of leuprolide, a synthetic, long-acting nonapeptide analog of the endogenous hormone gonadotropin-releasing hormone (GnRH), with potential antineoplastic activity. Upon administration, leuprolide binds to and activates the gonadotropin-releasing hormone receptor (GnRHR). The continuous stimulation of GnRHR by leuprolide results in both the desensitization of pituitary GnRHR and the inhibition of pituitary secretion of the gonadotropins follicle stimulating hormone (FSH) and luteinizing hormone (LH). In females, prolonged administration results in a decrease in estradiol production and suppression of ovarian function. Leuprolide also reduces testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression.
leuprolide mesylate: The mesylate salt form of leuprolide, a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH), with potential antineoplastic activity. Upon administration, leuprolide binds to and activates the gonadotropin-releasing hormone receptor (GnRHR). The continuous stimulation of GnRHR by leuprolide results in both the desensitization of pituitary GnRHR and the inhibition of pituitary secretion of the gonadotropins follicle stimulating hormone (FSH) and luteinizing hormone (LH). In males, this results in a significant decline in testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression.
Leuvectin: (Other name for: IL-2 plasmid DNA/lipid complex)
levamisole hydrochloride: The orally bioavailable hydrochloride salt of the synthetic imidazothiazole derivative levamisole with anthelminthic and immunostimulating activities. In immunosuppressed states, levamisole may restore immune function by: 1) stimulating antibody formation, 2) stimulating T-cell activation and proliferation, 3) potentiatiating monocyte and macrophage phagocytosis and chemotaxis and 4) increasing neutrophil mobility, adherence, and chemotaxis.
Levaquin: (Other name for: levofloxacin)
levetiracetam: A pyrrolidine with antiepileptic activity. The exact mechanism through which levetiracetam exerts its effects is unknown but does not involve inhibitory and excitatory neurotransmitter activity. Stereoselective binding of levetiracetam was confined to synaptic plasma membranes in the central nervous system with no binding occurring in peripheral tissue. Levetiracetam inhibits burst firing without affecting normal neuronal excitability, which suggests that it may selectively prevent hyper-synchronization of epileptiform burst firing and propagation of seizure activity.
Levitra: (Other name for: vardenafil hydrochloride)
Levlite: (Other name for: ethinyl estradiol/levonorgestrel)
levobupivacaine hydrochloride: The hydrochloride salt of levobupivacaine, an amide derivative with anesthetic property. Levobupivacaine reversibly binds voltage-gated sodium channels to modulate ionic flux and prevent the initiation and transmission of nerve impulses (stabilizing neuronal membrane), thereby resulting in analgesia and anesthesia. In comparison with racemic bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action.
levocarnitine: An amino acid derivative. Levocarnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain.
levocetirizine dihydrochloride: The dihydrochloride salt form of the active levorotatory enantiomer of cetirizine, levocetirizine; a third generation, non-sedating, selective histamine H1 receptor antagonist, with antihistamine, anti-inflammatory and potential anti-angiogenic activities. Levocetirizine competes with endogenous histamine for binding at peripheral H1-receptor sites on the effector cell surface. This prevents the negative symptoms associated with histamine release and an allergic reaction. In addition, as histamine plays an important role in angiogenesis during an allergic inflammatory reaction, blocking the action of histamine may modulate the expression of proangiogenic factors and thus may prevent angiogenesis. As a third-generation histamine H1 receptor antagonist, levocetirizine has fewer side effects than most second-generation antihistamines.
levodopa: An amino acid precursor of dopamine with antiparkinsonian properties. Levodopa is a prodrug that is converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. When in the brain, levodopa is decarboxylated to dopamine and stimulates the dopaminergic receptors, thereby compensating for the depleted supply of endogenous dopamine seen in Parkinson's disease. To assure that adequate concentrations of levodopa reach the central nervous system, it is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, thereby diminishing the decarboxylation and inactivation of levodopa in peripheral tissues and increasing the delivery of dopamine to the CNS.
levofloxacin: A broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Levofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth.
levoketoconazole: An orally available levorotary enantiomer of ketoconazole with potential steroidogenesis inhibitory activity. Following oral administration, levoketoconazole inhibits three cytochrome P450 family enzymes involved in glucocorticoid biosynthesis, 11beta-hydroxylase (CYP11B1), 17alpha-hydroxylase/17,20-lyase (CYP17A1) and steroid 21-hydroxylase (CYP21A2), which reduces the circulating levels of glucocorticoids. Therefore, this agent may normalize the high concentration of cortisol in the blood seen in patients with Cushing syndrome. Compared to racemic ketoconazole, the levo form is a more potent inhibitor of glucocorticoid synthesis. Additionally, this enantiomer is less likely to inhibit cholesterol 7alpha-hydroxylase (CYP7A1); therefore, its use may reduce the risk of hepatoxicity. Cushing syndrome is caused by high levels of cortisol in the blood either due to excessive production and secretion of corticosteroids, which is often the result of adrenocorticotropic hormone (ACTH)-secreting pituitary or adrenocortical neoplasms, or the use of synthetic corticosteroids.
levoleucovorin calcium: A levo isoform of leucovorin calcium with antineoplastic activity. Levoleucovorin is an active metabolite of folic acid, which does not require metabolism by dihydrofolate reductase. This agent counteracts the toxic effects of other folic acid derivative agents, rescuing the patient while permitting the antitumor activity of the folate antagonist. This agent also potentiates the effects of fluorouracil and its derivatives by stabilizing the binding of the drug's metabolite to its target enzyme, thus prolonging drug activity.
levonantradol: A synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) with antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2.
levonorgestrel: The levorotatory form of norgestrel and synthetic progestogen with progestational and androgenic activity. Levonorgestrel binds to the progesterone receptor in the nucleus of target cells, thereby stimulating the resulting hormone-receptor complex, initiating transcription, and increasing the synthesis of certain proteins. This results in a suppression of luteinizing hormone (LH) activity and an inhibition of ovulation, as well as an alteration in the cervical mucus and endometrium.
levonorgestrel-releasing intrauterine system: A long-acting, hormone-releasing, intrauterine device consisting of a small, T-shaped, polyethylene frame and a reservoired synthetic progesterone with progestational and potential antineoplastic activities. After insertion of this system into the uterus, the device slowly and gradually releases the hormone. Levonorgestrel acts by binding to the progesterone receptor in the nuclei of target cells, resulting in transcription activation and an alteration in protein synthesis. Subsequently, luteinizing hormone (LH) activity and ovulation are suppressed. Levonorgestrel may also exhibit antiproliferative activity in endometrial tissue.
Levopa: (Other name for: levodopa)
Levora: (Other name for: ethinyl estradiol/levonorgestrel)
Levothroid: (Other name for: levothyroxine sodium)
levothyroxine sodium: The sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects.
Levulan Kerastick: (Other name for: aminolevulinic acid hydrochloride)
Lexapro: (Other name for: escitalopram oxalate)
lexaptepid pegol: A proprietary 44-nucleotide L-stereoisomer RNA oligonucleotide conjugated to a 40 kDa polyethylene glycol (PEG) that targets hepcidin with potential anti-anemic activity. Upon intravenous or subcutaneous administration, lexaptepid pegol binds to hepcidin and prevents it from binding to the iron channel ferroportin, located on the basolateral surface of gastrointestinal enterocytes and the plasma membrane of macrophages. This prevents hepcidin-induced internalization and degradation of ferroportin, thus decreasing macrophage iron retention. In turn, binding of NOX-H94 to hepcidin normalizes plasma iron levels and increases erythropoiesis. This may inhibit anemia caused by inflammation. Hepcidin, a peptide hormone that plays a key role in the homeostasis of systemic iron, is upregulated during acute and chronic inflammation in response to cytokines. The unique mirror-image configuration of this agent renders it resistant to hydrolysis and shows a low antigenicity profile. Pegylation increases the half-life of this agent.
lexatumumab: A fully human monoclonal agonistic antibody directed against tumor necrosis factor-alpha (TNF-alpha)-related apoptosis-inducing ligand receptor-2 (TRAIL-R2) with potential antitumor activity. Mimicking the natural ligand TRAIL, lexatumumab binds to and activates TRAIL-R2, which may trigger apoptosis in and inhibit the growth of TRAIL-R2-expressing tumor cells. TRAIL-R2, also known as death receptor 5 (DR5), is a member of the TNF receptor family and is expressed on many malignant cell types.
lexibulin: An orally bioavailable small-molecule with tubulin-inhibiting, vascular-disrupting, and potential antineoplastic activities. Lexibulin inhibits tubulin polymerization in tumor blood vessel endothelial cells and tumor cells, blocking the formation of the mitotic spindle and leading to cell cycle arrest at the G2/M phase; this may result in disruption of the tumor vasculature and tumor blood flow, and tumor cell death.
Lexiscan: (Other name for: regadenoson)
Lialda: (Other name for: mesalamine)
liarozole fumarate: The orally active fumarate salt of the benzimidazole derivative liarozole with potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, resulting in an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. This agent also inhibits aromatase, the enzyme that catalyzes the final, rate-limiting step in estrogen biosynthesis.
Libtayo: (Other name for: cemiplimab-rwlc)
licartin: An immunoradioconjugate containing metuximab, an antibody fragment targeting the hepatocellular cancer (HCC)-associated antigen HAb18G/CD147, that is conjugated to the radioisotope iodine I 131, with potential antineoplastic activity. Upon administration, the metuximab moiety of licartin targets and binds to HAb18G/CD147 on HCC cells; upon internalization, the radioisotope I 131 delivers a cytotoxic dose of gamma radiation, thereby causing selective destruction of HAb18G/CD147-expressing cells. HAb18G/CD147, a member of CD147 family, is overexpressed in HCC and fibroblasts and its expression is associated with cancer cell progression and increased adhesion, invasion and metastasis.
licochalcone A: A derivative of the phenol chalconoid, found in and extracted from the roots of Glycyrrhiza species G. glabra and inflata, with potential anti-inflammatory, antibacterial, and anticancer activities. Upon administration, licochalcone A inhibits the phosphatidylinositol-3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) signaling pathway and inhibits the activity of c-Jun N-terminal kinase 1 (JNK-1), a member of the mitogen-activated protein kinase (MAPK) family that plays a role in the MAPK-mediated signaling pathway. Inhibition of the PI3K/Akt/mTOR- and MAPK-signaling pathways induces cell cycle arrest and apoptosis, decreases migration and invasion of cancer cells, and inhibits tumor cell proliferation. Licochalcone A also prevents the production of reactive oxygen species (ROS), and reduces oxidative stress through the nuclear factor-erythroid 2-related factor 2 (Nrf2) pathway.
licogliflozin: An inhibitor of the sodium-dependent glucose co-transporter (sodium-glucose transporter; sodium-glucose transport protein; sodium-glucose linked transporter; SGLT) family members 1 and 2 (SGLT1/2) with antihyperglycemic activity. By binding to and blocking SGLT1/2, licogliflozin suppresses the reabsorption of glucose in the proximal tubule within the kidneys and enhances urinary excretion of glucose. This normalizes blood glucose levels. SGLT1/2, parts of a transport system expressed in the proximal renal tubules, mediate the majority of renal glucose reabsorption from tubular fluid.
licorice: An herbal extract derived from the root of the plant Glycyrrhiza glabra with potential anti-inflammatory, antioxidant, and antineoplastic activities. Licorice root extract contains glycoside glycyrrhizinic acid and numerous flavonoids. Glycyrrhizinic acid in licorice root extract is hydrolyzed to glycyrrhetic acid (GA); GA inhibits 11 beta-hydroxysteroid dehydrogenase, resulting in inhibition of the conversion of cortisol to the inactive steroid cortisone and elevated cortisol levels. In addition, GA inhibits 17,20-lyase and 17 beta-hydroxysteroid dehydrogenase, resulting in decreased conversions of 17-hydroxyprogesterone to androstenedione and androstenedione to testosterone. The primary antioxidant found in licorice root, the flavonoid glabridin, may inactivate or inhibit the activities of some cytochrome P450 enzymes. In tumor cells, beta-hydroxy-DHP, another flavonoid, may induce Bcl-2 phosphorylation, apoptosis, and G2/M cell cycle arrest.
Lidex: (Other name for: fluocinonide cream)
lidocaine hydrochloride: The hydrochloride salt form of lidocaine, an aminoethylamide and a prototypical member of the amide class anesthetics. Lidocaine interacts with voltage-gated Na+ channels in the nerve cell membrane and blocks the transient increase in permeability of excitable membranes to Na+. This prevents the generation and conduction of nerve impulses and produces a reversible loss of sensation. Lidocaine hydrochloride also exhibits class IB antiarrhythmic effects. The agent decreases the flow of sodium ions into myocardial tissue, especially on the Purkinje network, during phase 0 of the action potential, thereby decreasing depolarization, automaticity and excitability.
lidocaine hydrochloride ophthalmic gel: An ophthalmic gel formulation containing the synthetic amide-type anesthetic lidocaine, with potential analgesic activity. Upon ophthalmic application, the active ingredient lidocaine binds to and blocks voltage-gated sodium channels in neuronal cell membranes. Lidocaine-mediated stabilization of neuronal membranes inhibits the initiation and conduction of nerve impulses, which numbs the nerves, prevents the trigemino-cardiac reflex and produces a reversible local anesthesia.
lidocaine mixture with tribenoside: A formulation composed of the local anesthetic lidocaine and the vasoprotective agent tribenoside that can be used for the treatment of hemorrhoids. Upon rectal administration of the lidocaine mixture with tribenoside, lidocaine stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the ionic fluxes required for the initiation and conduction of impulses. This causes local anesthesia and relieves pain. Tribenoside may exert anti-inflammatory, mild analgesic, wound-healing, fibrinolysis-promoting, membrane-stabilizing and venotropic properties. This may relieve pain, halt inflammation, protect blood vessels, and may help repair and heal wounds.
lidocaine patch 5%: A transdermal patch containing a 5 percent aqueous base solution of the synthetic amide-type anesthetic lidocaine with analgesic activity. Upon topical application and transdermal delivery, the active ingredient lidocaine binds to and blocks voltage-gated sodium channels in the neuronal cell membrane; lidocaine-mediated stabilization of neuronal membranes inhibits the initiation and conduction of nerve impulses and produces a reversible local anesthesia.
lidocaine topical: A synthetic aminoethylamide with local anesthetic activity applied topically to either the skin or mucous membranes. Lidocaine stabilizes the neuronal cell membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the initiation and conduction of nerve impulses and producing a reversible loss of sensation.
