NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

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aminolevulinic acid hydrochloride
A topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid hydrochloride (ALA HCl) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect. Check for active clinical trials using this agent. (NCI Thesaurus)
aminophylline
A methylxanthine and derivative of theophylline. Aminophylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Aminophylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart. Check for active clinical trials using this agent. (NCI Thesaurus)
aminopterin
A synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analogue, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synthesis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. Check for active clinical trials using this agent. (NCI Thesaurus)
aminothiadiazole
A synthetic derivative of nicotinamide adenine dinucleotide (NAD). Aminothiadiazole competitively inhibits inosine 5-monophosphate dehydrogenase, thereby disrupting the regulation of cell proliferation and differentiation in a number of cells. This agent is also a selective human adenosine A3 receptor antagonist. Check for active clinical trials using this agent. (NCI Thesaurus)
amiodarone hydrochloride
The hydrochloride salt of an iodine-rich benzofuran derivative with antiarrhythmic and vasodilatory activities. As a class III antiarrhythmic agent, amiodarone blocks the myocardial calcium, potassium and sodium channels in cardiac tissue, resulting in prolongation of the cardiac action potential and refractory period. In addition, this agent inhibits alpha- and beta-adrenergic receptors, resulting in a reduction in sympathetic stimulation of the heart, a negative chronotropic effect, and a decrease in myocardial oxygen demands. Amiodarone may cause vasodilation by stimulation of the release of nitric oxide and cyclooxygenase-dependent relaxing endothelial factors. Check for active clinical trials using this agent. (NCI Thesaurus)
Amitiza
(Other name for: lubiprostone)
amitriptyline hydrochloride
The hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities. Amitriptyline inhibits the re-uptake of norepinephrine and serotonin by the presynaptic neuronal membrane in the central nervous system (CNS), thereby increasing the synaptic concentration of norepinephrine and serotonin. Due to constant stimulation to these receptors, amitriptyline may produce a downregulation of adrenergic and serotonin receptors, which may contribute to the antidepressant activity. In the CNS the antinociceptive activity of this agent may involve high affinity binding to and inhibition of N-methyl-D-aspartate (NMDA) receptors and/or the enhancement of the action of serotonin at the spinal terminals of an opioid-mediated intrinsic analgesia system. Check for active clinical trials using this agent. (NCI Thesaurus)
amivantamab
A human bispecific antibody targeting both epidermal growth factor receptor EGFR and hepatocyte growth factor receptor (HGFR; cMet), with potential antineoplastic activity. Upon administration, amivantamab simultaneously targets and binds to wild-type or certain mutant forms of both EGFR and cMet expressed on cancer cells, thereby preventing receptor phosphorylation. This prevents the activation of both EGFR- and cMet-mediated signaling pathways. In addition, binding results in receptor degradation, which further inhibits EGFR- and cMet-mediated signaling. JNJ-61186372 also causes antibody-dependent cellular cytotoxicity (ADCC). Altogether, this results in the inhibition of tumor cell proliferation. EGFR and cMet, both upregulated or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
AML mRNA plus lysate loaded autologous dendritic cell vaccine
A cancer vaccine consisting of autologous dendritic cells loaded with separate preparations of acute myelogenous leukemia (AML) cell lysate and AML-specific messenger RNA (mRNA) with potential immunostimulatory and antineoplastic activities. Upon administration, AML mRNA plus lysate loaded autologous dendritic cell vaccine may elicit a potent cytotoxic T-cell (CTL) response against AML cells, resulting in tumor cell death. Autologous dendritic cells doubly-loaded with AML cell lysate and AML-specific mRNA may elicit superior primary, recall, and effector lytic immune responses compared to autologous dendritic cells loaded with tumor lysate or tumor mRNA alone. Check for active clinical trials using this agent. (NCI Thesaurus)
Ammoidin
(Other name for: methoxsalen)
ammonia N-13
A radiopharmaceutical composed of ammonia labeled with the radioisotope nitrogen N 13 that can be used, during positron emission tomography (PET), as a blood flow imaging agent and potentially as a tumor imaging agent. Upon intravenous administration, ammonia N 13 distributes to various organs in the body, such as the myocardium, liver, kidneys and brain. This agent is taken up by cells and is retained following conversion to glutamine N 13 by glutamine synthetase (GS). Upon PET, organ perfusion and the presence of cancer cells can be assessed. GS, an enzyme that catalyzes the synthesis of glutamine from glutamate and ammonia, is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
ammonium trichlorotellurate
A synthetic non-toxic tellurium derivative, structurally similar to cisplatin, with immunostimulatory and anti-hair loss properties. Ammonium trichlorotellurate induces production of colony stimulating factor (CSF), interleukin-2 (IL-2), and IL-2 receptors by increasing the calcium ion influx through the cell membrane and subsequently exerts its immunostimulatory effects through the CSF-mediated increase in macrophage/granulocytes. This agent is also a potent inducer of interferon and a spectrum of cytokines such as IL-1, IL-6, and tumor necrosis factor (TNF). In animal studies, ammonium trichlorotellurate exerts its anti-hair loss effect by inducing anagen and obstructing spontaneous catagen via promoting follicular keratinocyte proliferation and interfering with terminal differentiation, respectively. Check for active clinical trials using this agent. (NCI Thesaurus)
Amnesteem
(Other name for: isotretinoin)
AmnioFix
(Other name for: dehydrated human amnion/chorion membrane)
amnion-derived cellular cytokine solution
A topical cellular cytokine solution containing a distinct combination of growth factors and cytokines secreted by and released from amnion-derived multipotent progenitor (AMP) cells, with potential immunomodulating and skin healing activities. The amnion-derived cellular cytokine solution (ACCS) contains near physiological levels of transforming growth factor beta, tissue inhibitor of metalloproteinase-1 (TIMP-1) and TIMP-2, as well as the angiogenesis factors platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF) and angiogenin that are normally found in healing wounds. Upon spraying the solution onto affected areas, the cytokines and growth factors in ACCS appear to increase the migration, proliferation and differentiation of both keratinocytes and fibroblasts; enhance the migration and phagocytosis of macrophages in wounds; and increase epithelialization. Together these processes may accelerate skin healing and tissue repair. Also, ACCS may be beneficial in the treatment of radiation burns of the skin. Check for active clinical trials using this agent. (NCI Thesaurus)
Amoban
(Other name for: zopiclone)
amonafide dihydrochloride
The dihydrochloride salt of amonafide, an imide derivative of naphthalic acid. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis. Check for active clinical trials using this agent. (NCI Thesaurus)
amonafide L-malate
The malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis. Check for active clinical trials using this agent. (NCI Thesaurus)
amorphous calcium carbonate
A nutritional supplement composed of a proprietary synthetic and amorphous form of calcium carbonate, that can potentially be used to replenish calcium. Upon administration of amorphous calcium carbonate (ACC), the mineral calcium may give calcium supplementary support, improve bone, muscle and heart strength, improve performance and decrease bone-associated pain. Check for active clinical trials using this agent. (NCI Thesaurus)
amoxicillin
A broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Amoxicillin binds to and inactivates penicillin-binding protein (PBP) 1A located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)
amoxicillin-clavulanate potassium
A combination of the semisynthetic broad-spectrum antibiotic amoxicillin and the beta-lactamase enzyme inhibitor clavulanate potassium. Clavulanate potassium increases the serum half-life of amoxicillin by inhibiting beta-lactamase-mediated metabolism of amoxicillin. Amoxicillin inhibits bacterial cell wall synthesis by binding to penicillin binding proteins and inhibiting peptidoglycan synthesis, a critical component of bacterial cell walls. Check for active clinical trials using this agent. (NCI Thesaurus)