Lidoderm: (Other name for: lidocaine patch 5%)
Life-Mel: (Other name for: honey-based nutritional supplement)
Life-Mel Honey: (Other name for: honey-based nutritional supplement)
lifileucel: A preparation of autologous tumor infiltrating lymphocytes (TILs), with potential antineoplastic activity. TILs are isolated from a patient's tumor tissue, cultured in vitro with high-dose interleukin-2 (lL-2), further selected based on antigen specificity and tumor reactivity, and the selected TILs are subsequently expanded. Upon re-introduction of lifileucel into the patient, the TILs re-infiltrate the tumor, specifically recognize the tumor-associated antigens (TAAs), and initiate tumor cell lysis. IL-2 induces the proliferation and expansion of TILs in vitro.
ligand directed degrader BMS-986460: A ligand directed degrader (LDD) composed of an E3 ubiquitin ligase-binding moiety that is conjugated, via a linker, to an as of yet undisclosed moiety that targets a prostate specific tumor-associated antigen (TAA), with potential antineoplastic activity. Upon administration, LDD BMS-986460 specifically and simultaneously targets and binds to the TAA on prostate tumor cells and to E3 ubiquitin ligase, thereby creating a ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation of the TAA. This prevents TAA-mediated signaling and leads to an inhibition of the growth of tumor cells that overexpress the unidentified TAA.
lignin-derived polyphenolic composition with ammonium molybdate BP-C2: An orally bioavailable solution containing lignin-derived benzene-polycarboxylic acids mixed with ammonium molybdate, with potential use as an adjuvant and with potential radioprotective and regenerative activities. Upon oral administration, lignin-derived polyphenolic composition with ammonium molybdate BP-C2 is also able to stimulate the innate immune system and upregulates a variety of cytokines including interferon (IFN), tumor necrosis factor-alpha (TNF-alpha), granulocyte macrophage-colony stimulating factor (GM-CSF), and various interleukins (ILs) such as IL-6, IL-22 and IL-25, and induces the production of innate lymphoid cells. BP-C2 stimulates the production of intestinal epithelial cells thereby protecting the gastrointestinal (GI) tract against GI-induced cytotoxic side effects caused by certain anti-tumor agents. Additionally, BP-C2 scavenges free radicals, inhibits lipid oxidation, and protects cells against radiation-induced damage. Molybdenum, an essential micronutrient, acts as a cofactor in multiple detoxification system enzymes. BP-C2 may also stimulate the production of hematopoietic progenitor cells, thereby correcting hematological abnormalities such as anemia, thrombocytopenia and neutropenia, which are also caused by certain anti-cancer agents.
ligufalimab: A humanized immunoglobulin G4 (IgG4) monoclonal antibody targeting leukocyte surface antigen CD47, with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, ligufalimab targets and binds to CD47 expressed on tumor cells, blocking the interaction of CD47 with signal regulatory protein alpha (SIRPa) expressed on phagocytic cells. This prevents CD47/SIRPa-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of macrophage activation and phagocytosis of cancer cells. This induces pro-phagocytic signaling mediated by the binding of calreticulin (CRT), which is specifically expressed on the surface of tumor cells, to low-density lipoprotein (LDL) receptor-related protein-1 (LRP-1), which is expressed on macrophages, and results in macrophage activation and the specific phagocytosis of tumor cells. CD47, also called integrin-associated protein (IAP), is a tumor-associated antigen (TAA) expressed on normal, healthy hematopoietic stem cells (HSCs) and overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRPa, leads to the inhibition of macrophage activation and protects cancer cells from phagocytosis, thereby allowing cancer cells to proliferate.
lilotomab: A murine immunoglobulin G1 (IgG1) monoclonal antibody directed against the CD37 antigen with potential antineoplastic activity. Upon administration, lilotomab both activates the immune system to induce an antibody-dependent cell-mediated cytotoxicity (ADCC) against CD37-overexpressing tumor cells and induces apoptosis in these tumor cells. CD37 is a transmembrane glycoprotein expressed at high-levels on B-cells and to a lesser extent on T cells and myeloid cells, and is frequently overexpressed in certain B-cell malignancies.
limonene, (+)-: An oral dietary supplement containing a natural cyclic monoterpene, and a major component of the oil extracted from citrus peels, with potential chemopreventive and antineoplastic activities. Upon oral administration, D-limonene activates aldehyde dehydrogenase 3A1 (ALDH3A1), thereby decreasing aldehyde level. This may protect salivary stem/progenitor cells (SSPCs) from toxic aldehydes and prevent or improve radiation-induced xerostomia. Limonene and its metabolites perillic acid, dihydroperillic acid, uroterpenol and limonene 1,2-diol may also inhibit tumor growth through inhibition of p21-dependent signaling and may induce apoptosis via the induction of the transforming growth factor beta-signaling pathway. In addition, they inhibit post-translational modification of signal transduction proteins, resulting in G1 cell cycle arrest as well as differential expression of cell cycle- and apoptosis-related genes.
linaclotide acetate: The acetate salt form of linaclotide, a synthetic, fourteen amino acid peptide and agonist of intestinal guanylate cyclase type C (GC-C), which is structurally related to the guanylin peptide family, with secretagogue, analgesic and laxative activities. Upon oral administration, linaclotide binds to and activates GC-C receptors located on the luminal surface of the intestinal epithelium. This increases the concentration of intracellular cyclic guanosine monophosphate (cGMP), which is derived from guanosine triphosphate (GTP). cGMP activates the cystic fibrosis transmembrane conductance regulator (CFTR) and stimulates the secretion of chloride and bicarbonate into the intestinal lumen. This promotes sodium excretion into the lumen and results in increased intestinal fluid secretion. This ultimately accelerates GI transit of intestinal contents, improves bowel movement and relieves constipation. Increased extracellular cGMP levels may also exert an antinociceptive effect, through an as of yet not fully elucidated mechanism, that may involve modulation of nociceptors found on colonic afferent pain fibers. Linaclotide is minimally absorbed from the GI tract.
linagliptin: A potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. The inhibition of DPP-4 by linagliptin appears to be longer lasting than that by some other DPP-4 inhibitors tested.
Lindera obtusiloba extract: A dietary supplement composed of an ethanol extracted powder of Lindera obtusiloba, with potential antioxidant and anti-inflammatory activities. Upon administration, Lindera obtusiloba extract (LOE) may promote anti-oxidant activities through the activation of nuclear factor erythroid 2-related factor 2 (Nrf-2)/heme oxygenase 1 (HO-1)/ NAD(P)H dehydrogenase [quinone] 1 (NQO1), which reduces the production of reactive oxygen species (ROS) and lowers ROS-mediated oxidative stress. In addition, LOE may exert anti-inflammatory effects through the inhibition of the phosphorylation and activation of mitogen-activated protein kinases (MAPKs) and nuclear factor-kappa B (NF-kB).
linezolid: A synthetic oxazolidinone derivative, linezolid selectively inhibits an early step in bacterial protein synthesis and affects blood pressure through monoamine oxidase inhibition. It is effective against Gram-positive organisms, including methicillin-resistant Staphylococcus aureus strains, coagulase-negative Staphylococci, vancomycin-resistant Enterococci, and penicillin-resistant Streptococcus pneumoniae strains.
linifanib: An orally bioavailable, small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Linifanib inhibits members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families; it exhibits much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. This agent does not have a general antiproliferative effect due to its high dose requirement. However, linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as fms-related tyrosine kinase receptor-3 (FLT3).
linoleyl carbonate-paclitaxel: A formulation of the 6-omega fatty acid derivative 2’-linoleyl carbonate (LOC) conjugated to paclitaxel, a taxane compound extracted from the Pacific yew tree Taxus brevifolia, with potential antineoplastic activity. Paclitaxel binds to and stabilizes tubulin, thereby interfering with the dynamics of microtubule assembly/disassembly and resulting in the inhibition of cell division. LOC enhances the uptake of paclitaxel by tumor cells, thereby concentrating this agent in tumor cells compared to normal cells, and may decrease its toxicity profile; fatty acids serve as energy sources and biochemical precursors for the fast growing tumor cells.
Linomide: (Other name for: roquinimex)
linperlisib: An orally available selective inhibitor of the delta form of phosphatidylinositol 3-kinase (PI3-kinase subunit delta; PI3K-delta; PI3Kdelta), with potential antineoplastic activity. Upon oral administration linperlisib selectively binds to and inhibits PI3K-delta and prevents the activation of the PI3K/AKT signaling pathway. This decreases proliferation of and induces cell death in PI3K-delta over-expressing tumor cells. PI3K-delta also plays a key role in the B-cell receptor (BCR) signaling pathway and the proliferation of certain hematologic cancer cells. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells, thereby minimizing serious side effects.
linrodostat: An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, linrodostat specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, BMS-986205 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells, thereby inhibiting the growth of IDO1-expressing tumor cells. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
linsitinib: An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGFR-1 stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.
lintuzumab: A humanized recombinant monoclonal antibody directed against CD33, a cell surface antigen found on myeloid leukemia blasts and early hematopoietic progenitor cells. Lintuzumab stimulates antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing CD33, resulting in a decrease in tumor burden. The humanized version of this monoclonal antibody exhibits less immunogenicity and improved binding affinity compared to its murine counterpart.
linvoseltamab: A human, immunoglobulin G4 (IgG4) bispecific antibody directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17) and the T-cell surface antigen CD3, with potential immunostimulating and antineoplastic activities. Upon administration, linvoseltamab targets and binds to both CD3 on cytotoxic T lymphocytes (CTLs) and BCMA on BCMA-expressing tumor cells. This activates and redirects CTLs to BCMA-expressing tumor cells, leading to CTL-mediated killing of BCMA-expressing tumor cells. BCMA, a member of the tumor necrosis factor receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.
linzagolix: An orally bioavailable gonadotropin-releasing hormone (GnRH or LHRH) receptor antagonist, with potential hormone production inhibitory activity. Upon oral administration of linzagolix, this agent competes with GnRH for receptor binding and inhibits GnRH receptor signaling in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with hormonally dependent disease states such as hormone-dependent prostate cancer. In women, this prevents the production of estrogen by the ovaries and may relieve symptoms from sex-hormone dependent diseases, such as pain associated with endometriosis, heavy menstrual bleeding or uterine fibroids.
Linzess: (Other name for: linaclotide acetate)
Lioresal: (Other name for: baclofen)
liothyronine sodium: The sodium salt form of liothyronine, a synthetic form of the levorotatory isomer of the naturally occurring thyroid hormone triiodothyronine (T3). Liothyronine sodium binds to nuclear thyroid receptors which then bind to thyroid hormone response elements of target genes. As a result, liothyronine sodium induces gene expression that is required for normal growth and development. Liothyronine sodium is more potent and has a more rapid action than thyroxine (T4).
lipegfilgrastim: A long acting glyco-pegylated recombinant form of human granulocyte colony-stimulating factor (G-CSF), with hematopoietic activity. Similar to G-CSF, lipegfilgrastim binds to and activates specific cell surface receptors, and stimulates neutrophil progenitor proliferation and differentiation. Therefore, this agent may prevent the duration and incidence of chemotherapy-induced neutropenia. Compared to filgrastim, lipegfilgrastim has a prolonged plasma half-life.
Lipid Nanoparticle Encapsulated mRNA Encoding Human Single-chain IL-12 ABO2011: A formulation consisting of lipid nanoparticle (LNP)-encapsulated messenger RNA (mRNA) encoding human single-chain interleukin-12 (scIL-12), with potential immunomodulatory and antineoplastic activities. Upon intratumoral injection, the LNP moiety binds to the plasma membrane of nearby cells and releases the scIL-12 mRNA into the cells. The mRNA is then translated by the cellular protein translation machinery to produce scIL-12, which is secreted into the local tumor microenvironment (TME). IL-12 activates the immune system by promoting the secretion of interferon-gamma (IFN-g), activating natural killer cells (NKs), and inducing cytotoxic T-lymphocyte (CTL) responses, which may result in both decreased tumor cell proliferation and enhanced immune-mediated destruction of tumor cells.
lipid nanoparticle encapsulated mRNAs encoding human IL-12A/IL-12B MEDI-1191: A formulation consisting of lipid nanoparticle encapsulated messenger RNA (mRNA) encoding human interleukin-12 subunit beta (IL-12B; IL-12 subunit p40) and interleukin-12 subunit alpha (IL-12A; IL-12 subunit p35) with potential immunomodulatory and antineoplastic activities. Although the exact mechanism of action has not been completely characterized, upon intratumoral injection, the lipid nanoparticle moiety presumably binds to the plasma membrane of nearby cells and releases the IL-12A and IL-12B mRNA into the cell. The mRNA is then translated by the cellular protein translation machinery to produce a single-chain fusion protein of IL-12B and IL-12A subunits, which is secreted into the local tumor microenvironment (TME). Secretion of IL-12 activates the immune system by promoting the secretion of interferon-gamma, activating natural killer cells (NKs), and inducing cytotoxic T-cell responses, which may result in both decreased tumor cell proliferation and enhanced immune-mediated destruction of tumor cells.
lipid nanoparticle encapsulated MYC-targeting mRNA-based agent OTX-2002: A lipid nanoparticle (LNP)-based formulation consisting of a biscistronic mRNA that encodes two independent epigenomic controllers targeting the proto-oncogene MYC (c-Myc), with potential antineoplastic activity. Upon administration of LNP encapsulated MYC-targeting mRNA-based agent OTX-2002, the lipid formulation promotes the uptake by tumor cells. The biscistronic mRNA is then translated by the cellular protein translation machinery to produce two independent epigenomic controllers consisting of a DNA binding domain and an epigenetic effector protein. The two epigenomic controllers bind to regulatory regions on the MYC insulated genomic domain (IGD), a DNA loop bound by CTCF (CCCTC-binding factor). This downregulates MYC expression pre-transcriptionally, which may inhibit proliferation in susceptible tumor cells. MYC, a proto-oncogene overexpressed in a variety of cancers, plays a role in the regulation of transcription and cell proliferation.
lipid nanoparticle encapsulated self-replicating RNA encoding human IL-12 JCXH-211: A formulation consisting of lipid nanoparticle (LNP) encapsulating self-replicating RNA (srRNA) encoding human interleukin-12 (IL-12), with potential immunomodulatory and antineoplastic activities. Upon intratumoral injection of LNP encapsulated srRNA encoding human IL-12 JCXH-211, the LNPs bind to the plasma membrane of nearby tumor cells and release srRNA encoding IL-12 into the tumor cells. The srRNA amplifies within the tumor cells, and is translated by the cellular protein translation machinery to produce IL-12, which is secreted into the local tumor microenvironment (TME). The secretion of IL-12 activates the immune system by promoting the secretion of interferon-gamma (IFN-g), activating natural killer cells (NKs), and inducing cytotoxic T-lymphocyte (CTL) responses, which may enhance immune-mediated destruction of tumor cells and decrease tumor cell proliferation. In addition, the virus-based RNA replicon may trigger anti-viral innate immune responses, further killing tumor cells.
lipid nanoparticle encapsulated self-replicating RNA encoding human IL-12 STX-001: A formulation consisting of lipid nanoparticle (LNP) encapsulating self-replicating RNA (srRNA) encoding human interleukin-12 (IL-12), with potential immunomodulatory and antineoplastic activities. Upon intratumoral injection of LNP encapsulated srRNA encoding human IL-12 STX-001, the LNPs bind to the plasma membrane of nearby tumor cells and release srRNA encoding IL-12 into the tumor cells. The srRNA amplifies within the tumor cells, and is translated by the cellular protein translation machinery to produce IL-12, which is secreted into the local tumor microenvironment (TME). The secretion of IL-12 activates the immune system by promoting the secretion of interferon-gamma (IFN-g), activating natural killer cells (NKs), and inducing cytotoxic T-lymphocyte (CTL) responses, which may enhance immune-mediated destruction of tumor cells and decrease tumor cell proliferation.
lipid nanoparticle encapsulating glutathione S-transferase P siRNA NBF-006: A biodegradable, lyophilized lipid nanoparticle (LNP) encapsulating small interfering ribonucleic acid (siRNA) directed against glutathione S-transferase P (GSTP), with potential antineoplastic activity. Upon administration of LNP encapsulating GSTP siRNA NBF-006, the LNP formulation delivers the siRNA particles to the tumor cells where the GSTP siRNA targets and binds to GSTP mRNA. This results in the inhibition of the translation and expression of GSTP and may inhibit proliferation of KRAS-overexpressing tumor cells. GSTP, an enzyme overexpressed in many tumor cell types, is involved in modulating MAP kinase-related cell-signaling pathways.
lipid nanoparticle encapsulating hAQP1 circular RNA RXRG001: A formulation consisting of lipid nanoparticles (LNPs) encapsulating circular RNA (circRNA) encoding human aquaporin-1 (hAQP1), with potential saliva enhancing activity. Upon intraductal administration of LNP encapsulating hAQP1 circRNA RXRG001 to parotid gland(s), the LNP binds to the plasma membrane and releases the circRNA into the cell. The circRNA is then translated to produce hAQP1, which restores water permeability of the cell and increases saliva production. This may alleviate dry mouth symptoms. hAQP1, a water channel protein, is one of several highly conserved water channel proteins that mediates water permeability in cells of water-transporting tissues.
lipid nanoparticle encapsulating mRNA encoding Cas9 protein and TTR-targeting single guide RNA NTLA-2001: A lipid nanoparticle (LNP) formulation encapsulating messenger RNA (mRNA) encoding the clustered regularly interspaced short palindromic repeat (CRISPR)-associated protein 9 (Cas9) protein and a single guide RNA targeting transthyretin (TTR), that may decrease serum TTR concentration. Upon administration of LNP encapsulating mRNA encoding Cas9 protein and TTR-targeting single guide RNA NTLA-2001, the LNP moiety binds to the plasma membrane of nearby cells and releases the Cas9 mRNA and the TTR-targeting single guide RNA into the cells. The mRNA is then translated by the cellular protein translation machinery to produce Cas9, which gene-edits the TTR gene in vivo, thereby lowering the levels of misfolded TTR in the blood. This may reduce the accumulation of misfolded TTR protein in the tissues.