Amoxil
(Other name for: amoxicillin)
amphotericin B deoxycholate
The deoxycholate salt of amphotericin B, a polyene antifungal antibiotic produced by Streptomyces nodosus, with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, resulting in depolarization of the membrane; alterations in cell membrane permeability and leakage of important intracellular components; and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells. Check for active clinical trials using this agent. (NCI Thesaurus)
ampicillin sodium/sulbactam sodium
A combination formulation of the sodium salts of the antibiotic ampicillin and the beta-lactamase inhibitor sulbactam with antibacterial activity. Ampicillin, a broad-spectrum, semisynthetic penicillin, binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall, thereby interfering with the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. As a result, the cell wall is weakened and the cell lyses. The sulbactam component irreversibly binds to bacterial beta-lactamase at or near its active site, thereby interfering with substrate binding and inhibiting bacterial metabolism of penicillin and cephalosporin beta-lactam antibiotics, effectively extending their antibiotic spectrum to include many beta-lactam-resistant bacteria. Check for active clinical trials using this agent. (NCI Thesaurus)
Ampligen
(Other name for: rintatolimod)
Amplimexon
(Other name for: imexon)
amrubicin hydrochloride
The hydrochloride salt of a third-generation synthetic 9-amino-anthracycline with antineoplastic activity. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds. Check for active clinical trials using this agent. (NCI Thesaurus)
Amsa P-D
(Other name for: amsacrine)
amsacrine
An aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
amsilarotene
A retinobenzoic acid with potential antineoplastic activity. Amsilarotene inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression. Check for active clinical trials using this agent. (NCI Thesaurus)
amuvatinib
An orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Amuvatinib binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, amuvatinib inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors. This agent also suppresses the induction of DNA repair protein Rad51, thereby potentiating the activities of DNA damage-inducing agents. Mutant forms of c-Kit are often associated with tumor chemoresistance. Check for active clinical trials using this agent. (NCI Thesaurus)
anagrelide hydrochloride
The hydrochloride salt of a synthetic quinazoline derivative, anagrelide hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. Check for active clinical trials using this agent. (NCI Thesaurus)
anagrelide prolonged-release formulation
A prolonged-release tablet formulation containing the quinazoline anagrelide, with antiplatelet activity. Although the exact mechanism of action through which anagrelide exerts its effect has yet to be fully elucidated, this agent inhibits the maturation of megakaryocytes into platelets, which reduces platelet production. Anagrelide also inhibits cyclic AMP phosphodiesterase III (PDEIII), which prevents PDEIII-mediated platelet aggregation. This may prevent essential thrombocythemia and thrombosis. Check for active clinical trials using this agent. (NCI Thesaurus)
anakinra
A recombinant human nonglycosylated interleukin-1 (IL-1) receptor antagonist with potential antineoplastic activity. Anakinra binds to the IL-1 receptor, thereby blocking the binding of the IL-1 to and activation of its receptor. Blockade of IL-1 activity may inhibit the cascade of downstream pro-angiogenic factors such as vascular endothelial cell growth factor, tumor necrosis factor-alpha, and IL-6, resulting in inhibition of tumor angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
anamorelin hydrochloride
The orally bioavailable hydrochloride salt of a synthetic, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite. Check for active clinical trials using this agent. (NCI Thesaurus)
anastrozole
A nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth. Check for active clinical trials using this agent. (NCI Thesaurus)
anaxirone
A synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis. This agent has been shown to exhibit a broad spectrum of antineoplastic activity against experimental tumors, including those resistant to other alkylating agents. Check for active clinical trials using this agent. (NCI Thesaurus)
Ancef
(Other name for: cefazolin sodium)
ancitabine hydrochloride
The hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine. Check for active clinical trials using this agent. (NCI Thesaurus)
Ancobon
(Other name for: flucytosine)
Andro LA
(Other name for: testosterone enanthate)
AndroGel
(Other name for: testosterone gel)
androgen antagonist APC-100
An orally available, vitamin E derivative and androgen receptor (AR) antagonist with potential anti-oxidant, chemopreventative and antineoplastic activity. APC-100 binds to ARs in target tissues thereby inhibiting androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. By inhibiting the formation of the complex between androgen activated AR- and the AP1 transcription factor JunD, the expression of androgen-responsive genes is blocked. One such gene is spermidine/spermine N1-acetyl transferase gene (SSAT) which is responsible for the breakdown of polyamines, which are produced in high levels by prostatic epithelial cells, into reactive oxygen species (ROS) that cause cellular damage. APC-100 may ultimately lead to an inhibition of growth in both AR-dependent and AR-independent prostate tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor antagonist BAY 1161116
An orally bioavailable antagonist of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR antagonist BAY 1161116 specifically binds to AR, inhibits AR activation, and prevents AR-mediated signaling. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor antagonist ONC1-0013B
An orally bioavailable antagonist of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR antagonist ONC1-13B specifically binds to AR, prevents AR activation, downregulates AR expression and prevents AR-mediated signaling. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor antagonist SHR3680
An orally bioavailable androgen receptor (AR) antagonist with potential antineoplastic activity. Upon administration, SHR3680 competitively binds to AR in target tissues, which both prevents androgen-induced receptor activation and facilitates the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes, inhibits the expression of genes that regulate prostate cancer cell proliferation, and may lead to an inhibition of cell growth of AR-expressing tumor cells. ARs are overexpressed in prostate cancer and play a key role in prostate cancer cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor antagonist TAS3681
An orally bioavailable inhibitor of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR inhibitor TAS3681 specifically binds to AR. This prevents AR activation, downregulates AR and prevents AR-mediated signaling. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor antagonist TRC253
An orally bioavailable androgen receptor (AR) antagonist, with potential antineoplastic activity. Upon oral administration, AR antagonist TRC253 specifically binds to both wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus. This prevents binding to and transcription of AR-responsive genes, inhibits the expression of genes that regulate prostate cancer cell proliferation, and may lead to an inhibition of growth of tumor cells in which AR is overexpressed and/or mutated. AR is often overexpressed and/or mutated in prostate cancers and plays a key role in proliferation, survival and chemoresistance of tumor cells.
androgen receptor antisense oligonucleotide AZD5312
An antisense oligonucleotide targeting the androgen receptor (AR) mRNA, with potential antineoplastic activity. Upon intravenous administration, AZD5312 hybridizes with AR mRNA, which blocks translation of the AR protein. This both inhibits AR-induced tumor cell growth and promotes apoptosis in AR-overexpressing tumor cells. AR is overexpressed in certain breast and prostate cancers and is involved in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor antisense oligonucleotide EZN-4176
A locked nucleic acid (LNA)-based antisense oligonucleotide targeting the androgen receptor (AR) mRNA, with potential antineoplastic activity. Upon administration, EZN-4176 is hybridized and releases the complementary sequences of AR mRNA, thereby blocking translation of the AR protein and inhibiting AR-induced tumor cell growth and promoting tumor cell apoptosis in AR-overexpressing tumor cells. AR is overexpressed in certain breast and prostate cancers and is involved in tumor cell proliferation and survival. LNAs contain a methylene bridge linking 2'-oxygen and 4'-carbon of ribose sugar rings, thereby increasing their thermal stability and decreasing degradation.
androgen receptor degrader ARV-110
An orally available selective androgen receptor (AR)-targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. ARV-110 is composed of an AR ligand attached to an E3 ligase recognition moiety. Upon oral administration, ARV-110 targets and binds to the AR ligand binding domain. E3 ligase is recruited to the AR by the E3 ligase recognition moiety and the AR target protein is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome. This prevents the expression of AR target genes and halts AR-mediated signaling. This results in an inhibition of proliferation in AR-overexpressing tumor cells. In addition, the degradation of the AR protein releases the ARV-110 is released and can bind to additional AR target proteins. AR plays a key role in the proliferation of castration-resistant prostate cancer cells (CRPC). Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor degrader CC-94676
An orally bioavailable androgen receptor (AR) degrader, with potential antineoplastic activity. Upon administration, AR degrader CC-94676 causes degradation of AR, prevents AR-mediated signaling and inhibits the proliferation of AR-overexpressing tumor cells. AR plays a key role in tumor cell proliferation in castration-resistant prostate cancer (CRPC). Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor inhibitor EPI-506
An orally bioavailable, small molecule inhibitor of the N-terminal domain (NTD) of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR inhibitor EPI-506 specifically binds to the NTD of AR, thereby inhibiting both AR activation and the AR-mediated signaling pathway. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor inhibitor EPI-7386
An orally bioavailable, second-generation inhibitor of the N-terminal domain (NTD) of androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR inhibitor EPI-7386 specifically binds to the NTD of AR, thereby inhibiting both AR activation and the AR-mediated signaling pathway. This may inhibit cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in the proliferation, survival and chemoresistance of tumor cells. EPI-7386 may be more active and metabolically stable than first-generation AR NTD inhibitors. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor ligand-binding domain-encoding plasmid DNA vaccine MVI-118
A cancer vaccine containing pTVG4 plasmid DNA encoding the human androgen receptor (AR) ligand-binding domain (LBD) (pTVG-AR), with potential immunostimulating and antineoplastic activities. Upon intradermal administration of AR LBD-encoding plasmid DNA vaccine MVI-118, the plasmid DNA vaccine expresses AR LBD and may stimulate the host immune system to generate a cytotoxic T-lymphocyte (CTL) response against AR LBD-expressing prostate cancer cells. This reduces proliferation of AR-expressing tumor cells. AR, a tumor-associated antigen (TAA) overexpressed in prostate cancer cells, plays a key role in the development and progression of prostate cancer; its expression is correlated with poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
androgen receptor/glucocorticoid receptor antagonist CB-03-10
An orally bioavailable steroidal cortexolone derivative and antagonist of the androgen receptor (AR) and glucocorticoid receptor (GR), with potential antineoplastic activity. Upon oral administration, AR/GR antagonist CB-03-10 specifically binds to AR and GR, inhibits AR and GR activation, and prevents AR- and GR-mediated signaling. This leads to an induction of both extrinsic and intrinsic apoptotic pathways and inhibits cell growth in AR- and GR-overexpressing tumor cells. AR and GR are overexpressed in certain types of cancer cells and are involved in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
Android-F
(Other name for: fluoxymesterone)
androstane steroid HE3235
An orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agent inhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2. Check for active clinical trials using this agent. (NCI Thesaurus)
Anectine
(Other name for: succinylcholine chloride)
anetumab ravtansine
A fully human IgG1 monoclonal antibody directed against the cell surface glycoprotein mesothelin and conjugated to the maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody moiety of anetumab ravtansine targets and binds to the tumor associated antigen mesothelin; upon internalization, the DM4 moiety binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of mesothelin-expressing tumor cells. Mesothelin is overexpressed on all mesotheliomas as well as many ovarian and pancreatic cancers while minimally expressed on normal tissue. Check for active clinical trials using this agent. (NCI Thesaurus)
Aneustat
(Other name for: multifunctional/multitargeted anticancer agent OMN54)
ANF-Rho
(Other name for: pegfilgrastim anti-neutropenic factor)
Ang2/VEGF-binding peptides-antibody fusion protein CVX-241
A fusion protein containing angiopoietin-2 (Ang2) and vascular endothelial growth factor (VEGF) derived peptides covalently attached, via a proprietary diketone linker, to a proprietary humanized catalytic aldolase monoclonal antibody, with potential antiangiogenic and antineoplastic activities. The Ang2/VEGF peptide moieties of Ang2/VEGF-binding peptides-antibody fusion protein CVX-241 bind to Ang2 and VEGF receptors, which may inhibit tumor angiogenesis and tumor cell proliferation. The proprietary humanized catalytic IgG1 monoclonal aldolase antibody contains reactive lysine residues in its binding sites, which react covalently with compounds having a diketone function; the Ang2 and VEGFR peptide moieties are then covalently attached to the diketone linkers via a proprietary spacer. Both VEGF and Ang2 are upregulated in a variety of cancer cell types and play a crucial role in angiogenesis. This agent possesses an enhanced half-life compared to the naked peptides. Check for active clinical trials using this agent. (NCI Thesaurus)
Angelica sinensis root extract
An herbal extract derived from the root of the plant Angelica sinensis with possible antiinflammatory, antispasmodic, vasodilatory, estrogenic, and antitumor activities. Angelica sinensis contains volatile oils, including safrole, isosafrole, and n-butylphthalide; coumarin derivatives, including psoralens, bergapten, osthol, imperatorin, and oxypeucedanin; and ferulic acid. The coumarin derivatives in this agent may vasodilate and relax smooth muscle and may exhibit additive anticoagulant effects. Ferulic acid, a phenolic phytochemical present in plant cell walls, may neutralize free radicals such as reactive oxygen species. In addition, Angelica sinensis extract has been shown to inhibit the growth and induce apoptosis of glioblastoma mutltiforme brain tumor cells through p53-dependent and p53-independent pathways. Check for active clinical trials using this agent. (NCI Thesaurus)
Angiocal
(Other name for: anti-VEGF anticalin PRS-050-PEG40)
Angiocept
(Other name for: pegdinetanib)
angiogenesis inhibitor JI-101
An orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101 binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so, cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. The receptor tyrosine kinases VEGFR2, PDGFRb and EphB4 may be overexpressed in a number of different cancer cell types and may play crucial roles in tumor angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
angiogenesis/heparanase inhibitor PG545
A synthetic heparan sulfate mimetic with potential anti-angiogenic and antineoplastic activity. PG545 inhibits the cleavage of heparan sulfate from cell surface proteoglycan by heparanase and thus inhibits the neovascularization induced by interaction between heparan sulfate and other extracellular matrix proteins. In this manner, this agent may have the potential to slow the progression of growth of solid tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
angiostatin
Encoded by human PLG Gene (Plasminogen Family) and expressed in the kidney, angiostatin is an angiogenesis inhibitor present in plasma and other extracellular fluids that blocks neovascularization and mediates suppression of metastases. Containing at least three kringles, angiostatin is a 38-kD internal (serine protease) proteolytic fragment of plasminogen. Check for active clinical trials using this agent. (NCI Thesaurus)
Angiozyme
(Other name for: anti-FLT-1 ribozyme)
anguidine
A trichothecene mycotoxin and potent teratogen. Anguidine inhibits initiation of protein synthesis, resulting in the death of rapidly proliferating cells. Anguidine also has been shown to both potentiate and protect against the cytotoxic effects of other drugs. Check for active clinical trials using this agent. (NCI Thesaurus)