lipid nanoparticle encapsulating mRNAs encoding human OX40L/IL-23/IL-36gamma mRNA-2752: A lipid nanoparticle encapsulating mRNAs encoding for the human co-stimulatory protein tumor necrosis factor ligand superfamily member 4 (TNFSF4; OX40 Ligand; OX40L), the pro-inflammatory cytokines interleukin-23 (IL-23) and interleukin-36gamma (IL-36gamma), with potential immunomodulatory and anti-tumor activities. Upon intratumoral (IT) injection of the lipid nanoparticle encapsulated mRNAs encoding human OX40L/IL-23/IL-36gamma mRNA-2752, the lipid nanoparticle binds to the plasma membrane of cells and releases the mRNAs into the cell. The OX40L mRNA is then translated by the cellular protein translation machinery to produce OX40L protein, which is then expressed on the plasma membrane of the cells that internalized the OX40L mRNA. OX40L binds to and activates signaling pathways downstream of its cognate receptor tumor necrosis factor receptor superfamily member 4 (TNFRSF4; OX40), which is expressed on activated T-cells. OX40L/OX40 binding promotes increased cytokine production, which can induce proliferation of memory and effector T lymphocytes against the nearby tumor cells. The co-administration of IL-23 and IL-36gamma further stimulates anti-tumor immune responses. Altogether, this may enhance T cell mediated anti-tumor immune responses thereby killing of the tumor cells. OX40L, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) ligand superfamily, provides a co-stimulatory signal for the proliferation and survival of activated T-cells. IL-36gamma activates innate immune cells and promotes T-helper 1 (Th1) responses, whereas IL-23 has been implicated in Th1/Th17 immunity as well as in the modulation of antigen-presenting cells (APCs).
lipid nanoparticle-encapsulated EBV mRNA vaccine mRNA-1189: A vaccine consisting of a lipid nanoparticle (LNP) encapsulating four messenger RNAs (mRNAs) encoding the Epstein-Barr Virus (EBV) envelope glycoproteins gp42, gp220, gH and gL, with potential immunizing activity against EBV. Upon intramuscular administration of LNP-encapsulated EBV mRNA vaccine mRNA-1189, the LNP binds to the plasma membrane of cells and releases the mRNAs into the cells. The mRNAs are then translated by ribosomes to produce the EBV envelope glycoproteins. This may activate both humoral and cellular immune responses which may result in protection against EBV infection. EBV, a ubiquitous human herpes virus, is associated with infectious mononucleosis and various malignancies, including nasopharyngeal carcinoma, Hodgkin disease, non-Hodgkin lymphoma, and other lymphomas.
lipid nanoparticle-encapsulated OX40L mRNA-2416: A proprietary formulation consisting of a lipid nanoparticle encapsulating a synthetic messenger RNA (mRNA) encoding the human co-stimulatory protein tumor necrosis factor ligand superfamily member 4 (TNFSF4; OX40 Ligand; OX40L), with potential immunomodulatory and antitumor activities. Although the mechanism of action has not been completely characterized, following intratumoral injection of lipid nanoparticle encapsulated OX40L mRNA-2416, the lipid nanoparticle moiety presumably binds to the plasma membrane of nearby cells and releases the OX40L mRNA into the cell. The OX40L mRNA is then translated by the cellular protein translation machinery to produce OX40L protein, which is then expressed on the plasma membrane of the cells that internalized the OX40L mRNA. OX40L binds to and activates signaling pathways downstream of its cognate receptor tumor necrosis factor receptor superfamily member 4 (TNFRSF4; OX40), which is expressed on activated T cells. OX40L/OX40 binding promotes increased cytokine production, which can induce proliferation of memory and effector T lymphocytes. Altogether, this may enhance an immune response that promotes the killing of nearby tumor cells. OX40L, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) ligand family, provides a co-stimulatory signal for the proliferation and survival of activated T cells.
lipid-encapsulated anti-PLK1 siRNA TKM-PLK1: Short interfering RNAs (siRNAs) directed against polo-like kinase 1 (PLK1, STPK13), with potential antineoplastic activity. Upon administration of lipid-encapsulated anti-PLK1 siRNA TKM-PLK1, siRNA binds to PLK1 mRNA, which results in the inhibition of both the translation and expression of the PLK1 protein. Blockage of PLK1 expression prevents proper tumor cell mitosis, causes cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of PLK1-overexpressing tumor cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine kinase crucial in the regulation of mitosis; its expression is upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation. The pegylated lipid bilayer of SNALP provides stability and protects siRNA degradation; it facilitates uptake into the cell and release from endosomes.
Lipiodol: (Other name for: ethiodized oil)
Lipitor: (Other name for: atorvastatin calcium)
Lipo-Hepin: (Other name for: heparin sodium)
Lipo-Lutin: (Other name for: therapeutic progesterone)
Lipodox 50: (Other name for: pegylated liposomal doxorubicin hydrochloride)
lipopolysaccharide: An endotoxin and biologically active component of the Gram-negative bacterial cell wall that is a Toll-like receptor 4 (TLR4) agonist with potential immunostimulatory activity. Upon internalization, lipopolysaccharide (LPS) activates TLR4 which in turn activates the NFkappaB pathway, in addition to mitogen-activated protein kinases signaling pathways. This leads to the release of proinflammatory cytokines and stimulates an innate immune response against vaccine antigens.
liposomal alpha galactosylceramide: A liposomal formulation of alpha galactosylceramide, a synthetic glycolipid isolated from the Okinawan marine sponge (Agelas mauritianus) with potential immunosuppressing activity. Upon administration, alpha galactosylceramide serves as a ligand for CD1d which is expressed on various antigen-presenting cells (APCs) including dendritic cells (DCs), macrophages, and B-cells. This induces the activation of the immunoregulatory invariant natural killer T cells (iNKTs), which induces the expansion of tolerogenic regulatory DCs and, in turn, regulatory T cells (Tregs). Tregs may specifically suppress T-cell responses against host alloantigens, thereby reducing graft rejection while maintaining normal immune cell function. CD1d is a non-polymorphic, major histocompatibility complex (MHC) class I-like antigen-presenting molecule with an antigen-binding groove adapted for the presentation of lipid antigens.
liposomal amphotericin B: A liposome-encapsulated formulation of the polyene antifungal antibiotic amphotericin B produced by the bacterium Streptomyces nodosus with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, and alters cell membrane integrity, resulting in leakage of intracellular components and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells. Compared to amphotericin B alone, liposomal delivery of amphotericin B allows for a greater drug concentration in target tissues while decreasing systemic side effects.
liposomal Bcl-2 antisense oligonucleotide BP1002: A liposomal-based nanoparticle composed of an uncharged P-ethoxy antisense oligodeoxynucleotide (ODN) targeting Bcl-2 mRNA and incorporated in liposomes, with potential antineoplastic activity. Upon administration of liposomal Bcl-2 antisense oligonucleotide BP1002, this agent targets and hybridizes with Bcl-2 mRNA and inhibits the expression of Bcl-2 protein. This may induce tumor cell apoptosis of Bcl2-overexpressing tumor cells and may decrease tumor cell proliferation. Bcl2, a protein involved in regulating programmed cell death, is overexpressed in a wide variety of tumors. It promotes cellular survival and inhibits apoptosis.
liposomal belotecan: A sterically stabilized, pegylated liposomal formulation containing CKD602, a semi-synthetic analogue of campthotecin with potential antitumor activity. CKD602 inhibits the action of topoisomerase I, an enzyme that produces reversible single-strand breaks in DNA during DNA replication. CDK602 stabilizes the topoisomerase I and DNA complex, resulting in the inhibition of religation of DNA breaks, inhibition of DNA replication, and apoptotic cell death. The polyethylene glycol coating of liposomal belotecan allows for greater plasma circulation time, thus enhancing the concentration of CKD602 at the tumor site. Encapsulation of CKD602 preserves the active lactone form, resulting in an increased cytotoxic effect of CKD602.
liposomal c-raf antisense oligonucleotide: The liposomal formulation of a c-raf-1 antisense oligonucleotide, with potential antineoplastic activity. Liposomal c-raf antisense oligonucleotide targets the translation initiation site of human c-raf-1 mRNA, thereby blocking the expression and production of Raf-1 protein and thus inhibits tumor cell growth and development. Raf-1 plays a key role in the RAF/MEK/ERK signaling pathway, which regulates mammalian cell proliferation and growth. The liposomal formulation increases the solubility of the c-raf antisense oligonucleotide, thus improving its pharmacodynamic profile.
liposomal Chk1 inhibitor SMP-3124 SMP-3124LP: A liposomal formulation containing an inhibitor of checkpoint kinase 1 (chk1), with potential antineoplastic and chemosensitization activities. Upon administration of liposomal chk1 inhibitor SMP-3124 SMP-3124LP, SMP-3124 selectively targets and binds to chk1, thereby preventing activity of chk1 and abrogating the repair of damaged DNA. This may lead to an accumulation of damaged DNA, inhibition of cell cycle arrest, and induction of apoptosis. Chk1, an ATP-dependent serine/threonine kinase, is activated by DNA damage response and mediates cell cycle checkpoint control. It is essential for DNA repair and plays a key role in resistance to chemotherapeutic agents.
liposomal CMTR2 inhibitor AT-1965: A liposomal formulation containing an inhibitor of cap-specific mRNA (nucleoside-2-O-)-methyltransferase 2 (cap-methytransferase 2; CMTR2; MTR2; FTSJD1), with potential immunomodulating and antineoplastic activities. Upon administration, liposomal CMTR2 inhibitor AT1965 targets, binds to, and inhibits the activity of CMTR2. This causes the innate immune sensors to recognize the mRNA as non-self and results in an anti-viral immune response leading to the activation of B cells and resulting in a B-cell-mediated immune response against tumor cells. This induces tumor cell apoptosis and decreases tumor growth. CMTR2, a key protein in marking newly-synthesized RNA as self, plays a key role in tumor host immunity evasion. Increased expression of CMTR2 correlates with poor prognosis. It is overexpressed in a variety of tumor cells.
liposomal curcumin: A liposomal formulation containing curcumin, a poorly water-soluble polylphenol pigment isolated from the plant Curcuma longa, with potential antineoplastic, chemopreventive, antioxidant, anti-angiogenic and anti-inflammatory activities. Upon intravenous administration of liposomal curcumin, this agent blocks the formation of reactive-oxygen species, neutralizes free radicals, and exhibits anti-inflammatory properties as a result of inhibition of cyclooxygenases (COX) and other enzymes involved in inflammation. In addition, curcumin disrupts various cell signal transduction pathways involved in carcinogenesis, inhibits the activity of nuclear factor-kappa B (NF-kB), SRC, and annexin A2 (ANXA2), and reduces the expression of both matrix metalloproteinase-9 (MMP-9) and vascular endothelial growth factor receptor 2 (VEGFR2). This prevents and/or inhibits tumor cell formation and proliferation. Liposome encapsulation of curcumin improves its efficacy, when compared to the administration of unencapsulated curcumin.
liposomal daunorubicin citrate: A liposome-encapsulated form of the citrate salt of the anthracycline antineoplastic antibiotic daunorubicin. Daunorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Liposomal delivery of doxorubicin citrate improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects.
liposomal docetaxel: A formulation of the poorly soluble, semi-synthetic, second-generation taxane docetaxel encapsulated within liposomes, with antineoplastic activity. Upon intravenous administration, docetaxel binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell-cycle arrest at the G2/M phase and cell death. This liposomal formulation solubilizes docetaxel without the use of toxic solvents such as Tween 80, permitting the administration of larger doses of docetaxel while avoiding solvent-associated toxicity, including hypersensitivity reactions. In addition, liposomal delivery of docetaxel improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects while lowering the toxicity profile.
liposomal eribulin mesylate: A liposome-encapsulated formulation of the mesylate salt form of eribulin, a synthetic, macrocyclic ketone analogue of halichondrin B, a substance derived from the marine sponge genus Halichondria, with potential antineoplastic activity. Eribulin binds to the vinca domain of tubulin and inhibits both the polymerization of tubulin and the assembly of microtubules. This results in the inhibition of mitotic spindle assembly, the induction of cell cycle arrest at G2/M phase, as well as tumor cell apoptosis. Compared to the administration of eribulin alone, liposomal delivery of eribulin allows for a longer half-life, which allows increased drug concentration in target tissues while decreasing systemic toxicity.
liposomal HPV-16 E6/E7 multipeptide vaccine PDS0101: A liposomal nanoparticle-based therapeutic vaccine composed of the cationic lipid R-DOTAP (R-enantiomer of 1,2-dioleoyl-3-trimethylammonium-propane chloride) encapsulating six human papillomavirus 16 (HPV-16) E6 and E7 peptides, with potential immunostimulating activity. Upon subcutaneous administration of the liposomal HPV-16 E6 and E7 multipeptide vaccine, the nanoparticles are taken up by antigen presenting cells (APCs), specifically dendritic cells (DCs), which may stimulate the immune system to induce a cytotoxic T-lymphocyte response (CTL) against HPV-16 E6 and E7-expressing tumor cells. HPV-16 E6 and E7 are oncoproteins that play a key role in the tumorigenesis of a variety of cancers.
liposomal interleukin-2: A formulation in which liposomes are loaded with the cytokine interleukin-2 (IL-2). By activating cytotoxic T lymphocytes, such as lymphokine-activated killer cells, and increasing levels of the cytotoxic cytokines interferon-gamma (IFN-gamma) and transforming growth factor-beta (TGF-beta), IL-2 may exhibit antitumoral activity. Liposomal formulations of IL-2 may promote entry of the cytokine into target tumor cells and may be used as an immunoadjuvant in cancer vaccine therapy.
liposomal lurtotecan: A liposome-encapsulated formulation of lurtotecan with antineoplastic activity. Lurtotecan, a semisynthetic analogue of camptothecin, selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex during S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks. This ultimately results in an inhibition of DNA replication, inducing double-stranded DNA breakages, obstruction of RNA and protein synthesis and triggering apoptosis. Furthermore, this agent also stimulates degradation of topoisomerase I, likely mediated through ubiquitin-proteasomal pathway. Liposomal delivery of lurtotecan improves its penetration and delivery into tumors while lowering systemic side effects.
liposomal mitoxantrone hydrochloride: A formulation composed of the hydrochloride salt form of the anthracenedione antibiotic mitoxantrone encapsulated within liposomes, with potential antineoplastic activity. Upon intravenous administration, mitoxantrone intercalates into and forms crosslinks with DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, which both results in DNA strand breaks and prevents DNA synthesis. This leads to the induction of apoptosis in the rapidly dividing cancer cells. The liposomal delivery of mitoxantrone improves drug penetration into tumors and decreases drug clearance, thereby increasing drug circulation and therapeutic efficacy while lowering the toxic effects.
liposomal MUC1/PET-lipid A vaccine: A cancer vaccine comprised of a 43 amino acid epitope from glycoprotein MUC1 (mucin 1) and the synthetic Toll-like receptor 4 (TLR-4) agonist PET lipid A encapsulated in cholesterol/dipalmitoylphosphatidylcholine (DPPC)/dimyristoylphosphatidylglycerol (DMPG) liposomes, with potential immunostimulatory and antineoplastic activities. The MUC1 epitope is composed of two 20 amino glycosylated VNTR (various number tandem repeats) from human MUC1A and including 6 glycosylated sites modified by Tn (alfa-N-acetyl-D-galactosamine). Immunization of liposomal MUC1/PET-lipid A vaccine results in an antibody as well as a cytotoxic T-lymphocyte (CTL) response against hypoglycosylated MUC1 expressing tumor cells. The tumor associated antigen MUC1, a type І transmembrane protein, is overexpressed and aberrantly glycosylated in a variety of tumor cells. As a vaccine adjuvant, PET lipid A, also known as penta erythritol lipid A, stimulates both cellular and humoral responses to the vaccine antigen.
liposomal NDDP: A synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotoxicity. Because DNA mismatch-repair (MMR) complexes do not recognize DACH–platinum adducts, DNA repair mechanisms are inhibited, overcoming limitations observed with other platinum-based agents. In addition, the liposomal encapsulation improves the bioavailability of NDDP and reduces its toxicity profile.
liposomal oxaliplatin: A liposomal formulation of the prodrug oxaliplatin, an organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a 'leaving group', with antineoplastic activity. After displacement of the labile oxalate ligand leaving group, the active oxaliplatin derivatives monoaquo and diaquo DACH platinum alkylate macromolecules, and form both inter- and intra-strand platinum-DNA crosslinks; inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity ensue. The DACH side chain appears to inhibit alkylating-agent resistance. A leaving group is an atom or a group of atoms that is displaced as a stable species taking with it its bonding electrons.
liposomal rhenium Re 186: A therapeutic preparation consisting of the beta-emitting radioisotope rhenium Re 186 encapsulated in a nanoliposome, with potential antineoplastic activity. Upon intratumoral infusion of liposomal rhenium Re 186, the radioisotope releases radiation, which directly kills the tumor cells. The nanoliposomes facilitate the retention of the radioisotope by the tumor cells and localize the radiocytotoxicity to the tumor while sparing surrounding normal, healthy cells. Re-186 has a short half-life and a short path length, which contributes further to limiting the radiotoxicity to the tumor cells.