anhydrous enol-oxaloacetate
The anhydrous form of enol-oxaloacetate, a small molecule blood glutamate scavenger, that can be used to lower glutamate plasma levels, and has potential neuroprotective activity. Upon administration, enol-oxaloacetate targets and binds to glutamate in the bloodstream. This lowers glutamate plasma levels and lowers the free glutamate available to be picked up by cells, such as tumor brain cells, thereby preventing glutamate metabolism and glutamate-mediated signaling. This prevents the proliferation of rapidly growing cells, such as brain tumor cells. And by lowering glutamate plasma levels, a molecular imbalance is formed and glutamate is excreted across the blood-brain barrier, resulting in lower free brain glutamate. This may help protect the brain from excitotoxicity in conditions where there is a surge of glutamate production, such as traumatic brain injury, thereby protecting neuronal cells. Glutamate, a non-essential amino acid and the major excitatory neurotransmitter in the central nervous system (CNS), provides energy and generates building blocks for the production of macromolecules, which are needed for cellular growth and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
anidulafungin
A cyclic lipopeptide echinocandin derivative with antifungal activity. Anidulafungin inhibits 1,3 beta-D-glucan synthase, an enzyme involved in fungal cell wall synthesis, resulting in cell lysis and death. This agent is active against Candida species and Aspergillus. Check for active clinical trials using this agent. (NCI Thesaurus)
aniline mustard
An alkylating mustard with antineoplastic activity. Aniline mustard forms covalent linkages with nucleophilic centers, resulting in depurination, base miscoding and strand scission, and crosslinking of DNA strands, all of which contribute to its cytotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)
anlotinib hydrochloride
The hydrochloride salt form of anlotinib, a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth. Check for active clinical trials using this agent. (NCI Thesaurus)
Annonaceous acetogenins
A family of naturally occurring polyketides that consist of C32 or C34 long chain fatty acids and combined with a propan-2-ol unit at C-2 to form a gamma-lactone, which are isolated from various species of the plant family Annonaceae, with potential antineoplastic and antimicrobial activity. Annonaceous acetogenins bind to the ubiquinone catalytic site(s) within the mitochondrial NADH:ubiquinone oxidoreductase (complex I), and block the electron transport chain in mitochondria. In addition, the acetogenins bind to and block the activity of ubiquinone-linked NADH oxidase, an enzyme overexpressed in the plasma membranes of cancer cells. This inhibits adenosine triphosphate (ATP) production, decreases intracellular ATP levels, and induces tumor cell apoptosis. Compared to normal cells, cancer cells have higher ATP demands. The Annonaceous acetogenins also inhibit microbial glucose dehydrogenase 6. Check for active clinical trials using this agent. (NCI Thesaurus)
Ansaid
(Other name for: flurbiprofen)
Antabuse
(Other name for: disulfiram)
anthocyanin-rich corn extract
A corn-based, water-soluble extract rich in the polyphenol anthocyanin, with potential antioxidant, anti-inflammatory and chemoprotective activities. Upon administration of the anthocyanin-rich corn extract, the anthocyanins scavenge reactive oxygen species (ROS), which protects healthy cells from radiation-induced oxidative stress and DNA damage. In addition, anthocyanins modulate the expression of various genes and proteins involved in inflammation, tumor cell proliferation, angiogenesis, tumor cell invasion and differentiation. This agent also chelates metals and induces the expression of enzymes involved in Phase II antioxidant and detoxification pathways, which may further protect cells against oxidative stress induced by toxins and carcinogens. Check for active clinical trials using this agent. (NCI Thesaurus)
anthracycline analogue GPX-150
A synthetic non-cardiotoxic analogue of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Anthracycline analogue GPX-150 intercalates DNA and impedes the activity of topoisomerase II, inducing single and double-stranded breaks in DNA; inhibiting DNA replication and/or repair, transcription, and protein synthesis; and activating tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti c-KIT antibody-drug conjugate LOP628
An antibody-drug conjugate (ADC) consisting of a humanized monoclonal antibody against the stem cell factor receptor c-Kit (SCFR) and conjugated, via a non-cleavable linker, to the cytotoxic agent maytansine, with potential antineoplastic activity. The monoclonal antibody moiety of anti c-KIT ADC LOP628 targets and binds to the cell surface antigen c-Kit. After antibody-antigen interaction followed by internalization, the maytansine moiety binds to tubulin, inhibits microtubule assembly, and induces microtubule disassembly. This leads to a disruption of mitosis and the inhibition of cell proliferation in cancer cells expressing c-Kit. c-Kit, a transmembrane protein and receptor tyrosine kinase, is overexpressed in solid tumors and hematological malignancies; it plays a key role in the regulation of cell differentiation and proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-5T4 antibody-drug conjugate ASN004
An antibody-drug conjugate (ADC) composed of an antibody directed against 5T4 and conjugated, via a non-cleavable linker, to a proprietary polymer carrying multiple auristatin analog molecules via a cleavable linker, with potential antineoplastic activity. Upon administration, the antibody moiety of ASN004 selectively binds to cells expressing the 5T4 oncofetal antigen. After internalization and cleavage within the tumor cell cytosol, free auristatin analog molecules binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types; its expression is correlated with increased invasiveness. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-5T4 antibody-drug conjugate PF-06263507
An antibody-drug conjugate composed of an antibody directed against 5T4 and conjugated, via the stable linker maleimidocaproyl (mc), to the microtubule inhibitor monomethyl auristatin phenylalanine (MMAF), with potential antineoplastic activity. Upon administration, the antibody moiety of PF-06263507 selectively binds to cells expressing the 5T4 oncofetal antigen. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAF binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types; its expression is correlated with increased invasiveness. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-5T4 antibody-drug conjugate SYD1875
An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the oncofetal antigen 5T4 and site-specifically conjugated to a duocarmycin-based linker-drug valine-citrulline-seco-DUocarmycin-hydroxyBenzamide-Azaindole (vc-seco-DUBA), with potential antineoplastic activity. Upon administration, the antibody moiety of SYD1875 selectively binds to cells expressing the 5T4 oncofetal antigen. After internalization and cleavage within the tumor cell by proteases, the free and activated duocarmycin payload binds to the minor groove of DNA and alkylates adenine at the N3 position, which eventually leads to tumor cell apoptosis. 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types; its expression is correlated with increased invasiveness. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-A33 monoclonal antibody KRN330
A recombinant fully human monoclonal antibody directed against the human A33 antigen, with potential immunomodulatory and antineoplastic activity. Anti-A33 monoclonal antibody KRN330 recognizes and binds to the human A33 antigen, which may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against A33-positive colorectal cancers. A33 antigen, a 43 kDa transmembrane glycoprotein of the immunoglobulin superfamily, is highly and homogenously expressed in 95% of colorectal cancer cancers with only restricted expression in normal colonic mucosa and small bowel epithelia. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-A5B1 integrin monoclonal antibody PF-04605412
A monoclonal antibody directed against the human alpha5beta1 integrin with potential antiangiogenic and antineoplastic activities. Anti-alpha5beta1 integrin monoclonal antibody PF-04605412 selectively binds to alpha5beta1 integrin, preventing the binding of integrin ligands. This may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alpha5beta1-expressing tumor cells. Alpha5beta1 integrin, a cell adhesion and signaling receptor, is often overexpressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-ACTR/4-1BB/CD3zeta-viral vector-transduced autologous T lymphocytes ACTR087
Autologous T lymphocytes that are genetically modified and transfected with a viral vector expressing the ACTR gene, a proprietary gene encoding for an antibody-coupled T cell receptor (ATCR), with potential antineoplastic activity. The ACTR contains the extracellular Fc receptor CD16 domain, normally found on certain immune cells, such as natural killer (NK) cells, coupled to the co-immunostimulatory signaling domain 4-1BB, normally expressed on T cells, and linked to the intracellular CD3 zeta domain (CD3z), which is needed for TCR signaling. Upon reintroduction into the patient and co-administration of a cancer-specific antibody, the co-administered antibody targets and binds to the tumor-associated antigen (TAA) expressed on the tumor cell. In turn, this induces the activation of the ACTR087 cells and destruction of the tumor cells by a) releasing cytotoxins that directly kill cancer cells; b) releasing cytokines that trigger an immune response and recruit other immune-mediated killer cells to kill the tumor cells; b) targeting and killing adjacent tumor cells that are not bound to the antibody; c) inducing T-cell proliferation and thereby further enhancing the T-cell mediated tumor cell attack. CD3 zeta is one of several membrane-bound polypeptides found in the TCR/CD3 complex; it enhances the survival and persistence of T lymphocytes. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of the TAA. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AG7 antibody drug conjugate AbGn-107
An antibody drug conjugate (ADC) composed of a monoclonal antibody that targets the tumor-associated antigen (TAA) AG7 and is linked, through a hydrophilic, self-immolative linker, to a proprietary cytotoxic payload, with potential antineoplastic activity. Upon administration of AbGn-107 the antibody moiety targets and binds to the AG7 antigen expressed on a variety of cancer cells. Upon binding and internalization, the linker is cleaved and the payload is released, binds to tubulin, inhibits tubulin polymerization and kills the AG7-expressing tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AGS-16 monoclonal antibody AGS-16M18
A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-16 with potential antineoplastic activity. Anti-AGS-16 monoclonal antibody AGS-16M18 selectively binds to AGS-16, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) in tumor cells expressing AGS-16. While normally expressed at low levels in the proximal tubules of the kidney, AGS-16 has been found to be overexpressed in more than 95% of kidney and 40% of liver neoplasms. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AGS-5 antibody-drug conjugate ASG-5ME
An antibody drug conjugate (ADC) containing the fully human IgG2k monoclonal antibody targeting an epitope of SLC44A4 (AGS-5) linked, via a valine-citrulline (vc) maleimidocaproyl (mc) linker, to the antimicrotubulin drug monomethyl auristatin E (MMAE), with potential antineoplastic activity. The monoclonal antibody moiety of ASG-5ME selectively binds to AGS-5. After internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis. SLC44A4, potentially a sodium-dependent transmembrane transport protein, is overexpressed on more than 80 percent of samples derived from patients with pancreatic, prostate and gastric cancers. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AGS-8 monoclonal antibody AGS-8M4
A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-8 with potential antineoplastic activity. Anti-AGS-8 monoclonal antibody AGS-8M4 selectively binds to AGS-8, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing AGS-8. While normally expressed at low levels in the heart in response to ischemia, AGS-8 has been found to be expressed in more than 70% of ovarian neoplasms. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-ALK-1 monoclonal antibody PF-03446962
A fully human, IgG2 monoclonal antibody directed against activin-like receptor kinase 1 (ALK-1) with potential antineoplastic activity. Anti-ALK-1 monoclonal antibody PF-03446962 binds to and neutralizes ALK-1. This may disrupt tumor endothelial cell function and inhibit tumor angiogenesis, eventually leading to an inhibition of tumor cell proliferation. ALK-1, a member of the transforming growth factor beta (TGF-b) type I receptor family, is overexpressed on endothelial cells in a variety of tumor cell types and increases endothelial cell proliferation and migration. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-alpha BCMA/anti-alpha CD3 T-cell engaging bispecific antibody TNB-383B
A T-cell engaging bispecific antibody (T-BsAb) directed against the tumor-associated antigen (TAA) human alpha B-cell maturation antigen (aBCMA) and against the alphaCD3 (aCD3) antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. TNB-383B is composed of two aBCMA moieties in sequence on one arm, a single aCD3 arm, and a silenced IgG4 Fc. Upon administration of anti-aBCMA/aCD3 T-cell engaging bispecific antibody TNB-383B, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and BCMA found on BCMA-expressing tumor cells. This activates and redirects CTLs to BCMA-expressing tumor cells, which results in the CTL-mediated cell death 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. Binding to aCD3 preferentially activates effector over regulatory T cells and stimulates minimal cytokine release. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AMHR2 monoclonal antibody GM102
An engineered, humanized, low fucose monoclonal antibody against mullerian hormone receptor II (Müllerian Inhibiting Substance Receptor II; AMHR2; AMHRII), with potential antineoplastic activity. Upon administration, anti-AMHR2 monoclonal antibody GM102 targets, binds to and inhibits AMHR2 and its downstream signaling pathways. GM102 primarily induces antibody dependent cellular cytotoxicity (ADCC) directed against AMHR2-expressing tumor cells through binding to CD16 (Fc-gammaRIIIa) that is present on immune effector cells. Decreased antibody fucosylation increases its affinity for binding to CD16 and ultimately enhances ADCC. AMHR2 is expressed in a subset of gynecological cancers. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-amyloid monoclonal antibody NEOD001
A monoclonal antibody against amyloid with potential use in the treatment of amyloid light chain (AL) and AA amyloidosis. Upon intravenous administration, anti-amyloid monoclonal antibody NEOD001 specifically binds to amyloid fibrils. This prevents the formation of amyloid deposits in certain organs and facilitates their clearance. It also reduces the level of amyloid deposits in organs and prevents organ dysfunction. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-androgen siRNA SXL01
A small-interfering RNA (siRNA) directed against androgen receptor (AR), with potential antineoplastic activity. Upon administration of anti-AR siRNA SXL01, the siRNAs bind to AR mRNAs, which may result in the inhibition of translation of the AR protein. By preventing AR expression, AR-mediated signaling is decreased, which leads to growth inhibition for AR-expressing tumor cells. AR, overexpressed in a variety of cancers, is involved in cellular proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-ANG2 monoclonal antibody MEDI-3617
A fully human IgG1 monoclonal antibody against angiopoietin 2 (ANG2), with potential antiangiogenic activity. Anti-ANG2 monoclonal antibody MEDI-3617 binds to Ang2 and interferes with the interaction between Ang2 and its receptor TEK tyrosine kinase (Tie2), thereby resulting in the disruption of vascular remodeling. This may inhibit angiogenesis and may eventually lead to an inhibition of tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
antiangiogenic drug combination TL-118
A proprietary, oral suspension containing a combination of agents comprised of a nonsteroidal anti-inflammatory agent, an alkylating agent, a histamine H2 antagonist and a sulfonamide with potential anti-angiogenic and antineoplastic activities. Antiangiogenic drug combination TL-118 is administrated as a specific dosing regimen and may result in a synergistic effect and reduce angiogenesis and inhibit tumor cell proliferation.