liposomal SN-38: The liposomal formulation of SN-38 (7-ethyl-10-hydroxy-camptothecin), a biologically active metabolite of the prodrug irinotecan, with potential antineoplastic activity. SN-38 binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication, and apoptosis. SN-38 has been reported to exhibit up to 1,000-fold more cytotoxic activity against various cancer cells in vitro than irinotecan. The liposomal formulation of SN-38 increases the solubility of SN-38, which is a relatively insoluble compound, and improves the pharmacodynamic profile as compared to SN-38 alone.
liposomal T4N5 lotion: A topical lotion that contains the enzyme T4-bacteriophage endonuclease V encapsulated within liposomes. With topical liposomal delivery, the DNA repair enzyme T4-bacteriophage endonuclease V is transported into skin cells, where the enzyme enters cell nuclei and binds to and incises pyrimidine dimers, thereby catalyzing the first reaction step of the cellular excision repair pathway for removing DNA replication-inhibiting pyrimidine dimers produced within duplex DNA through exposure to ultraviolet (UV) irradiation. In vitro and in vivo studies indicate that T4N5 liposomes increases repair of DNA damage caused by UV irradiation.
liposomal topotecan FF-10850: A liposome encapsulated formulation of the semisynthetic camptothecin analogue topotecan with potential antineoplastic activity. Upon administration, liposomal topotecan FF-10850 preferentially releases topotecan, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminate, into the tumor environment. Topotecan inhibits topoisomerase I activity by stabilizing the topoisomerase I-DNA covalent complexes during S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. The novel liposome used in this agent prolongs its serum half-life while promoting efficient drug delivery into the cytosol from the endosome compartment of the tumor cell, which may minimize the adverse effect of bone marrow suppression.
liposomal topotecan hydrochloride: The hydrochloride salt of a semisynthetic derivative of camptothecin mixed with sphingomyelin/cholesterol and sonicated to form small unilamellar vesicles containing topotecan, with potential antineoplastic activity. Liposomal opotecan hydrochloride mediates efficient drug delivery of topotecan into the cytosol from the endosome compartment. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery.
liposomal tretinoin: An intravenous formulation of tretinoin (vitamin A acid or all-trans retinoic acid) encased in liposomes. Tretinoin is a naturally occurring retinoic acid agent that binds to and activates retinoic acid receptors (RAR), effecting changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of carcinogenesis. This agent also inhibits telomerase, leading to telomere shortening and eventual apoptosis of certain tumor cell types. Liposome encapsulation extends the half-life of intravenously administered tretinoin.
liposomal vinorelbine: A formulation of the semisynthetic vinca alkaloid, vinorelbine, encapsulated within liposomes, with antineoplastic activity. Vinorelbine binds to tubulin and prevents formation of the mitotic spindle, resulting in cell cycle arrest in metaphase. Like other vinca alkaloids, vinorelbine may also interfere with the metabolism of nucleic acids, lipids, amino acids, cAMP, and glutathione, as well as other biological processes including calmodulin-dependent Ca2+-transport, ATPase activity, or cellular respiration. Liposomal delivery of vinorelbine improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile.
liposomal vinorelbine tartrate: A formulation of the tartrate salt form of vinorelbine, a semisynthetic vinca alkaloid, encapsulated within liposomes, with potential antineoplastic activity. Upon intravenous administration, vinorelbine binds to tubulin within tumor cells and prevents the formation of the mitotic spindle, resulting in cell cycle arrest, induction of apoptosis and an inhibition of tumor cell growth. Compared to the administration of vinorelbine alone, the liposomal formulation improves drug penetration into tumors and decreases drug clearance, thereby increasing vinorelbine's efficacy while lowering the toxicity profile.
liposome-encapsulated daunorubicin-cytarabine: A liposomal formulation containing a fixed combination of the antineoplastic agents cytarabine and daunorubicin in a 5:1 molar ratio. Liposome-encapsulated daunorubicin-cytarabine has been designed to provide optimal delivery of a specific ratio of cytarabine to daunorubicin, one that has been shown to be synergistic in vitro. The antimetabolite cytarabine competes with cytidine for incorporation into DNA, inhibiting DNA synthesis. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Daunorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in the cytotoxic lipid peroxidation of cell membrane lipids.
liposome-encapsulated doxorubicin citrate: A formulation of the citrate salt of the antineoplastic anthracycline antibiotic doxorubicin, encapsulated within liposomes, with antitumor activity. Doxorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and RNA synthesis. This agent also interacts with cell membrane lipids causing lipid peroxidation. Liposomal delivery of doxorubicin improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects while lowering the toxicity profile.
liposome-encapsulated miR-34 mimic MRX34: A liposomal formulation containing a nucleotide that mimics the human tumor suppressor microRNA (miRNA) miR-34, with potential antineoplastic activity. Upon administration, liposome-encapsulated MRX34 mimics miR-34 by inhibiting the expression of a variety of oncogenes including MYC, MET, BCL2, and beta-catenin. This induces cell cycle arrest, senescence and apoptosis in susceptible tumor cells. miR-34 is downregulated in most solid and hematologic malignancies and regulates the expression of a variety of genes. This miRNA plays an important role in the inhibition of cancer cell stemness, metastasis and cancer cell survival.
liposome-encapsulated RB94 plasmid DNA gene therapy agent SGT-94: A systemic gene therapy anti-cancer agent composed of cationic liposomes, which encapsulates plasmid DNA encoding for the tumor suppressor gene RB94 and is complexed with anti-transferrin receptor single chain antibody fragment (TfRscFv), with potential antineoplastic activity. Upon systemic administration of liposome-encapsulated RB94 plasmid DNA gene therapy agent SGT-94, the TfRscFv portion of this agent selectively targets the tumor cells expressing transferrin receptors. TfRscFv binding to the transferrin receptor allows receptor-mediated endocytosis and transfection, followed by the expression of RB94 gene. This induces tumor cell apoptosis through an as-of-yet unknown pathway. RB94 is a modified, N-terminal truncated form of the full-length protein retinoblastoma gene RB110, and exerts enhanced antitumor activity. The transferrin receptor (TfR) functions in cellular iron uptake through its interaction with transferrin, and is overexpressed in a variety of tumor types.
liposome-encapsulated recombinant human Cu/Zn superoxide-dismutase: A topical hydrophilic gel containing a recombinant form of the human Cu/Zn superoxide dismutase (SOD1), a cytoplasmic antioxidant enzyme, encapsulated in liposomes with potential anti-inflammatory and adjuvant activities. Upon application of liposome-encapsulated recombinant human Cu/Zn SOD as a thin film on the irradiated area, the recombinant SOD1 is released and scavenges free oxygen radicals, thereby protecting cells from oxidative stress. This may prevent radiation-induced dermatitis as well as other types of skin reactions.
liposome-encapsulated TAAs mRNA vaccine W_ova1: A vaccine consisting of messenger RNA (mRNA) encoding three tumor-associated antigens (TAAs) specific for ovarian cancer that are encapsulated in liposomes, with potential immunomodulating and antineoplastic activities. Upon administration of the liposome-encapsulated TAAs mRNA vaccine W_ova1, the liposomes bind to the plasma membrane of cells and release the mRNA into the cells. The mRNA is then translated by ribosomes to produce the TAAs. The TAAs are presented to the immune system which may activate both humoral and cellular immune responses against the ovarian cancer cells expressing these TAAs.
liposome-incorporated Grb2 antisense oligodeoxynucleotide: A liposomal formulation containing the antisense oligodeoxynucleotide (ODN) growth factor receptor-bound protein 2 (Grb2), with potential antineoplastic activity. Upon administration, liposome-incorporated Grb2 antisense oligodeoxynucleotide binds directly to and blocks Grb2 mRNA, thereby preventing Grb2 protein synthesis, leading to inhibition of cell proliferation of cancer cells overexpressing Grb2. Grb2, an adaptor protein involved in growth signaling pathways, is upregulated in certain tumor cells.
Lipotecan: (Other name for: camptothecin analogue TLC388)
Liquamar: (Other name for: phenprocoumon)
liraglutide: A long-acting, fatty acylated glucagon-like peptide-1 (GLP-1) analog administered subcutaneously, with antihyperglycemic activity. Liraglutide's prolonged action and half-life of 11-15 hours are attributed to the attachment of the fatty acid palmitic acid to GLP-1 that reversibly binds to albumin. Albumin binding protects liraglutide from immediate degradation and elimination and causes GLP-1 to be released from abumin in a slow and consistent manner. This agent may cause thyroid C-cell tumors and increases the risk of acute pancreatitis.
lirilumab: A fully human monoclonal antibody against killer-cell immunoglobulin-like receptors (KIR), with potential antineoplastic activity. Upon administration, lirilumab binds to KIR, thereby preventing the binding of KIR ligands to KIR on natural killer (NK) cells. By blocking these inhibitory receptors, NK cells become activated and attack cancer cells leading to tumor cell death. KIR, a member of the immunoglobulin superfamily, is expressed on the surface of NK cells.
lisaftoclax: An orally bioavailable and selective inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon oral administration, lisaftoclax targets, binds to and inhibits the activity of Bcl-2. This restores apoptotic processes in tumor cells. Bcl-2 is overexpressed in many cancers and plays an important role in the negative regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival.
lisdexamfetamine dimesylate: The dimesylate form and prodrug of the d-isomer of amphetamine, a non-catecholamine sympathomimetic amine with central nervous system (CNS) stimulating activity. Upon administration, lisdexamphetamine is converted to dextroamphetamine through cleavage of the lysine group. Dextroamphetamine acts by facilitating the release of catecholamines, particularly noradrenaline and dopamine, from its storage sites in nerve terminals in the CNS, and inhibits their uptake within the mesocorticolimbic system, a major component of the brain reward system, resulting in measurable behavioral changes such as euphoria, mental alertness and excitement and appetite suppression. As a CNS stimulant, this agent may increase blood pressure.
lisinopril: An orally bioavailable, long-acting angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Lisinopril, a synthetic peptide derivative, specifically and competitively inhibits ACE, which results in a decrease in the production of the potent vasoconstrictor angiotensin II and, so, diminished vasopressor activity. In addition, angiotensin II-stimulated aldosterone secretion by the adrenal cortex is decreased which results in a decrease in sodium and water retention and an increase in serum potassium.
lisocabtagene maraleucel: A preparation of a defined ratio of CD4+ and CD8+ autologous T lymphocytes transduced with a lentiviral vector expressing a chimeric antigen receptor (CAR) containing an anti-CD19 single chain variable fragment (scFv) fused to the signaling domain of 4-1BB (CD137), the zeta chain of the TCR/CD3 complex (CD3-zeta), and a truncated form of the human epidermal growth factor receptor (EGFRt), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, lisocabtagene maraleucel is directed to and induces selective toxicity in CD19-expressing tumor cells. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. Devoid of both ligand binding domains and tyrosine kinase activity, the expressed EGFRt both facilitates in vivo detection of the administered, transduced T cells and can promote elimination of those cells through a cetuximab-induced antibody dependent cellular cytotoxicity (ADCC) response. The 4-1BB costimulatory signaling domain enhances both proliferation of T cells and antitumor activity.
Listeria monocytogenes-LLO-prostate cancer neoantigens vaccine ADXS-504: An off-the-shelf (OTS) cancer vaccine containing a live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding a fusion protein composed of specific prostate cancer (PC) neoantigens fused to a fragment of the immunostimulant listeriolysin O (LLO) protein, with potential immunostimulatory and antineoplastic activities. Upon administration of the Lm-LLO-PC neoantigens vaccine ADXS-504, the expressed LLO-PC neoantigens is processed by antigen presenting cells (APCs), presented to the immune system by both major histocompatibility complex (MHC) I and II molecules, and activates the immune system to exert both an innate and adaptive immune response involving the recruitment and activation of T lymphocytes against neoantigen-expressing prostate cancer cells as well as the inhibition of tumor-infiltrating T regulatory cells (T regs) and myeloid-derived suppressor cells (MDSCs). This further modulates the tumor microenvironment (TME) and further results in tumor cell eradication. The neoantigens in ADXS-504 are composed of public hotspot mutations and proprietary tumor associated antigen (TAAs).
Listeria monocytogenes-LLO-PSA vaccine ADXS31-142: A cancer vaccine containing a live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding a fusion protein composed of the tumor-associated antigen (TAA) human prostate-specific antigen (PSA) fused to a fragment of the immunostimulant listeriolysin O (LLO) protein, with potential immunostimulatory and antineoplastic activities. Upon administration of the Lm-LLO-PSA vaccine ADXS31-142, the expressed LLO-PSA is processed by antigen presenting cells (APCs), presented to the immune system by both major histocompatibility complex (MHC) I and II molecules, and activates the immune system to exert both an innate and adaptive immune response involving the recruitment and activation of T lymphocytes against PSA-expressing tumor cells as well as the inhibition of tumor-infiltrating T-regulatory cells (T regs) and myeloid-derived suppressor cells (MDSCs). This eventually results in tumor cell lysis.
Lithane: (Other name for: lithium carbonate)
lithium carbonate: The carbonate salt of lithium, a soft alkali metal, with antimanic and hematopoietic activities. Lithium interferes with transmembrane sodium exchange in nerve cells by affecting sodium, potassium-stimulated adenosine triphosphatase (Na+, K+-ATPase); alters the release of neurotransmitters; affects cyclic adenosine monophosphate (cAMP) concentrations; and blocks inositol metabolism resulting in depletion of cellular inositol and inhibition of phospholipase C-mediated signal transduction. The exact mechanism through which lithium exerts its mood-stabilizing effect has not been established. In addition, lithium stimulates granulocytopoiesis and appears to increase the level of pluripotent hematopoietic stem cells by stimulating the release of hematopoietic cytokines and/or directly acting on hematopoietic stem cells.
Lithobid: (Other name for: lithium carbonate)
Lithonate: (Other name for: lithium carbonate)
Lithotabs: (Other name for: lithium carbonate)
litronesib: An inhibitor of the kinesin-related motor protein Eg5 with potential antineoplastic activity. Litronesib selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and consequently cell death in tumor cells that are actively dividing. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein that plays an essential role during mitosis, particularly in the regulation of spindle dynamics, including assembly and maintenance.
live attenuated measles virus vaccine: A live, attenuated measles vaccine with potential antineoplastic activity. Upon subcutaneous administration, live attenuated measles virus vaccine may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against measles-positive tumor cells. Measles virus has been shown to be present in some non-small cell lung cancers.
live freeze-dried lactic acid bacteria probiotic: A probiotic containing live, cultivated, freeze-dried lactic acid bacteria with gastrointestinal (GI) protective, anti-inflammatory, immunomodulating and potential antitumor properties. Oral administration of probiotic bacteria help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier, interfere with the attachment of pathogenic bacteria and other harmful substances and may bind to and degrade carcinogens. This may prevent inflammation and possibly cancer. In addition, these bacteria produce lactic acid, thereby creating an acidic environment that is unfavorable for pathogens.
live-attenuated double-deleted Listeria monocytogenes bacteria JNJ-64041809: A proprietary, live-attenuated, double-deleted (LADD) strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding multiple, as of yet undisclosed, tumor-associated antigens (TAAs), with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, live-attenuated double-deleted Listeria monocytogenes bacteria JNJ-64041809 is taken up by antigen-presenting cells (APCs), including dendritic cells (DCs). The TAAs are subsequently expressed by the APCs and then processed and presented to the immune system by both major histocompatibility complex (MHC) class I and II molecules. This activates the immune system and leads to the recruitment and activation of cytotoxic T lymphocytes (CTLs) against the TAA-expressing tumor cells, eventually resulting in tumor cell lysis. Two genes contributing to the virulence of Lm have been removed to minimize the risk of infection.
live-attenuated Listeria monocytogenes encoding EGFRvIII-NY-ESO-1 vaccine ADU-623: A live-attenuated, double-deleted strain of the Gram-positive bacterium Listeria monocytogenes (Lm) encoding a mutant form of the tumor-associated antigens, epidermal growth factor receptor (EGFRvIII) and the cancer/testis antigen NY-ESO-1, with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, live-attenuated Listeria monocytogenes encoding EGFRvIII-NY-ESO-1 vaccine targets dendritic cells and expresses EGFRvIII and NY-ESO-1. This promotes both a potent innate immune response and an adaptive immune response involving the recruitment and activation of T lymphocytes against EGFRvIII and NY-ESO-1-expressing tumor cells, which results in tumor cell lysis.
live-attenuated listeria-encoding human mesothelin vaccine CRS-207: A recombinant Listeria-based cancer vaccine containing a live-attenuated strain of the facultative intracellular bacterium Listeria monocytogenes (Lm) expressing human mesothelin with potential immunostimulatory and antineoplastic activities. Upon administration of this vaccine, Listeria invade professional phagocytes within the immune system and express mesothelin, which may activate a cytotoxic T-lymphocyte (CTL) response against mesothelin-expressing tumor cells, resulting in tumor cell lysis. In addition, the Listeria vector itself may induce a potent innate and adaptive immunity unrelated to mesothelin expression. Mesothelin is a cell surface glycoprotein involved in cell adhesion and is overexpressed in many epithelial-derived cancers, including pancreatic, ovarian and lung cancers, and malignant mesotheliomas.
liver cancer neoantigens-sensitized autoimmune cells IPM001: A preparation of autoimmune cells that have been sensitized to liver cancer neoantigens, with potential immunostimulating and antineoplastic activities, Upon administration of the liver cancer neoantigens-sensitized autoimmune cells IPM001, these cells may eradicate the liver cancer cells.
livmoniplimab: A humanized monoclonal antibody directed against the transforming growth factor beta (TGFbeta) activator, glycoprotein A repetitions predominant (GARP; leucine-rich repeat-containing protein 32; LRRC32), with potential immunomodulating and antineoplastic activities. Upon administration, livmoniplimab selectively targets and binds to GARP which interferes with the production and release of active TGFbeta by regulatory T cells (Tregs). Selective inhibition of the release of TGFbeta from Tregs leads to a reversal of immunosuppression thereby increasing the immune response to tumor cells. GARP, a leucine-rich repeat-containing protein, is essential for the expression of TGFbeta on the cell surface of activated Tregs; it plays an important role in regulation of the immune cell function.
lixumista acetate: The acetate salt form of lixumistat, an orally bioavailable biguanide compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon administration, lixumistat inhibits oxidative phosphorylation, decreases mitochondrial function, prevents tumor cell metabolism and deprives tumor cells of energy, thereby preventing tumor cell proliferation. Mitochondrial OxPhos is overactivated in cancer cells and plays a key role in tumor cell proliferation. Drug resistant tumor cells are very susceptible to decreased mitochondrial OxPhos as they cannot easily compensate for the decrease in mitochondrial function by increasing glycolysis.