anti-APRIL monoclonal antibody BION-1301
A humanized monoclonal antibody targeting a proliferation-inducing ligand (APRIL; tumor necrosis factor ligand superfamily member 13; TNFSF13), with potential antineoplastic and immune checkpoint inhibitory activities. Following administration, anti-APRIL monoclonal antibody BION-1301 binds to APRIL and inhibits its binding to both of its receptors, B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17) and transmembrane activator and CAML Interactor (TACI; tumor necrosis factor receptor superfamily member 13B; TNFRSF13B). This inhibits the activation of both BCMA and TACI, and their downstream signaling pathways, which prevents tumor growth, tumor cell adhesion to bone marrow cells and immune suppression. Additionally, BION-1301 may reduce APRIL-induced drug resistance which occurs in some tumors. APRIL, an extracellular protein and member of the tumor necrosis factor ligand superfamily (TNFSF), is expressed by bone marrow plasma cells and myeloid cells, and overexpressed in multiple myeloma (MM), chronic lymphocytic leukemia (CLL), and colorectal carcinoma. APRIL induces immune suppression and tumor progression through the activation of BCMA- and TACI-dependent signaling pathways. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AXL fusion protein AVB-S6-500
A soluble fusion protein comprised of the extracellular domain of the receptor tyrosine kinase (RTK) AXL (UFO) fused to a human immunoglobulin G1 (IgG1) Fc domain, with potential antineoplastic activity. Upon administration, AXL Fc fusion protein AVB-S6-500 selectively binds to growth arrest-specific protein 6 (GAS6), the endogenous ligand for AXL. This may inhibit GAS6/AXL-mediated signaling, which plays a key role in tumor cell proliferation, survival, invasion and metastasis, as well as immune evasion and resistance to other anticancer agents. AXL, a member of the Tyro3, AXL and Mer (TAM) family of RTKs, is overexpressed by many tumor cell types and its expression is associated with drug resistance and poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AXL monoclonal antibody-MMAE conjugate
An antibody-drug conjugate (ADC), consisting of a human monoclonal antibody directed against AXL receptor tyrosine kinase (AXL; UFO) and conjugated, through a protease-cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of HuMax-AXL-ADC binds to AXL, which is expressed on the surfaces of a variety of cancer cell types. Upon endocytosis and enzymatic cleavage, MMAE is released into the tumor cell cytosol, where it binds to tubulin and inhibits tubulin polymerization; this may result in G2/M phase arrest and apoptosis. AXL, a member of the TAM (TYRO3, AXL and MER) family of receptor tyrosine kinases and overexpressed by many tumor cell types, plays a key role in tumor cell proliferation, survival, invasion and metastasis; its expression is associated with drug resistance and poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-AXL/PBD antibody-drug conjugate ADCT-601
An antibody-drug conjugate (ADC), consisting of a humanized immunoglobulin (Ig) G1 monoclonal antibody directed against AXL receptor tyrosine kinase (AXL; UFO) that is site-specifically conjugated to PL1601, which contains a valine-alanine cleavable linker and SG3199, a cytotoxic pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of anti-AXL/PBD antibody-drug conjugate ADCT-60 binds to AXL, which is expressed on the surfaces of a variety of cancer cell types. Upon endocytosis and enzymatic cleavage, free PBD is released and forms highly cytotoxic DNA interstrand cross-links, thereby blocking cell division and killing AXL-expressing cancer cells. AXL, a member of the TAM (TYRO3, AXL and MER) family of receptor tyrosine kinases, is overexpressed by many tumor cell types, and plays a key role in tumor cell proliferation, survival, invasion and metastasis; its expression is associated with drug resistance and poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-B4 blocked ricin immunotoxin
An immunotoxin comprised of an anti-B4 (anti-CD19) murine monoclonal antibody linked to the modified plant-derived toxin blocked ricin. The antibody moiety of anti-B4 blocked ricin immunotoxin binds to B lymphocytes that express B4; after internalization of the immunotoxin by the B4-expressing B cell, the ricin moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in the B lymphocyte 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. "Blocked" ricin is ricin which has been chemically modified such that the lectin binding sites of the B chain (galactose-binding sites) have been blocked by covalent attachment of affinity ligands, leaving the ribosome-inactivating activity of the ricin A chain intact. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-B7-H3 antibody DS-5573a
An antibody directed against the immunoregulatory protein B7-homologue 3 (B7-H3, CD276), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, anti-B7-H3 antibody DS-5573a binds to the cell surface antigen B7-H3, thereby blocking B7-H3-mediated signaling. This abrogates the inhibitory effect on T-cell activation and may activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against B7-H3-expressing tumor 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. It is a negative regulator of the T-cell activation and and its overexpression plays a key role in tumor cell invasion and metastasis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-B7-H3/DXd antibody-drug conjugate DS-7300a
An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against the immunoregulatory protein B7-homologue 3 (B7-H3, CD276) conjugated, via an enzymatically cleavable tetrapeptide-based linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan (DX-8951) derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration of the anti-B7-H3/DXd ADC DS-7300a, the anti-B7-H3 antibody targets and binds to B7-H3-expressing tumor cells. Upon cellular uptake and lysosomal degradation of the linker, DXd targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication and apoptosis. This inhibits the proliferation of B7-H3-expressing tumor 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. It plays a key role in tumor growth and immune responses. The ADC allows for reduced systemic exposure and enhanced delivery of the cytotoxic agent DXd. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-B7-H4 monoclonal antibody FPA150
A fully human, glycoengineered monoclonal antibody targeting B7-H4 (V-set domain-containing T-cell activation inhibitor 1; VTCN1; B7x; B7S1) with potential antineoplastic and immune checkpoint inhibitory activities. Upon intravenous administration, anti-B7-H4 monoclonal antibody FPA150 binds to B7-H4 on the surface of tumor cells, thereby preventing B7-H4 binding to T cells and abrogating the B7-H4-mediated negative regulation of T-cell activation. This increases a cytotoxic T-lymphocyte (CTL)-mediated immune response against B7-H4-expressing tumor cells. In addition, the afucosylated Fc region of the anti-B7-H4 monoclonal antibody FPA150 enhances its binding affinity for human FcgammaRIIIa receptors (CD16) on natural killer (NK) cells, resulting in enhanced antibody-dependent cellular cytotoxicity (ADCC) against B7-H4-expressing tumor cells. B7-H4, a member of the B7 family of immune modulators, is upregulated in a variety of tumor cell types and negatively regulates T-cell immune responses. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-B7-H4 monoclonal antibody FPA150
A fully human, glycoengineered monoclonal antibody targeting B7-H4 (V-set domain-containing T-cell activation inhibitor 1; VTCN1; B7x; B7S1) with potential antineoplastic and immune checkpoint inhibitory activities. Upon intravenous administration, anti-B7-H4 monoclonal antibody FPA150 binds to B7-H4 on the surface of tumor cells, thereby preventing B7-H4 binding to T cells and abrogating the B7-H4-mediated negative regulation of T-cell activation. This increases a cytotoxic T-lymphocyte (CTL)-mediated immune response against B7-H4-expressing tumor cells. In addition, the afucosylated Fc region of the anti-B7-H4 monoclonal antibody FPA150 enhances its binding affinity for human FcgammaRIIIa receptors (CD16) on natural killer (NK) cells, resulting in enhanced antibody-dependent cellular cytotoxicity (ADCC) against B7-H4-expressing tumor cells. B7-H4, a member of the B7 family of immune modulators, is upregulated in a variety of tumor cell types and negatively regulates T-cell immune responses. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA antibody SEA-BCMA
A humanized, afucosylated monoclonal antibody created using the proprietary, sugar-engineered antibody (SEA) platform and directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; TNFRSF17), with potential immunoadjuvant activity. Upon administration, the anti-BCMA antibody SEA-BCMA targets and binds to BCMA expressed on tumor cells. When administered with antibody-coupled T-cell receptor (ACTR)-expressing T cells, the ACTR-expressing T cells bind, with high affinity, to the anti-BCMA antibody SEA-BCMA. This activates the ACTR T-cells and the T cells induce specific cytotoxic T-lymphocyte (CTL)-mediated cytotoxicity toward BCMA-expressing tumor cells. BCMA, a cell surface protein and member of the tumor necrosis factor (TNF) receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA SparX protein plus BCMA-directed anti-TAAG ARC T cells CART-ddBCMA
An immunotherapeutic combination agent composed of antigen receptor complex T cells (ARC-T cells) which contain a proprietary binding domain specific for a universal TAG instead of a single chain variable fragment (scFv) binding domain, and a tumor-targeting antigen protein, soluble protein antigen-receptor X-linker (sparX) protein, containing a TAG moiety fused to two B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17) binding domains, with potential antineoplastic activities. Upon administration of the anti-BCMA sparX protein plus BCMA-directed ARC T-cells CART-ddBCMA, the sparX protein, with its two BCMA binding domains, specifically targets and binds to two BCMA expressed on tumor cells. In turn, the ARC-T cells, with their anti-TAG domain, target and bind to the TAG domain on the sparX protein. This directly links the ARC-T cells to the BCMA-expressing tumor cells, through the ARC-T cell- sparX -tumor cell complex formation, thereby causing direct tumor cell killing. BCMA, a tumor-associated antigen (TAA), is found on the surfaces of plasma cells and is overexpressed on a variety of tumor cell types. Compared to anti-BCMA CAR-T cells, CART-ddBCMA, containing ARC-T cells that are re-programmed in vivo by the TAG sparX protein, shows enhanced efficiency and an improved safety profile. As ARC-T activity is dependent on the sparX dose administered, the rate of tumor cell killing, and related toxicities are also dependent on the sparX dose administered. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA/anti-CD3 bispecific antibody REGN5459