Lm-tLLO-neoantigens vaccine ADXS-NEO: A proprietary, personalized plasmid DNA-based cancer vaccine composed of a live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) carrying a proprietary plasmid vector encoding multiple, patient-specific, immunogenic neoepitopes fused to a truncated form of the immunostimulant listeriolysin O (tLLO), with potential immunostimulatory and antineoplastic activities. Upon administration of the Lm-tLLO-neoantigens vaccine ADXS-NEO, the ADXS-NEO is taken up by antigen presenting cells (APCs), such as dendritic cells (DCs), and the expressed tLLO-neoantigens fusion protein is processed and presented to the immune system by both major histocompatibility complex (MHC) I and II molecules. This activates the immune system to exert both innate and adaptive immune responses involving the recruitment and activation of T lymphocytes against the tumor-associated antigens (TAAs) specifically expressed by the patient's tumor cells, and inhibits the immunosuppressive tumor-infiltrating T-regulatory cells (Tregs) and myeloid-derived suppressor cells (MDSCs) within the tumor microenvironment (TME). This results in tumor cell lysis. The various unique mutation-derived TAAs that are used in ADXS-NEO are identified from a biopsy of the patient's tumor.
LMB-1 immunotoxin: A chimeric protein consisting of the Fv portion of a monoclonal antibody attached to a fragment of Pseudomonas exotoxin A without its cell-binding region. LMB-1 immunotoxin targets B3, a Lewis Y-related carbohydrate epitope found on some solid tumors. The antibody attaches to the tumor cell and the exotoxin stops protein synthesis by inactivating elongation factor 2.
LMB-2 immunotoxin: A fusion protein consisting of the Fv portion of a monoclonal antibody attached to a 38-kDa fragment of the Pseudomonas exotoxin A (with amino acids 365-380 deleted). LMB-2 immunotoxin targets the interleukin 2 receptor (also known as IL-2R or CD25) which is expressed on activated normal T and B cells and macrophages and on the cells of various hematologic malignancies. The antibody attaches to the IL-2R on the cell membrane, facilitating the entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis.
LMB-7 immunotoxin: A single chain chimeric protein consisting of a monoclonal antibody fragment attached to a portion of the Pseudomonas exotoxin A. LMB-7 immunotoxin attaches to B3, a Lewis Y-related carbohydrate epitope on some solid tumor cells. The antibody attaches to the cell and the exotoxin inhibits protein synthesis by inactivating elongation factor 2.
LMB-9 immunotoxin: A recombinant disulfide stabilized anti-Lewis Y IgG immunotoxin containing a 38 KD toxic element derived from the Pseudomonas aeruginosa exotoxin A and a monoclonal antibody fragment, designed to target adenocarcinomas expressing Lewis Y. LMB-9 immunotoxin attaches to tumor cells, facilitating he entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis.
LmddA-LLO-chHER2 fusion protein-secreting live-attenuated Listeria cancer vaccine ADXS31-164: A cancer vaccine containing a live, highly attenuated strain of the Gram-positive bacterium Listeria monocytogenes (LmddA) encoding a fusion protein composed of a chimeric peptide comprised of three highly immunogenic epitopes of the human tumor-associated antigen (TAA) HER2/neu (chHER2) fused to a non-hemolytic fragment of the immunostimulant listeriolysin O (LLO) protein, with potential immunostimulatory and antineoplastic activities. Upon administration of the LmddA-LLO-chHER2 vaccine ADXS31-142, the LmddA is taken up by phagocytic cells; then the listeriolysin portion of the expressed LLO-chHER2 can form pores in the phagolysosomes and the fusion protein can escape into the cytosol. In turn, the LLO-chHER2 is processed and presented to the immune system by major histocompatibility complex (MHC) I on the phagocytic cells. Antigen presentation activates the immune system to exert an immune response involving the recruitment and activation of T ymphocytes against HER2-expressing tumor cells, and inhibits tumor-infiltrating T-regulatory cells (Tregs) and myeloid-derived suppressor cells (MDSCs). This eventually results in tumor cell lysis. HER2/neu, a tyrosine kinase receptor belonging to the epidermal growth factor receptor (EGFR) family, is overexpressed in various tumor cell types.
LMP-2:340-349 peptide vaccine: A peptide cancer vaccine containing amino acid residues 340-349 of the Epstein-Barr virus (EBV) latent membrane protein-2 (LMP-2) with potential immunostimulating and antineoplastic activities. Vaccination with LMP-2:340-349 peptide may boost the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.
LMP-2:419-427 peptide vaccine: A peptide cancer vaccine containing amino acid residues 419-427 of the latent membrane protein-2 (LMP-2) of the Epstein-Barr virus (EBV) with potential immunostimulating and antineoplastic activities. Vaccination with the LMP-2:49-427 peptide vaccine may boost the immune system to mount a specific cytotoxic T-lymphocyte response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.
LMP/BARF1/ EBNA1-specific cytotoxic T lymphocytes: A preparation of allogeneic cytotoxic T-lymphocytes (CTL) made specifically reactive to three Epstein-Barr virus (EBV) proteins, latent membrane protein (LMP) 1, BamH1-A rightward frame-1 (BARF1) and EBV nuclear antigen 1 (EBNA1), with potential antineoplastic activity. Administration of LMP1/BARF1/ EBNA1-specific CTLs to patients with LMP1/BARF1/EBNA1-positive tumors may result in a specific CTL response against the tumor cells expressing these antigens, which can result in both cell lysis and the inhibition of tumor cell proliferation. LMP1, BARF1 and EBNA1 are expressed in various, EBV-associated malignancies, including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma.
LMP1-specific chimeric antigen receptor-expressing T lymphocytes: A preparation of cytotoxic T lymphocytes (CTL) transfected with a chimeric antigen receptor (CAR) specifically recognizing the Epstein-Barr virus (EBV) latent membrane protein 1 (LMP1; LMP-1), with potential antineoplastic activity. Upon administration of the LMP1-specific CAR-expressing T lymphocytes to patients with LMP1-positive tumors, the CTLs specifically target and lyse tumor cells expressing LMP1, thereby inhibiting tumor cell proliferation. The tumor-associated antigen (TAA) LMP1 is expressed in various malignancies, including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma.
LMP2-specific IL-12-secreting T cell receptor-transduced T lymphocytes: A preparation of T lymphocytes that have been genetically modified to encode a T-cell receptor (TCR) specific for Epstein-Barr virus (EBV) latent membrane protein (LMP) 2, with potential antineoplastic activity. Upon administration, the LMP2-specific IL-12 secreting TCR-transduced T lymphocytes (TCR-T) recognize and bind to EBV LMP2, which may promote cell death and inhibit the growth of tumor cells expressing LMP2. In addition, IL-12 expression activates the immune system by promoting the secretion of interferon-gamma, activating natural killer cells (NKs), and inducing cytotoxic T-cell responses, which may result in both decreased cell proliferation and increased cell death in LMP2-expressing tumor cells. As a tumor associated antigen (TAA), LMP2 is expressed in various EBV-associated malignancies including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma.
LMP2-specific T-cell receptor-transduced autologous T lymphocytes: A preparation of autologous T lymphocytes that have been genetically modified to express a T-cell receptor (TCR) specific for the Epstein-Barr virus (EBV) latent membrane protein (LMP) 2, with potential immunomodulating and antineoplastic activities. Upon administration, LMP2-specific TCR-transduced autologous T lymphocytes recognize and bind to LMP2, which may promote cell death and inhibit the growth of tumor cells expressing LMP2. LMP2 is expressed in various EBV-associated malignancies.
LMP2a-specific cytotoxic T-lymphocytes: A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to Epstein-Barr virus (EBV) latent membrane protein-2A (LMP2A), with potential antineoplastic activity. T-lymphocytes are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP2A. Subsequently, LMP2A-specific CTLs are exposed to EBV infected cells transfected with adenovirus encoding LMP2A, thereby further stimulating CTLs. Administered to patients with EBV-positive tumors, LMP2A-specific CTLs target LMP2A-positive cells, resulting in cell lysis and inhibition of cancer cell proliferation. EBV LMP2A may be expressed in various malignancies, including nasopharyngeal carcinoma and Hodgkin and non-Hodgkin lymphomas.
LMP7 inhibitor M3258: An orally bioavailable, potent, selective, reversible inhibitor of the large multifunctional peptidase 7 (LMP7, Beta5i, PSMB8), a chymotrypsin-like, proteolytic subunit of the immunoproteasome, with potential antineoplastic activity. Upon oral administration, LMP7 inhibitor M3258 targets and inhibits the proteolytic activity of the LMP7 subunit of immunoproteasome, thereby blocking its deubiquitylating activity. This blocks the ubiquitin proteasome degradation pathway, prevents the degradation of defective proteins, and leads to an accumulation of poly-ubiquitylated proteins. This induces the unfolded protein response (UPR) and results in both the induction of tumor cell apoptosis and the inhibition of tumor cell growth. Proteasomes are large multi-subunit protease complexes that degrade unneeded or damaged proteins that have been ubiquitinated, thereby restoring protein homeostasis. Unlike the constitutive proteasome, which is expressed in most tissues, immunoproteasome is specifically present in normal and malignant hematopoietic cells, including multiple myeloma. Immunoproteasome degrades ubiquitinated proteins, generates peptides for presentation on MHC class I, and plays a key role in the adaptive immune response and inflammatory diseases.
lobaplatin: A third-generation, water-soluble platinum compound with potential antineoplastic activity. Lobaplatin forms highly reactive, charged, platinum complexes that bind to nucleophilic groups such as GC- and AG-rich sites in DNA, inducing intrastrand DNA cross-links. These cross-links will ultimately result in induction of apoptosis and cell growth inhibition. Compared to first and second generation platinum compounds, lobaplatin appears to be more stable, less toxic, have a better therapeutic index and may overcome tumor resistance.
lobradimil: A synthetic analog of bradykinin. Lobradimil is a potent, specific bradykinin B-2 receptor agonist that stimulates B-2 receptors expressed on the surface of brain capillary endothelial cells, thereby reversibly increasing the permeability of the blood-brain barrier (BBB). Compared to bradykinin, this agent possesses enhanced receptor selectivity, greater plasma stability, and a longer half-life.
locally-acting temozolomide formulation SI-053: A powder for gel formulation containing the cytotoxic alkylating agent temozolomide (TMZ), an imidazotetrazine derivative of the alkylating agent dacarbazine, immobilized on the polymeric carrier dextran phosphate, with potential antineoplastic activity. The TMZ formulation SI-053 forms a viscous gel upon reconstitution in water. Upon local intraoperative administration of the gel into the cavity that is formed after resection of the brain tumor, SI-053 allows for local and prolonged action of TMZ. TMZ is converted at physiologic pH to the short-lived active compound 5-(3-methyl-(triazen-1-yl)-imidazole)-4-carboxamide (monomethyltriazenoimidazole carboxamide; MTIC). The cytotoxicity of MTIC is due to methylation of DNA, particularly at the O6 and N7 positions of guanine residues, resulting in cell cycle arrest, inhibition of DNA replication and the induction of apoptosis. The local administration of TMZ allows for the local destruction of the remaining tumor cells immediately after the removal of the tumor and may prevent the recurrence of tumor growth while having no severe systemic toxicity.
lodapolimab: A monoclonal antibody directed against programmed cell death-1 ligand 1 (PD-L1) with immune checkpoint inhibitory and potential antineoplastic activities. Upon administration, lodapolimab binds to PD-L1 and prevents the interaction of PD-L1 with its receptor programmed cell death protein 1 (PD-1). This inhibits the activation of PD-1 and its downstream signaling pathways, which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells.
Lodine: (Other name for: etodolac)
Lodosyn: (Other name for: carbidopa)
lometrexol: A folate analog antimetabolite with antineoplastic activity. As the 6R diastereomer of 5,10-dideazatetrahydrofolate, lometrexol inhibits glycinamide ribonucleotide formyltransferase (GARFT), the enzyme that catalyzes the first step in the de novo purine biosynthetic pathway, thereby inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation. The agent has been shown to be active against tumors that are resistant to the folate antagonist methotrexate.
lomonitinib: An orally bioavailable inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) mutations and interleukin-1 receptor-associated kinase 4 (IRAK4), with potential antineoplastic activity. Upon oral administration, lomonitinib targets, binds to and inhibits the activity of FLT3 mutations, including the FLT3-ITD-F691L gatekeeper mutation, while sparing the wild-type form of FLT3. This inhibits the proliferation of FLT3 mutant-expressing cancer cells. In addition, lomonitinib targets, binds to, and inhibits the kinase activity of IRAK4. This inhibits IRAK4-mediated signaling and may reduce adaptive resistance to FLT3 inhibition as toll-like receptor (TLR) activation plays an important role in resistance to FLT3 inhibition. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. IRAK4, a serine/threonine-protein kinase, plays a key role in both the TLR and IL-1R signaling pathways.
Lomotil: (Other name for: diphenoxylate hydrochloride/atropine sulfate)
lomustine: A nitrosourea with antineoplastic activity. Lomustine alkylates and crosslinks DNA, thereby inhibiting DNA and RNA synthesis. This agent also carbamoylates DNA and proteins, resulting in inhibition of DNA and RNA synthesis and disruption of RNA processing. Lomustine is lipophilic and crosses the blood-brain barrier.
lomvastomig: A bispecific antibody directed against both the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; TIM3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, lomvastomig simultaneously targets and binds to both TIM-3 and PD-1 expressed on certain T cells. This blocks the interaction of TIM-3 with some of its physiologic ligands and prevents the activation of PD-1 by its ligands, programmed cell death-1 ligand 1 (PD-L1) or 2 (PD-L2). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which may lead to a reduction in tumor growth. TIM-3, a transmembrane protein and immune checkpoint receptor, is often co-expressed with PD-1 on tumor-antigen-specific T cells. Dual checkpoint blockade of PD-1 and TIM-3 may enhance T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone.
lonafarnib: A synthetic tricyclic derivative of carboxamide with antineoplastic properties. Lonarfanib binds to and inhibits farnesyl transferase, an enzyme involved in the post-translational modification and activation of Ras proteins. Ras proteins participate in numerous signalling pathways (proliferation, cytoskeletal organization), and play an important role in oncogenesis. Mutated ras proteins have been found in a wide range of human cancers.
lonaprisan: An orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist; binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Unlike many other antiprogestins such as mifepristone, this agent does not appear to convert to an agonist in the presence of protein kinase A (PKA) activators and shows high antiprogestagenic activity on both progesterone receptor (PR) isoforms PR-A and PR-B.
loncastuximab tesirine-lpyl: An antibody-drug conjugate (ADC) consisting of an anti-CD19 humanized monoclonal antibody conjugated, via a cleavable linker comprised of valine-alanine and maleimide, to a cytotoxic, cross-linking agent pyrrolobenzodiazepine (PBD) dimer, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the monoclonal antibody portion of loncastuximab tesirine targets the cell surface antigen CD19 on various cancer cells. Upon antibody/antigen binding and internalization, the cytotoxic PBD moiety is released. The imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA and inhibits DNA replication, which inhibits the proliferation of CD19-overexpressing tumor cells. CD19, a transmembrane receptor and tumor-associated antigen (TAA), is expressed on a number of B-cell-derived cancers.
long PD-L1 peptide vaccine: A peptide cancer vaccine composed of a long peptide, containing amino acids 19 through 27 (FMTYWHLLNAFTVTVPKDL), obtained from the tumor-associated antigen (TAA) and immune checkpoint molecule programmed cell death-1 ligand 1 (PD-L1), with potential immunomodulating and antineoplastic activities. Upon vaccination with long PD-L1 peptide vaccine, the peptide may activate the immune system to induce an immune response against PD-L1-expressing cells. This may induce a cytotoxic T-lymphocytes (CTLs)-mediated immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed on many human cancer cell types as well as on antigen presenting cells (APCs) and immunosuppressive cells in the tumor micro-environment (TME), such as regulatory T cells (Tregs). PD-L1 binding to its cognate receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) on T cells suppresses the immune system and results in increased immune evasion and decreased CTL activation.
long peptide vaccine 7: A peptide vaccine consisting of a combination of seven synthetic long peptides (SLPs), which are each about 30 amino acids in size, and derived from cancer-testis antigens (CTA) and melanocytic differentiation proteins (MDP), with potential immunostimulating and antitumor activities. Upon administration, long peptide vaccine 7 may stimulate the host immune system to mount a cytotoxic T-cell lymphocyte (CTL) response against tumor cells expressing these peptides. CTA and MDP are overexpressed in a variety of cancer cell types.
long-acting recombinant Erwinia asparaginase JZP341: A long-acting and recombinant form of asparaginase (Erwinia asparaginase; crisantaspase), with potential antineoplastic activity. Upon administration of long-acting recombinant Erwinia asparaginase JZP-341, the recombinant asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia. This depletes cancer cells of asparagine, which blocks protein synthesis and tumor cell proliferation. Asparagine is critical to protein synthesis in cancer cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase.
long-acting release pasireotide: A long-acting release (LAR) formulation containing pasireotide, a synthetic long-acting cyclohexapeptide, with somatostatin-like activity. Upon intramuscular administration of the LAR formulation of pasireotide, this somatostatin analog strongly binds to and activates somatostatin receptor (SSTR) subtypes 1, 2, 3, and 5. This leads to an inhibition in the secretion of human growth hormone (hGH) and results in decreased production of insulin-like growth factor (IGF-1), which may inhibit IGF-1-mediated cell signaling pathways. This may lead to an inhibition in tumor cell growth and an increase in apoptosis in IGF-1-overexpressing tumor cells. In addition, this agent causes a reduction in adrenocorticotropic hormone (ACTH), which leads to an inhibition of cortisol secretion. ACTH-producing tumors cause hypersecretion of cortisol which results in many unwanted symptoms. This agent may also block other key survival pathways such as the phosphatidylinositol 3-kinase (PI3K) and the mitogen-activated protein kinase (MAPK) signaling pathways. Pasireotide also inhibits vascular endothelial growth factor (VEGF) secretion, thereby decreasing angiogenesis and tumor cell growth in VEGF-overexpressing tumor cells. The long-acting form of pasireotide allows for less frequent administration as compared to the original form of this agent. SSTRs are overexpressed by some neuroendocrine and non-neuroendocrine tumor cells.
Lonquest: (Other name for: lipegfilgrastim)
Lonquex: (Other name for: lipegfilgrastim)
Lonsurf: (Other name for: trifluridine and tipiracil hydrochloride)
loperamide hydrochloride: The hydrochloride salt form of loperamide, a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity. Loperamide acts on the mu-receptors in the intestinal mucosa. This leads to a decrease in gastrointestinal motility by decreasing the circular and longitudinal smooth muscle activity of the intestinal wall. This slows intestinal transit and allows for more water and electrolyte absorption from the intestines. Loperamide is not significantly absorbed from the gut and does not cross the blood-brain barrier. Therefore it has no central nervous system effects.
Lopid: (Other name for: gemfibrozil)
lopinavir: A protease inhibitor used against human immunodeficiency virus (HIV). Lopinavir competitively inhibits the HIV-1 protease, an enzyme that mediates the cleavage of Gag, Gag-Pol and Nef precursor polypeptides into their mature proteins, including protease, reverse transcriptase, and integrase. Inhibition of HIV-1 protease prevents cleavage of the viral polyprotein precursor and results in the release of immature, noninfectious virions.
Lopressor: (Other name for: metoprolol tartrate)
Loprox Lotion: (Other name for: ciclopirox olamine lotion)
Lopurin: (Other name for: allopurinol)
Loqtorzi: (Other name for: toripalimab-tpzi)
loratadine: A piperidine histamine H1-receptor antagonist with anti-allergic properties and without sedative effects. Loratadine blocks the H1 histamine receptor and prevents the symptoms that are caused by histamine activity on capillaries, bronchial smooth muscle, and gastrointestinal smooth muscle, including vasodilatation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscle. Loratadine does not cross the blood-brain barrier and does not cause central nervous system effects.
lorazepam: A benzodiazepine with anxiolytic, anti-anxiety, anticonvulsant, anti-emetic and sedative properties. Lorazepam enhances the effect of the inhibitory neurotransmitter gamma-aminobutyric acid on the GABA receptors by binding to a site that is distinct from the GABA binding site in the central nervous system. This leads to an increase in chloride channel opening events, a facilitation of chloride ion conductance, membrane hyperpolarization, and eventually inhibition of the transmission of nerve signals, thereby decreasing nervous excitation.
Lorbrena: (Other name for: lorlatinib)
Lorcet: (Other name for: hydrocodone/acetaminophen)
lorigerlimab: A hinge stabilized immunoglobulin G4 (IgG4) tetravalent bispecific antibody-like protein directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PDCD1; CD279) and cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, lorigerlimab specifically binds to both PD-1 and CTLA4 expressed on tumor-infiltrating lymphocytes (TILs) and inhibits the PD-1- and CTLA4-mediated downregulation of T-cell activation and proliferation. Dual blockade of PD1 and CTLA4 pathways provides enhanced activity against PD1+CTLA4+ double positive cells and may increase T-cell activation and proliferation compared to the blockade of either immune checkpoint alone.
lorlatinib: An orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. Upon administration, lorlatinib binds to and inhibits both ALK and ROS1 kinases. The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells. In addition, PF-06463922 is able to cross the blood brain barrier. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.
lorpucitinib: An orally bioavailable pan-inhibitor of the Janus associated-kinases (JAKs), with potential immunomodulatory and anti-inflammatory activities. Upon oral administration, lorpucitinib works in the gastrointestinal (GI) tract where it targets, binds to and inhibits the activity of the JAKs, thereby disrupting JAK-signal transducer and activator of transcription (STAT) signaling pathways and the phosphorylation of STAT proteins. This may inhibit the release of pro-inflammatory cytokines and chemokines, reducing inflammatory responses and preventing inflammation-induced damage. The Janus kinase family of non-receptor tyrosine kinases, which includes tyrosine-protein kinase JAK1 (Janus kinase 1; JAK1), tyrosine-protein kinase JAK2 (Janus kinase 2; JAK2), tyrosine-protein kinase JAK3 (Janus kinase 3; JAK3) and non-receptor tyrosine-protein kinase TYK2 (tyrosine kinase 2), plays a key role in cytokine signaling and inflammaton.
lorvotuzumab mertansine: An immunoconjugate of a humanized murine monoclonal antibody (huN-901) and DMI, a semi-synthetic derivative of the plant-derived ansa macrolide maytansine. The antibody moiety of lorvotuzumab mertansine selectively attaches to CD56 antigen, a neural cell adhesion molecule (NCAM)) expressed on the surface of cells of small cell lung cancer (SCLC) and other neuroendocrine (NE) tumors. Thus, the DMI conjugate is targeted specifically to CD56-expressing tumor cells, where it inhibits tubulin polymerization and assembly, resulting in inhibition of mitosis and cell cycle arrest in the S phase.
losartan: A non-peptide angiotensin II antagonist with antihypertensive activity. Upon administration, losartan and its active metabolite selectively and competitively blocks the binding of angiotensin II to the angiotensin I (AT1) receptor. This blocks the vasoconstricting and aldosterone-secreting actions of angiotensin II, leading to a decrease in blood pressure. Angiotensin II, formed from angiotensin I by angiotensin-converting enzyme (ACE), stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle.
losartan potassium: The potassium salt of losartan, a non-peptide angiotensin II receptor antagonist with antihypertensive activity. Losartan selectively and competitively binds to the angiotensin II receptor (type AT1) and blocks the binding of angiotensin II to the receptor, thus promoting vasodilatation and counteracting the effects of aldosterone. Converted from angiotensin I by angiotensin-converting enzyme (ACE), angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, decreasing sodium excretion and increasing potassium excretion, and acts as a vasoconstrictor in vascular smooth muscle.
Lotensin: (Other name for: benazepril hydrochloride)
Lotrimin: (Other name for: clotrimazole)
lovastatin: A lactone metabolite isolated from the fungus Aspergillus terreus with cholesterol-lowering and potential antineoplastic activities. Lovastatin is hydrolyzed to the active beta-hydroxyacid form, which competitively inhibits 3-hydroxyl-3-methylgutarylcoenzyme A (HMG-CoA) reductase, an enzyme involved in cholesterol biosynthesis. In addition, this agent may induce tumor cell apoptosis and inhibit tumor cell invasiveness, possibly by inhibiting protein farnesylation and protein geranylgeranylation, and may arrest cells in the G1 phase of the cell cycle. The latter effect sensitizes tumor cells to the cytotoxic effects of ionizing radiation.
Lovaxin C: (Other name for: axalimogene filolisbac)
Lovaza: (Other name for: omega-3-acid ethyl esters)
Lovenox: (Other name for: enoxaparin sodium)
Lozanoc: (Other name for: itraconazole)
LRP-1-targeted peptide-drug conjugate GRN1005: A peptide-drug conjugate containing the taxane paclitaxel covalently linked to the proprietary 19 amino acid peptide angiopep-2, in a 3:1 ratio, with potential antineoplastic activity. Upon administration, LRP-1-targeted peptide-drug conjugate GRN1005, via angiopep-2 moiety, binds to LRP-1 (low density lipoprotein receptor-related protein 1), which is highly expressed in blood brain barrier (BBB) and glioma cells. This binding allows the transcytosis of the agent across the BBB and the delivery of the cytotoxic agent paclitaxel. Compared to paclitaxel alone, GRN1005 is able to increase the concentration of paclitaxel in the brain and is also able to specifically deliver paclitaxel to LRP-1-overexpressing tumor cells, both in the brain and in the periphery.
LRP5 antagonist BI 905681: An antagonist of the lipoprotein receptor-related protein (LRP) 5, with potential antineoplastic and immunomodulating activities. Upon administration, LRP5 antagonist BI 905681 targets and binds to LRP5, thereby blocking the binding of Wnt ligands to LRP5. This prevents the formation of the serpentine receptor Frizzled (FZD)-Wnt-LRP5 trimeric complex and prevents the inactivation of the beta-catenin degradation complex, which leads to beta-catenin degradation. This inhibits the Wnt/beta-catenin signaling pathway, prevents the beta-catenin-mediated activation of Wnt target genes, and inhibits the proliferation and survival of Wnt/beta-catenin-driven tumor cells. In addition, inhibition of Wnt signaling by BI 905681 prevents Wnt-mediated immune escape, thereby re-activating the immune system, specifically inducing the activation of dendritic cells (DCs) and activation as well as infiltration of cytotoxic T cells into the tumor tissue. The FZD-Wnt-LRP5 trimeric complex induces phosphorylation of LRP5 intracellular domain leading to inactivation of the beta-catenin degradation complex, allowing beta-catenin accumulation; stabilized beta-catenin enters the nucleus and acts as a transcriptional activator of Wnt target genes. Wnt/beta-catenin signaling plays a key role in tumor cell proliferation and survival, and resistance to immunotherapy.
LRP5/6 antagonist BI 905677: A humanized biparatopic nanobody composed of two blocking domains for the Wnt ligand co-receptors lipoprotein receptor-related proteins (LRP) 5 and 6, with potential antineoplastic and immunomodulating activities. Upon administration, BI 905677 targets and binds to LRP5 and LRP6, thereby blocking the binding of Wnt ligands to LRP5/6. This prevents the activation of the Frizzled (FZD)-Wnt-LRP5/6 trimeric complex and prevents the inactivation of the beta-catenin degradation complex, which leads to beta-catenin degradation. This inhibits the Wnt/beta-catenin signaling pathway, prevents the beta-catenin-mediated activation of Wnt target genes, and inhibits the proliferation and survival of Wnt-driven tumor cells. In addition, inhibition of Wnt signaling by BI 905677 prevents Wnt-mediated immune escape, thereby re-activating the immune system, specifically inducing the activation of dendritic cells (DCs) and activation as well as infiltration of cytotoxic T cells into the tumor tissue. The FZD-Wnt-LRP5/6 trimeric complex induces phosphorylation of LRP5 or LRP6 intracellular domains leading to inactivation of the beta-catenin degradation complex, allowing beta-catenin accumulation; stabilized beta-catenin enters the nucleus and acts as a transcriptional activator of Wnt target genes. Wnt/beta-catenin signaling plays a key role in tumorigenesis and resistance to immunotherapy.
LSD1 inhibitor GSK2879552: An orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, GSK2879552 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the dimethylated form of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival.
LSD1 inhibitor SYHA1807: An orally available inhibitor of lysine-specific demethylase 1 (LSD1; KDM1A), with potential antineoplastic activity. Upon oral administration, LSD1 inhibitor SYHA1807 targets, binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1 is overexpressed in a number of tumor cell types. LSD1 acts on histone H3 as a transcription co-repressor through demethylation of lysine 4 (H3K4) or as a transcription co-activator through demethylation of lysine 9 (H3K9).
LSD1 inhibitor TAS1440: An orally available inhibitor of lysine-specific demethylase 1 (LSD1; KDM1A), with potential antineoplastic activity. Upon oral administration, LSD1 inhibitor TAS1440 specifically targets, binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1 is overexpressed in a number of tumor cell types. LSD1 acts on histone H3 as a transcription co-repressor through demethylation of lysine 4 (H3K4) or as a transcription co-activator through demethylation of lysine 9 (H3K9).
LSD1/HDAC6 inhibitor JBI-802: An orally bioavailable inhibitor of two proteins that are part of the corepressor to the silencer repressor element 1 (RE1) silencing transcription factor (REST) complex (CoREST complex): histone deacetylase (HDAC) type 6 (HDAC6; HDAC-6) and lysine-specific demethylase 1 (LSD1; KDM1A), with potential antineoplastic activity. Upon oral administration, LSD1/HDAC6 inhibitor JBI-802 targets, binds to and inhibits the activity of HDAC6, and prevents the HDAC6-mediated aggresomal degradation of ubiquitinated proteins. This results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This results in a selective transcription of tumor suppressor genes, tumor suppressor protein-mediated inhibition of tumor cell division and an induction of apoptosis in tumor cells that overexpress HDAC6. It also modulates genes involved in immune suppression. In addition, JBI-802 specifically targets, binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. HDAC6, which is upregulated in many tumor cell types, deacetylates chromatin histone proteins. LSD1 is overexpressed in a number of tumor cell types. LSD1 acts on histone H3 as a transcription co-repressor through demethylation of lysine 4 (H3K4) or as a transcription co-activator through demethylation of lysine 9 (H3K9).
lubiprostone: A bicyclic fatty acid derived from prostaglandin E1 and a chloride channel activator with laxative activity. Upon intake, lubiprostone specifically binds to and activates the type 2 chloride channel (ClC-2) in the apical membrane of the gastrointestinal epithelium. This produces an efflux of chloride ions, thereby drawing water into the gastrointestinal lumen. The resulting increased amounts of intestinal fluid soften the stool, increase motility, and improve bowel movements.