A human bispecific antibody directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17) and another directed against the T-cell surface antigen CD3, with potential immunostimulating and antineoplastic activities. Upon administration, anti-BCMA/anti-CD3 bispecific antibody REGN5459 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. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA/CD3 BiTE antibody AMG 420
A short half-life bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; TNFRSF17), fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-BCMA/CD3 BiTE antibody AMG 420, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and BCMA found on BCMA-expressing tumor cells. This activates and redirects CTLs to BCMA-expressing tumor cells, which results in the CTL-mediated cell death 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. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA/CD3 BiTE antibody AMG 701
A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; TNFRSF17), fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-BCMA/CD3 BiTE antibody AMG 701, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and BCMA found on BCMA-expressing tumor cells. This activates and redirects CTLs to BCMA-expressing tumor cells, which results in the CTL-mediated cell death 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. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA/CD3 BiTE antibody REGN5458
A human bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFvs): one directed again the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17) and another directed against the CD3 antigen expressed on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration, anti-BCMA/anti-CD3 BiTE REGN5458 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. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BCMA/PBD ADC MEDI2228
An antibody-drug conjugate (ADC) consisting of a fully human monoclonal antibody against the tumor-associated antigen (TAA) B-cell maturation antigen (BCMA, TNFRSF17) that is site-specifically conjugated, via a protease-cleavable linker, to a cytotoxic, DNA minor groove crosslinking agent and pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of anti-BCMA/PBD ADC MEDI2228, the antibody moiety targets the cell surface antigen BCMA expressed on certain cancer cells. Upon antibody/antigen binding, internalization and lysosome-mediated cleavage, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of BCMA-overexpressing tumor cells. BCMA, a receptor for a proliferation-inducing ligand (APRIL; tumor necrosis factor ligand superfamily member 13; TNFSF13), and B-cell activating factor (BAFF), is a member of the tumor necrosis factor (TNF) receptor superfamily and plays a key role in plasma survival; it is found on the surfaces of plasma cells and is overexpressed on malignant plasma cells. Check for active clinical trials using this agent. (NCI Thesaurus)
antibiotic SQ109
An orally available, acid-stable diamine antibiotic, with potential antimicrobial activity against a variety of bacteria including Helicobacter pylori (H. pylori) and Mycobacterium tuberculosis (M. tuberculosis). As an ethambutol analogue with asymmetric structure, SQ109 does not act on the same target as ethambutol. However, this agent interferes with cell wall synthesis, thereby causing weakening of the cell wall and ultimately cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate ABBV-011
An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against an as of yet undisclosed tumor-associated antigen (TAA) linked to an undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-011 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills tumor cells expressing this particular TAA through an as of yet undisclosed mechanism. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate ABBV-085
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-085 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action.
antibody-drug conjugate ABBV-155
An antibody-drug conjugate (ADC) composed of an as of yet undisclosed monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-155 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate ABBV-176
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against the prolactin receptor (PRLR) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-176 targets and binds to PRLR expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the PRLR-expressing tumor cells, through an as of yet unknown mechanism of action. PRLR, a tumor-associated antigen (TAA), is overexpressed by a variety of tumor cell types. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate ADC XMT-1536
A proprietary antibody-drug conjugate (ADC) composed of XMT-1535, a proprietary, humanized monoclonal antibody against human sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi2b), site-specifically linked, via a protease cleavable linker, to the proprietary cytotoxic aurastatin derivative auristatin F-HPA (AF-HPA; auristatin F-hydroxypropylamide), with potential antineoplastic activity. XMT-1536 is produced via the proprietary dolaflexin ADC conjugation platform, which promotes the conjugation of between 10 and 15 AF-HPA payload molecules to each XMT-1535 antibody. Upon administration of XMT-1536, the antibody moiety targets and binds to NaPi2b expressed on tumor cells. Upon binding, internalization by endosomes/lysosomes, and enzymatic cleavage, the AF-HPA binds to tubulin and inhibits microtubule polymerization, which results in G2/M phase arrest and apoptosis of NaPi2b-expressing tumor cells. NaPi2b, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells and plays a key role in the transport of inorganic phosphate (Pi) and the maintenance of phosphate homeostasis. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate anti-TIM-1-vcMMAE CDX-014
A human immunoglobulin G1 (IgG1) monoclonal antibody-drug conjugate (ADC) targeting the extracellular domain of T-cell immunoglobulin mucin-1 (TIM-1) (clone CR014) and linked, via a valine-citrulline (vc) peptide linker, to the potent cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of ADC Anti-TIM-1-vcMMAE CDX-014, the monoclonal antibody moiety targets and binds to TIM-1. Upon internalization and proteolytic cleavage, MMAE is released into the cytosol of TIM-1-expressing tumor cells, binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. TIM-1 is upregulated in a variety of cancer cell types while only minimally expressed in healthy tissue. The linkage system in CDX-014 is highly stable in plasma, resulting in cytotoxic specificity for TIM-1-positive cells. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate BAY79-4620
A monoclonal antibody (MoAb) directed against the MN protein with potential antineoplastic activity. Upon administration of BAY79-4620, this MoAb may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response and an antibody mediated cellular cytotoxicity (ADCC) against MN-expressing tumor cells. MN, a transmembrane glycoprotein, is expressed in some human carcinomas and appears to be involved in cancer cell proliferation and transformation. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate DFRF4539A
An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against a specific myeloma antigen and conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DFRF4539A selectively binds to a specific protein expressed on the surface of myeloma cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate MEDI7247
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against an unnamed tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of MEDI7247 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate SC-002
An antibody-drug conjugate (ADC) composed of an as of yet publicly unknown monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-002 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate SC-003
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-003 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate SC-004
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to a currently undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-004 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate SC-005
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to a currently undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-005 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate SC-006
An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-006 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-drug conjugate SC-007
An antibody-drug conjugate (ADC) composed of a monoclonal antibody against an undisclosed tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of SC-007 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)
antibody-like CD95 receptor/Fc-fusion protein CAN-008
A human, soluble fusion protein consisting of the extracellular domain of the CD95 receptor fused to the Fc-domain of the human IgG antibody, with potential antineoplastic activity. Upon administration, antibody-like CD95 receptor/Fc-fusion protein CAN-008 binds to the CD95 ligand (CD95L) and blocks the binding of CD95L to the CD95 receptor. In tumor cells, blockage of CD95L-mediated signaling pathways may prevent cell migration and invasive cell growth; in healthy cells, blockage of CD95L-mediated signaling pathways may prevent apoptosis and may protect cell damage. Activation of the CD95 receptor plays an important role in the initiation of apoptosis in healthy cells or the invasive growth of cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BTLA monoclonal antibody TAB004