Lucanix: (Other name for: belagenpumatucel-L)
lucanthone: An orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1 (APEX1 or APE1), with anti-schistosomal and potential antineoplastic activity. Lucanthone intercalates DNA and interferes with the activity of topoisomerases I and II during replication and transcription, thereby inhibiting the synthesis of macromolecules. In addition, this agent specifically inhibits the endonuclease activity of APE1, without affecting its redox activity, resulting in unrepaired DNA strand breaks which may induce apoptosis. Therefore, lucanthone may sensitize tumor cells to radiation and chemotherapy. Furthermore, lucanthone inhibits autophagy through the disruption of lysosomal function. The multifunctional nuclease APE1 is a key component for DNA repair; its expression is often correlated with tumor cell resistance to radio- and chemotherapy.
lucatumumab: A monoclonal antibody directed against the B-cell surface antigen CD40 with potential antineoplastic activity. Lucatumumab binds to and inhibits CD40, thereby inhibiting CD40 ligand-induced cell proliferation and triggering cell lysis via antibody-dependent cellular cytotoxicity (ADCC) in cells overexpressing CD40. CD40, an integral membrane protein found on the surface of B lymphocytes, is a member of the tumor necrosis factor receptor superfamily and is highly expressed in a number of B-cell malignancies.
Lucentis: (Other name for: ranibizumab)
lucitanib: A novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity. Lucitanib inhibits VEGFR-1, -2, -3 and FGFR-1, -2 kinases in the nM range, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and FGFRs belong to the family of receptor tyrosine kinases that may be upregulated in various tumor cell types.
Ludiomil: (Other name for: maprotiline hydrochloride)
Lugol's solution: A solution composed of iodine and potassium iodide, which can be used as a reagent and antiseptic, with potential use in cancer diagnosis. The iodine in Lugol’s solution selectively binds to alpha-1,4 glucans found in polysaccharides, such as glycogen. Lugol’s solution reacts with glycogen in normal, healthy non-keratinized, squamous epithelium and the iodine-glucan complex stains the glycogen-containing cells dark brown. Cancer cells are devoid of glycogen, so these cells will stay unstained. The presence of cancer cells can be detected by the degree of staining and the neoplastic cells can be surgically removed. High-grade intraepitheial neoplasia has almost no glycogen-containing epithelium.
Lumakras: (Other name for: sotorasib)
Lumason: (Other name for: sulfur hexafluoride lipid microspheres)
Lumirem: (Other name for: ferumoxsil oral suspension)
Lumitene: (Other name for: beta carotene)
Lumoxiti: (Other name for: moxetumomab pasudotox-tdfk)
lumretuzumab: An immunoconjugate containing a glycoengineered, humanized monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3), with potential antineoplastic activity. Upon administration, lumretuzumab binds to the extracellular domain of HER3 and inhibits HER3 dimerization; thereby, preventing EGFR-dependent signaling. In addition, RO5479599 stimulates the immune system to exert antibody-dependent cellular cytotoxicity (ADCC). This may decrease proliferation of HER3-overexpressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors; it has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.
lumrotatug: A monoclonal antibody directed against the human cell surface glycoprotein ADP-ribosyl cyclase 1 (CD38), with potential antineoplastic activity. Upon administration, lumrotatug specifically targets and binds to CD38 expressed on tumor cells. This may trigger antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), antibody-dependent cellular phagocytosis (ADCP) and apoptosis, resulting in cell lysis and depletion of CD38-expressing tumor cells. In addition, lumrotatug inhibits the extracellular enzyme activity of CD38. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies. It plays an important role in the regulation of migration and receptor-mediated adhesion, as well as various cell functions through its multiple ecto- and endo-enzymatic activities.
Lunesta: (Other name for: eszopiclone)
lung tumor-associated antigen: A tumor-associated antigen derived from the cell surface antigen of lung cancer cells. Lung tumor-associated antigen could be used as a diagnostic marker or as a form of immunotherapy targeted against lung cancer cells.
lung-targeted immunomodulator QBKPN: A proprietary, lung-targeted, site specific immunomodulator (SSI), with potential immunostimulating and antineoplastic activities. Although the exact type and composition of the lung-targeted immunomodulator QBKPN has yet to be fully disclosed, upon subcutaneous administration, this agent is able to activate a local innate immune response in the lung tissue. This results in an increased number of M1 macrophages, which induces a shift from M2 to M1 macrophage dominance in the tumor microenvironment, and stimulates the recruitment of other immune cells. The M1 macrophages exert antitumor activity and eradicate lung cancer cells through phagocytosis. QBKPN does not induce a systemic immune response or affect other organs or tissues. Altogether, this SSI may decrease tumor cell growth in the lungs. SSIs contain specific, inactivated components of pathogens, such as bacteria and/or viruses, which normally cause an acute infection in the specific organ or tissue of interest.
lunresertib: An orally bioavailable inhibitor of the human membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1), with potential antineoplastic activity. Upon oral administration, lunresertib targets, binds to and inhibits the activity of PKMYT1. This results in the inhibition of CDK1 phosphorylation, which may promote both premature mitosis and a prolonged mitotic arrest, and lead to the accumulation of unrepaired DNA damage and apoptosis in susceptible tumor cells, such as CCNE1-overexpressing tumor cells. PKMYT1 phosphorylates CDK1 specifically when CDK1 is complexed to cyclins, which blocks progression from G2 into mitosis.
Lunsumio: (Other name for: mosunetuzumab-axgb)
Lupron Depot: (Other name for: leuprolide acetate)
lurbinectedin: A synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. Lurbinectedin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death.
lurtotecan: A semisynthetic analogue of camptothecin with antineoplastic activity. Lurtotecan selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. As a consequence of the formation of this complex, both the initial cleavage reaction and religation steps are inhibited and subsequent collision of the replication fork with the cleaved strand of DNA results in inhibition of DNA replication, double strand DNA breakage and triggering of apoptosis. Independent from DNA replication inhibition, lurtotecan also inhibits RNA synthesis, multi-ubiquitination and degradation of topoisomerase I and chromatin reorganization.
luspatercept-aamt: A soluble, recombinant fusion protein composed of a modified form of the extracellular domain of human activin receptor type IIb (ActRIIb) and linked to the human IgG1 Fc domain, with red blood cell stimulating activity. Upon subcutaneous administration, luspatercept-aamt inhibits several ligands in the transforming growth factor (TGF)-beta superfamily. This prevents activation of a variety of TGF-beta superfamily members involved in late stage erythropoiesis and results in an increased differentiation and proliferation of erythroid progenitors. Luspatercept-aamt acts at a different, later stage than erythropoietin. This agent ultimately enhances red blood cell production and prevents anemia.
Lutathera: (Other name for: lutetium Lu 177 dotatate)
Luteohormone: (Other name for: therapeutic progesterone)
luteolin: A naturally-occurring flavonoid, with potential anti-oxidant, anti-inflammatory, apoptosis-inducing and chemopreventive activities. Upon administration, luteolin scavenges free radicals, protects cells from reactive oxygen species (ROS)-induced damage and induces direct cell cycle arrest and apoptosis in tumor cells. This inhibits tumor cell proliferation and suppresses metastasis.
lutetium Lu 177 AB-3PRGD2: A radiopharmaceutical agent comprised of a pegylated cyclic arginine-glycine-aspartic acid (RGD) dimer (PRGD2) labeled with lutetium Lu 177, with potential antineoplastic activity against alphaVbeta3 integrin-expressing tumor cells. Upon administration of lutetium Lu 177 AB-3PRGD2, the RGD moiety binds to alphaVbeta3 integrin on alphaVbeta3 integrin-expressing tumor cells. The tumor cells can be eradicated upon direct cytotoxicity through beta radiation. AlphaVbeta3 integrin, a member of the integrin receptor family, is overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells; this receptor plays a key role in angiogenesis, tumor proliferation and survival.
lutetium Lu 177 anti-CA19-9 monoclonal antibody 5B1: A radioimmunoconjugate comprised of a human monoclonal antibody (huMAb-5B1) against the carbohydrate antigen sialyl Lewis A (carbohydrate antigen 19-9; CA19-9) that is conjugated to the chelator 2-(p-isothiocyanatobenzyl)-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-A''-DTPA) and labeled with the beta-emitting radioisotope lutetium Lu 177 (Lu 177), with radioisotopic activity and potential use as an antineoplastic radiotherapeutic and an imaging agent in both planar imaging and single-photon emission computed tomography (SPECT). The antibody moiety of Lu 177 anti-CA19-9 monoclonal antibody 5B1 targets and binds to CA19-9-expressing tumor cells. This may promote killing of CA19-9-expressing tumor cells through the local induction of both complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). Additionally, upon binding and internalization, the Lu 177 moiety can deliver a cytotoxic dose of beta radiation to the CA19-9-expressing tumor cells. Furthermore, the radioisotope moiety may be imaged using planar imaging and SPECT, thus allowing evaluation of the pharmacokinetic profile of the agent, and the imaging and quantification of CA19-9-expressing tumor cells, respectively. CA19-9, a Lewis-type carbohydrate antigen overexpressed on a number of different tumor cell types, plays a key role in tumor cell survival and metastasis.
lutetium Lu 177 anti-PD-L1 nanobody RAD204: A radioimmunoconjugate composed of a nanobody directed against programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274) and labeled with the beta-emitting radioisotope lutetium Lu 177, with potential imaging activity of PD-L1 tumor antigen expression during single-photon emission computerized tomography/computerized tomography (SPECT/CT) and with potential antineoplastic activity. Upon administration of lutetium Lu 177 anti-PD-L1 nanobody RAD204, the RAD204 moiety targets and binds to the PD-L1 expressed on certain tumor cells. Upon uptake and imaging, the radioisotope moiety can be visualized and the extent of PD-L1 expression can be assessed. Also, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to PD-L1-expressing tumor cells. PD-L1, a transmembrane protein, is overexpressed on the surface of many cancer cell types.
lutetium Lu 177 DOTA-biotin: A radioconjugate of biotin conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with the beta-emitting isotope lutetium Lu 177 (Lu-177) that can be used for radioimmunotherapeutic purposes. Lutetium Lu 177 DOTA-biotin could be used in pre-targeting radioimmunotherapy, which pretreats the lesion with oxidized avidin that binds to protein amino groups on cells. As avidin binds to biotin, the radioisotope can be selectively delivered to cancer cells leading to tumor cell eradication.
lutetium Lu 177 DOTA-N3-CTT1403: A radioconjucate consisting of CTT1403, a phosphoramidate-based irreversible inhibitor of human prostate-specific membrane antigen with an albumin binding moiety, connected via click chemistry to lutetium Lu 177-dodecanetetraacetic acid-azide (177Lu-DOTA-N3), with potential antineoplastic activity. Upon administration, lutetium Lu 177-DOTA-N3-CTT1403 targets and binds to PSMA expressed on tumor cells via its CTT1403 moiety, and upon internalization, delivers cytotoxic beta radiation directly to PSMA-expressing tumor cells. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on most prostate tumor cells. The albumin binding motif extends circulation half-life thereby improving tumor cell uptake of the radioconjugate.
lutetium Lu 177 DOTA-tetulomab: A radioimmunoconjugate, which consists of a monoclonal antibody against the cell-surface antigen CD37 covalently linked, via the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. The antibody moiety of lutetium Lu 177 DOTA-tetulomab binds to CD37 on tumor B-cells. Upon internalization, the radioisotope moiety delivers a cytotoxic dose of beta radiation to CD37-expressing tumor cells. CD37, a transmembrane glycoprotein, is overexpressed in B-cell malignancies.
lutetium Lu 177 dotatate: A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential imaging and antineoplastic activities. Lutetium Lu 177 dotatate binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Tyr3-octreotate (TATE) is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NET and their metastases, while most other normal tissues express low levels of SSTRs.
lutetium Lu 177 DPI-4452 Debio 0228: A radioconjugate composed of the DOTA cyclic peptide DPI-4452, a carbonic anhydrase IX (CAIX; CA9)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against CAIX-expressing tumor cells. Upon intravenous administration, lutetium Lu 177 DPI-4452 Debio 0228 targets and binds to CAIX-expressing tumor cells. Upon binding, CAIX-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. CAIX is a hypoxia-inducible transmembrane glycoprotein that catalyzes the reversible reaction and rapid interconversion of carbon dioxide and water to carbonic acid, protons, and bicarbonate ions. Induced by hypoxia, CAIX is overexpressed in various hypoxic tumors and plays a key role in intra- and extracellular pH regulation, cancer cell progression, tumor aggressiveness ad resistance to treatment.
lutetium Lu 177 EB-PSMA-617: A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the Evans blue (EB) moiety and linked via the macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 EB-PSMA-617, EB-PSMA-617 targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors. EB-PSMA-617 also binds to serum albumin, which extends its circulation half-life. This may improve tumor uptake and efficacy of the agent.
lutetium Lu 177 FF58: A radioconjugate composed of FF58, a non-arginine-glycine-aspartic acid (Arg-Gly-Asp/RGD) small molecule targeting the transmembrane receptors integrin alpha V beta 3 (avb3) and 5 (avb5), linked to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against integrin avb3/5-expressing tumor cells. Upon administration, lutetium Lu 177 FF58 targets and binds to integrin avb3/5-expressing tumor cells. Upon binding, integrin avb3/5-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. Integrin avb3/5, members of the integrin receptor family, are overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells; they play key roles in angiogenesis, tumor proliferation and survival.
lutetium Lu 177 LNC1004: A radioconjugate consisting of an Evans blue (EB) modified fibroblast activation protein inhibitor (FAPi), conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecane tetraacetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration of lutetium Lu 177 LNC1004, the FAPi moiety targets and binds to FAP-expressing cancer-associated fibroblasts (CAFs). Upon binding and internalization, the radioconjugate specifically delivers a cytotoxic dose of beta radiation to FAP-expressing CAFs. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
lutetium Lu 177 ludotadipep: A radioconjugate composed of ludotadipep, a prostate-specific membrane antigen (PSMA)-targeting agent, linked to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon administration, lutetium Lu 177 ludotadipep targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
lutetium Lu 177 monoclonal antibody CC49: A radioimmunoconjugate of the humanized monoclonal antibody (MoAb) CC49 labeled with lutetium 131 (Lu-177). MoAb CC49 binds to the pancarcinoma tumor-associated glycoprotein (TAG)-72 with high affinity. Lu-177 MoAb CC49 delivers gamma radiation emitting Lu-177 nuclide directly to tumor cells that express TAG-72, and so may be used in radioimmunotherapeutic treatment of cancers.
lutetium Lu 177 NYM032: A radioconjugate composed of NYM032, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration, lutetium Lu 177 NYM032 targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by direct cytotoxicity through beta radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
lutetium Lu 177 PP-F11N: A radioconjugate composed of PP-F11N, a gastrin analog, conjugated to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and potential use as an imaging agent for scintigraphy. Following intravenous administration, the PP-F11N moiety binds to the cholecystokinin-2 (CCK-2) receptor. Subsequently, the CCK-2 receptor-expressing tumor cells can be visualized scintigraphically. In addition, the radioisotope moiety delivers a cytotoxic dose of beta radiation to CCK-2 receptor-expressing tumor cells. CCK-2 receptors are expressed on a variety of tumor cell types.
lutetium Lu 177 PSMA-10.1: A radioconjugate composed of PSMA-10.1, a prostate-specific membrane antigen (PSMA)-targeting ligand and radiolabeled with the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 PSMA-10.1, PSMA-10.1 targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
lutetium Lu 177 PSMA-EB-01: A radioconjugate composed of PSMA-EB-01, a human prostate-specific membrane antigen (PSMA)-targeting ligand conjugated to the Evans blue (EB) moiety, and linked to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 PSMA-EB-01, PSMA-EB-01 targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors. The EB moiety of PSMA-EB-01 binds to serum albumin, which extends its circulation half-life. This may improve tumor uptake and efficacy of the agent.
lutetium Lu 177 rsopatamab tetraxetan: A radioimmunoconjugate consisting of rosopatamab, a humanized monoclonal antibody (MoAb) against the external domain of the prostate-specific membrane antigen (PSMA) that is linked, via the chelating agent, dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and imaging activity during single-photon emission computerized tomography/computerized tomography (SPECT/CT). Upon administration, lutetium Lu 177 rosopatamab tetraxetan binds to PSMA expressed on certain tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to PSMA-expressing cells. PSMA is overexpressed in the malignant prostate and its metastases.
lutetium Lu 177 satoreotide tetraxetan: A radioconjugate consisting of the somatostatin antagonistic peptide satoreotide tetraxetan (JR11) that is linked, via the chelating agent dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and imaging activity during positron emission tomography/computed tomography (PET/CT). Upon administration, lutetium Lu 177-DOTA-JR11 binds to somatostatin receptors (SSTRs), with high affinity for SSTR2, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most normal tissues express low levels of SSTRs.
lutetium Lu 177 vipivotide tetraxetan: A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 vipivotide tetraxetan, vipivotide tetraxetan targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
lutetium Lu 177 XT117: A radioconjugate composed of XT117, a fibroblast activation protein inhibitor (FAPi), conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against FAP-expressing cancer-associated fibroblasts (CAFs). Upon administration, lutetium Lu 177 XT117 targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing CAFs are destroyed by 177Lu through the specific delivery of beta particle radiation. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME) of various cancers.
lutetium Lu 177-capromab: A radioimmunoconjugate consisting of capromab linked to lutetium Lu 177 via the bifunctional macrocyclic chelator methoxy-tetraazacyclododecane-tetraacetic acid (MeO-DOTA) with potential antineoplastic activity. Lutetium Lu 177-capromab binds to human prostate specific membrane antigen (PSMA) expressed on tumor cell surfaces via its capromab moiety and, upon internalization, delivers cytotoxic beta radiation directly to PSMA-expressing tumor cells. PSMA is a cell surface glycoprotein abundantly expressed by prostate epithelium and is typically overexpressed by prostate cancer cells.
lutetium Lu 177-DOTA: A radioconjugate composed of the chelating agent 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) labeled with the beta-emitting isotope lutetium Lu 177 (Lu-177), that can be used for radioimmunotherapeutic purposes. Upon administration, Lu-177-DOTA may act as a hapten for pretargeted radioimmunotherapy, and delivers targeted beta radiation.
lutetium Lu 177-DOTA-ABM-5G: A radioconjugate composed of 5G, an agent targeting an as of yet undisclosed target, conjugated, via the bifunctional, macrocyclic chelating agent 1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetra-acetic acid (DOTA) and an albumin binding moiety (ABM), to the radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration of lutetium Lu 177-DOTA-ABM-5G, the 5G moiety targets and binds to a specific target on tumor cells. Upon binding, lutetium Lu 177 delivers a cytotoxic dose of beta radiation to the tumor cells.
lutetium Lu 177-DOTA-di-HSG peptide IMP-288: A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide lutetium (Lu) 177. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered Lu-177-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; Lu-177 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized scintigraphically.
lutetium Lu 177-DOTA-EB-TATE: A radioconjugate consisting of Evans blue (EB) modified, tyrosine-containing somatostatin analog, Tyr3-octreotate (TATE), conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecane tetraacetic acid (DOTA), and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential imaging and antineoplastic activities. Upon intravenous administration, Lutetium Lu 177-DOTA-EB-TATE binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTRs (SSTR2s), present on the cell membranes of many neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR2-positive cells. The incorporation of an albumin-binding moiety through EB modification allows Lutetium Lu 177-DOTA-EB-TATE to reversibly bind to endogenous albumin, potentially extending half-life and increasing targeted accumulation of the drug in tumors. SSTRs, especially SSTR2s, are expressed at relatively higher levels in many tumor cell types and tumor blood vessels, compared to normal tissues.
lutetium Lu 177-DOTA-IPN01087: A radioconjugate consisting of the neurotensin receptor type 1 (NTR1) antagonist, IPN01087 (3BP-227), that is linked, via the chelating agent, dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity and imaging activity during positron emission tomography/computed tomography (PET/CT). Upon administration, lutetium Lu 177-DOTA-IPN01087 binds to NTR1 expressed on certain tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to NTR1-expressing cells. NTR1, a G-protein coupled receptor, is highly expressed in ductal pancreatic adenocarcinoma but not in normal pancreatic tissue.
lutetium Lu 177-DTPA-omburtamab: A radioimmunoconjugate consisting of omburtamab, a murine immunoglobulin G1 (IgG1) antibody directed against the surface immunomodulatory glycoprotein human B7-homolog 3 (B7-H3, CD276), conjugated, via the chelating agent diethylenetriaminepentaacetic acid (DTPA), to the radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon intracerebroventricular administration of lutetium Lu 177-DTPA-omburtamab, the omburtamab moiety binds to B7-H3 expressed on certain tumor cells. Upon binding, lutetium Lu 177-DTPA-omburtamab delivers a cytotoxic dose of beta radiation to B7-H3-expressing cells. B7-H3, a type I transmembrane protein and a member of the B7 co-stimulatory protein superfamily, is overexpressed on certain tumor cell types and on various immune cells but is minimally expressed by normal human tissues. B7-H3 is a negative regulator of T-cell activation; its overexpression plays a key role in immuno-evasion, tumor cell invasion and metastasis, and is correlated with poor prognosis.
lutetium Lu 177-EB-LM3: A radioconjugate composed of LM3, a human somatostatin receptor (SSTR) antagonist, conjugated to the albumin-binding dye Evans blue (EB) and linked to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against SSTR-expressing tumor cells. Upon administration, lutetium Lu 177-EB-LM3 targets and binds to SSTRs that are present on the cell membranes of many types of neuroendocrine tumors (NETs). Upon binding, SSTR-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. This agent also binds to serum albumin with its EB moiety which increases this agent’s half-life and decreases its rate of clearance. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTRs.
lutetium LU 177-edotreotide: A radioconjugate consisting of the somatostatin analogue edotreotide labeled with lutetium Lu 177 with potential antineoplastic activities. Lutetium Lu 177-edotreotide binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide (Tyr3-octreotide or TOC) and chelated by the bifunctional, macrocyclic chelating agent dodecanetetraacetic acid (DOTA).
lutetium Lu 177-NeoB: A radioconjugate consisting of the gastrin-releasing peptide receptor (GRPR) antagonist, NeoB, linked via the chelating agent, dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration, lutetium Lu 177 NeoB targets and binds to GRPRs present on certain tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to GRPR-expressing cells. GRPR, also known as bombesin receptor subtype 2, is a G protein-coupled receptor that is overexpressed in some cancer types.
lutetium Lu 177-PSMA-I&T: A radioconjugate composed of PSMA-I&T, a human prostate-specific membrane antigen (PSMA)-targeting ligand linked, via the bifunctional, macrocyclic chelating agent 1,4,7,10-tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid (DOTAGA; DOTA-GA), to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon administration of lutetium Lu 177-PSMA-I&T, PSMA-I&T targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
lutetium Lu-177 girentuximab: A radioimmunoconjugate consisting of the chimeric monoclonal antibody cG250 linked to the low energy beta-emitting radioisotope Lutetium 177, via the bifunctional macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), with potential antineoplastic activity. The antibody moiety of lutetium Lu-177-DOTA-chimeric monoclonal antibody cG250 binds to renal cell carcinoma (RCC) cells expressing the RCC-associated antigen G250; a cytotoxic dose of beta radiation is selectively delivered to G250-expressing RCC cells upon internalization of the radioimmunoconjugate.
lutetium Lu-177 PNT2002: A radioconjugate composed of PNT2002, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity. Upon administration of lutetium Lu-177 PNT2002, the PNT2002 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on the majority of prostate tumor cells.
lutetium Lu-177 PSMA-R2: A radioconjugate composed of PSMA-R2, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of 177Lu-PSMA-R2, the PSMA-R2 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on the majority of prostate tumor cells.
Lutex: (Other name for: motexafin lutetium)
lutikizumab: A dual-variable domain (DVD) immunoglobulin G1 kappa (IgG1k) against the inflammatory cytokine human interleukin-1 alpha (IL-1a) and beta (IL-1b), with potential anti-inflammatory activity. Upon administration, lutikizumab targets, binds to, and neutralizes IL-1a/b thereby preventing the activity of IL-1a and IL-1b. This may inhibit IL1a/b-mediated inflammatory responses. This may reduce pain and slows tissue destruction and structural progression in diseases in which IL-1a/b are upregulated. IL1a/b, inflammatory mediators, play key roles in immune regulation and inflammatory processes.
Lutrin: (Other name for: motexafin lutetium)
luveltamab tazevibulin: An antibody drug conjugate (ADC) composed of SP8166 (H01), an anti-folate receptor alpha (FolRa; FOLR1) human immunoglobulin G1 (IgG1) antibody, conjugated to a proprietary cleavable drug linker, SC239, containing a tubulin-targeting 3-aminophenyl hemiasterlin warhead, SC209, with potential antineoplastic activity. Upon intravenous administration, the SP8166 antibody moiety targets and binds to FolRa expressed on certain tumor cells. Upon binding, internalization, and enzymatic cleavage, the cytotoxic SC209 moiety induces tumor cell death in FolRa-expressing cells. FolRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers including serous and epithelial ovarian cancer, endometrial adenocarcinoma, non-small cell lung cancer and triple negative breast cancer. In contrast, FolRa expression is limited in normal tissues.
Luvox: (Other name for: fluvoxamine maleate)
LV.IL-2/B7.1-transduced AML blast vaccine: A whole-cell cancer vaccine, containing human acute myeloid leukemic (AML) blasts that have been genetically engineered to express a B7.1/IIL-2 fusion protein encoded by a self-inactivating lentiviral vector (LV), with potential antineoplastic and immunomodulating activities. Upon administration, LV.IL-2/B7.1-transduced AML blast vaccine may stimulate a host cytotoxic T lymphocyte (CTL) response against AML cells. The single fusion protein encoded by the LV is postsynthetically cleaved to produce biologically active membrane-anchored B7.1 and secreted IL-2 in AML blasts; combined expression of IL-2 and the co-stimulatory molecule B7.1 by AML blasts may increase stimulation of both allogeneic and autologous cytotoxic T cells.
LY6K/VEGFR1/VEGFR2 multipeptide vaccine: A multipeptide vaccine consisting of peptides derived from lymphocyte antigen 6 complex locus K (LY6K) and type I and II vascular endothelial growth factor receptors (VEGFRs) with potential antineoplastic activity. Upon administration, LY6K/VEGFR1/VEGFR2 multipeptide vaccine may elicit an antitumor cytotoxic T-lymphocyte (CTL) immune response against LY6K-expressing tumor cells and/or VEGFR-expressing vascular endothelial cells involved in tumor angiogenesis. LY6K is a tumor-associated antigen (TAA) that occurs singly in glycosylphosphatidyl-inositol (GPI)-linked cell-surface glycoproteins or as three-fold repeated domain in the urokinase-type plasminogen activator receptor; VEGFRs are cell surface receptors that stimulate endothelial cell proliferation, invasion, angiogenesis, and vasculogenesis upon ligand binding and receptor activation.
Lyc-O-Mato: (Other name for: lycopene)
lycopene: A linear, unsaturated hydrocarbon carotenoid, the major red pigment in fruits such as tomatoes, pink grapefruit, apricots, red oranges, watermelon, rosehips, and guava. As a class, carotenoids are pigment compounds found in photosynthetic organisms (plants, algae, and some types of fungus), and are chemically characterized by a large polyene chain containing 35-40 carbon atoms; some carotenoid polyene chains are terminated by two 6-carbon rings. In animals, carotenoids such as lycopene may possess antioxidant properties which may retard ageing and many degenerative diseases. As an essential nutrient, lycopene is required in the animal diet.
Lymphazurin: (Other name for: isosulfan blue)
Lymphir: (Other name for: denileukin diftitox-cxdl)
LymphoCide: (Other name for: epratuzumab)
lymphodepleted autologous CD4-directed CAR T cells: A preparation of autologous peripheral blood T lymphocytes (PBTLs) that have been genetically modified to express a chimeric antigen receptor (CAR) specific for the T-cell surface antigen CD4, administered with lymphodepletion, with potential immunostimulating and antineoplastic activities. Upon administration, lymphodepleted autologous CD4-directed CAR T cells specifically recognize and kill CD4-expressing tumor cells. CD4, a tumor-associated antigen (TAA), is overexpressed in various lymphomas, including peripheral T-cell lymphoma, angioimmunoblastic T-cell lymphoma and anaplastic large cell lymphoma.
lymphoid progenitor cell: A hematopoietic stem cell that is committed to differentiate into T cells, B cells, and natural killer (NK) cells.
lymphokine-activated killer cells: Killer cell lymphocytes activated in the presence of interleukin-2 (IL-2). Lymphokine-activated killer cells (LAKs) are cytotoxic effector cells with an exceptionally wide target cell spectrum including normal and malignant cells of different origins. LAK cells exhibit a profound heterogeneity with regard to phenotype surface marker expression; it remains to be determined if they represent a unique cell lineage.
Lymphoseek: (Other name for: technetium Tc 99m-labeled tilmanocept)
LymphoStat-B: (Other name for: belimumab)
Lynparza: (Other name for: olaparib)
lyophilized black raspberry lozenge: A lozenge containing lyophilized black raspberry with potential antioxidant, pro-apoptotic and chemopreventive activities. In addition to vitamins, minerals, and phytosterols, black raspberries are rich in flavonols. Of the flavonols present in this agent, the anthocyanins appear to contribute significantly to this agent’s chemopreventive effects by inhibiting the activation of several signal transduction pathways, including the mitogen-activated protein kinase-mediated pathways, and certain transcription factors, such as nuclear factor kappa B (NF-kB), activator protein-1 (AP-1) complex, and nuclear factor in activated T-cells (NFAT). This in turn modulates the expression of downstream target genes that are upregulated in a variety of cancer cell types, including inducible nitric oxide synthase, cyclooxygenase-2, vascular endothelial growth factor and the anti-apoptotic protein survivin.
lyophilized black raspberry saliva substitute: A saliva substitute (or artificial saliva) containing lyophilized black raspberry with potential antioxidant, pro-apoptotic and chemopreventive activities. In addition to vitamins, minerals and phytosterols, black raspberries are rich in flavonols of which the anthocyanins appear to contribute significantly to this agent’s chemopreventive effects. Anthocyanins inhibit the activation of several signal transduction pathways, including the mitogen-activated protein kinase-mediated pathways, and certain transcription factors, such as nuclear factor kappa B (NF-kB), activator protein-1 (AP-1) complex, and nuclear factor in activated T-cells (NFAT). This in turn modulates the expression of downstream target genes that are upregulated in a variety of cancer cell types, including inducible nitric oxide synthase, cyclooxygenase-2, vascular endothelial growth factor and the anti-apoptotic protein survivin.
lyophilized human recombinant interferon-beta 1a FP-1201: A lyophilized form of recombinant human interferon (IFN) beta-1a (rhIFNb-1a), with potential protective activity. Upon dissolution of lyophilized rhIFNb-1a FP-1201 and intravenous administration, IFNb-1a upregulates the expression of and increases the levels of 5’-nucleotidase (CD73). This induces adenosine monophosphate (AMP) degradation and the production of adenosine. Adenosine acts to enhance endothelial barrier function via adenosine receptor activation and may prevent or reduce the increased vascular leakage that is due to the lack of adenosine. By increasing adenosine, rhIFNb-1a may protect the lining of blood vessels and thereby reduce inflammation. In addition, FP-1201 may prevent cytokine release syndrome (CRS) and immune effector cell associated-neurotoxicity syndrome (ICANS) toxicities in certain patients receiving CAR T-cell therapy. CD73 is abundantly expressed by normal endothelial cells.
lyophilized inactivated group A Streptococcus TARA-002: A lyophilized formulation containing cultures of the low-virulent Su strain of group A Streptococcus pyogenes, treated and killed with penicillin G, with potential immunostimulating and antineoplastic activities. Upon intravesical administration, lyophilized inactivated group A Streptococcus TARA-002 may, as an immunostimulant, activate both the innate and adaptive immune system. This enhances neutrophils, monocytes and lymphocyte tumor infiltration and increases the production of key immune mediators, including interleukins IL-6, IL-8, IL-12, interferon (IFN)-gamma and tumor necrosis factor (TNF)-alpha, and vascular endothelial growth factor (VEGF), thereby inducing antitumor immune responses. TARA-002 is based on the same master cell bank of genetically distinct group A Streptococcus pyogenes as OK-432.
Lyrica: (Other name for: pregabalin)
lysine-specific demethylase 1 inhibitor INCB059872: An orally available inhibitor of lysine-specific demethylase 1 (LSD1; lysine-specific histone demethylase 1A; KDM1A), with potential antineoplastic activity. Upon administration, INCB059872 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. Altogether, this may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family, is overexpressed in certain tumor cells and plays a key role in the regulation of gene expression and in tumor cell growth and survival.
lyso-thermosensitive liposomal doxorubicin: A temperature-sensitive liposomal formulation of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Upon intravenous administration, circulating thermosensitive liposomes are activated locally by increasing the tumor temperature to 40-41 degrees Celsius using an external heat source. The elevated temperature causes compositional changes in the liposomes, creating openings that allow for the release of encapsulated doxorubicin. Compared to non-thermosensitive liposomes, lyso-thermosensitive liposomes deliver higher concentrations of a cytotoxic agent to a heat-treated tumor site while sparing normal tissues unexposed to heat treatment.
Lysodren: (Other name for: mitotane)
Lysteda: (Other name for: tranexamic acid)
Lytgobi: (Other name for: futibatinib)