A recombinant humanized immunoglobulin G4 kappa (IgG4k) monoclonal antibody directed against B- and T-lymphocyte attenuator (BTLA), with potential immunomodulating and antineoplastic activities. Upon intravenous infusion administration, anti-BTLA monoclonal antibody TAB004 targets and binds to BTLA. This prevents BTLA-mediated inhibition of T-cell activation leading to antigen specific T-cell proliferation and activation of a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. BTLA, an immunoglobulin (Ig) receptor family member expressed on activated T and B lymphocytes, subsets of dendritic cells (DCs), macrophages, and nature killer (NK) cells, is an immune checkpoint involved in suppressing immune responses. It mediates inhibition of human tumor-specific CTLs upon engagement by tumor expressed herpesvirus-entry mediator (HVEM). Check for active clinical trials using this agent. (NCI Thesaurus)
anti-BTN3A agonistic monoclonal antibody ICT01
A humanized agonistic monoclonal antibody directed against butyrophilin subfamily 3 member A (BTN3A; CD277), with potential immunomodulating and antineoplastic activities. Upon administration, the anti-BTN3A agonistic monoclonal antibody ICT01 targets and binds to BTN3A present on epithelial and tumor cells. BTN3A binding may sensitize tumor cells to gamma 9 delta 2 (Vg9Vd2) T-cell killing. The Vg9Vd2 T cells secrete effector cytokines and exert a cytolytic effect on tumor cells. This may abrogate BTN3A-mediated tumor immunity and may enhance anti-tumor immune response. BTN3A, a member of the butyrophilin superfamily of immunomodulators, is upregulated in tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-C4.4a antibody-drug conjugate BAY1129980
An antibody-drug conjugate (ADC) composed of an antibody against a structural homolog of the urokinase-type plasminogen activator receptor (uPAR) and tumor-associated antigen, C4.4a, and conjugated with a cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, anti-C4.4a antibody-drug conjugate BAY1129980 targets and binds to C4.4a-expressing tumor cells. Upon binding and cell entry, the cytotoxic agent kills the tumor cell. C4.4a, a glycolipid-anchored membrane protein and a member of the Ly-6 family, is overexpressed by a variety of cancer cell types whereas it is minimally expressed on healthy cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-C5aR monoclonal antibody IPH5401
A human monoclonal antibody targeting the C5a receptor (C5aR), with potential immunomodulating activity. Upon administration, the anti-C5aR monoclonal antibody IPH5401 specifically targets, binds to and blocks C5aR expressed on subsets of myeloid-derived suppressor cells (MDSCs) and neutrophils. This prevents the binding of its ligand C5a to C5aR and prevents the C5aR-mediated activation and accumulation of these cells in the tumor microenvironment (TME), and abrogates the secretion of inflammatory and angiogenic factors by these cells. This results in the activation of T cells and natural killer (NK) cells, the induction of anti-tumor immune responses and inhibits tumor cell proliferation. C5a, a factor in the complement cascade, is often overexpressed in tumors, where it attracts and activates MDSCs and neutrophils in the TME. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CA19-9 monoclonal antibody 5B1
A human monoclonal antibody against the carbohydrate antigen sialyl-Lewis A (carbohydrate antigen 19-9; CA19-9), with potential antineoplastic activity. Upon administration, monoclonal antibody 5B1 binds to CA19-9 and kills CA19-9-expressing tumor cells, possibly through the induction of both complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). CA19-9 is overexpressed on a number of different tumor cell types, and plays a key role in tumor cell survival and metastasis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CA6-DM4 immunoconjugate SAR566658
An immunoconjugate consisting of a humanized monoclonal antibody against the tumor-associated sialoglycotope CA6 (huDS6) conjugated to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. The anti-CA6 monoclonal antibody moiety of SAR566658 targets and binds to the cell surface antigen CA6. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CA6-expressing tumor cells. The CA6 epitope is found on a variety of solid tumors, including breast, ovarian, cervical, lung and pancreatic tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
anticachexia agent MT-102
A small molecule with potential anticachexia activity. The anticachexia agent MT-102 may increase protein synthesis and decrease muscle protein breakdown. This may result in improved body weight, muscle mass and may improve weakness and fatigue associated with cancer-related cachexia. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CCR7 antibody-drug conjugate JBH492
An antibody-drug conjugate (ADC) composed of an antibody targeting CC chemokine receptor 7 (CCR7) and conjugated to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. Upon administration of anti-CCR7 ADC JBH492, the antibody moiety targets and binds to CCR7 on tumor cells. Upon antibody/antigen binding and internalization, the ADC releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics. This results in the inhibition of cell division and cell growth of CCR7-expressing tumor cells. CCR7, a G-protein coupled receptor, is normally expressed by subsets of immune cells and overexpressed by various types of cancer cells. Its overexpression has been associated with lymph node metastasis and poor survival. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD117 monoclonal antibody JSP191
A humanized monoclonal antibody directed against CD117 (tyrosine-protein kinase KIT; c-Kit; mast/stem cell growth factor receptor; SCFR), that can potentially be used to deplete hematopoietic stem cells (HSCs). Upon administration, the anti-CD117 monoclonal antibody JSP191 targets and binds to CD117. This prevents the binding of stem cell factor (SCF) to its receptor CD117 on HSCs. As CD117 binding to SCF is critical for survival and maintenance of blood forming stem cells, blocking this interaction causes the HSCs that are present in the bone marrow niches to be depleted. JSP191 can potentially be used as a conditioning regimen to prepare patients for hematopoietic stem cell transplantation. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123 ADC IMGN632
An antibody-drug conjugate (ADC) consisting of a humanized anti-CD123 (interleukin-3 (IL-3) receptor alpha chain; IL3RA) immunoglobulin G1 (IgG1) monoclonal antibody conjugated, via a cleavable linker, to a cytotoxic, DNA-alkylating payload, which is an indolino-benzodiazepine dimer containing an imine moiety, with potential antineoplastic activity. Upon administration of anti-CD123 ADC IMGN632, the antibody moiety targets the cell surface antigen CD123. Upon antibody/antigen binding, internalization, and lysosome uptake, the cytotoxic moiety is released, and covalently binds to and alkylates DNA with its imine moiety. This results in cell cycle arrest in S-phase, which leads to apoptosis and inhibition of cell growth in cells overexpressing CD123. CD123, the alpha subunit of the IL-3 receptor, regulates the proliferation, survival and differentiation of hematopoietic cells. CD123 is overexpressed on a variety of cancers. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123 monoclonal antibody KHK2823
A fully human monoclonal antibody against CD123 (interleukin-3 receptor alpha chain) with potential antineoplastic activity. Anti-CD123 monoclonal antibody KHK2823 binds to and neutralizes CD123, which is upregulated on leukemic stem cells (LSC) found in myelodysplastic syndrome (MDS) or acute myeloid leukemia (AML). This agent may inhibit IL-3-dependent signaling and proliferation and may prevent the uncontrolled growth and differentiation of mutated LSC. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123 x anti-CD3 bispecific antibody XmAb14045
An anti-CD123/anti-CD3 bispecific monoclonal antibody, in which most of the naturally-occurring Fc domain is maintained, with potential immunostimulatory and antineoplastic activities. Anti-CD123/CD3 monoclonal antibody XmAb14045 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD123, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of XmAb14045, this bispecific antibody simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of hematological malignancies; its expression is low or absent in normal hematopoietic progenitors and stem cells. The Fc domain on the antibody prolongs the half-life of the bispecific antibody and enhances T-cell-mediated tumor cell killing through its binding to the Fc receptors. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123/CD3 bispecific antibody APVO436
An immunoglobulin Fc-modified bispecific monoclonal antibody against the tumor-associated antigen (TAA) CD123 and the human T-cell surface antigen CD3 bispecific monoclonal antibody, with potential immunostimulatory and antineoplastic activities. Upon administration, anti-CD123/CD3 monoclonal antibody APVO436 simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This results in the activation and proliferation of T-cells and causes CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of hematological malignancies; its expression is low or absent in normal hematopoietic progenitors and stem cells. The Fc domain on the antibody prolongs the half-life of the bispecific antibody. Compared to some other CD123 x CD3 targeting bispecific antibodies, APVO436 causes less cytokine release upon T-cell stimulation. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123/CD3 bispecific antibody JNJ-63709178
A humanized anti-CD123/anti-CD3 bispecific monoclonal antibody, with potential immunostimulating and antineoplastic activities. Anti-CD123/CD3 bispecific antibody JNJ-63709178 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD123, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of JNJ-63709178, this bispecific antibody simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of cancers; its expression is low or absent in normal, healthy cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123/CD3 BiTE antibody SAR440234
A bispecific T-cell engager (BiTE) antibody comprised of a humanized Fc-silenced immunoglobulin G1 (IgG1) backbone and two single-chain variable fragments (scFvs): one directed against the CD3 antigen expressed on T lymphocytes and another directed against the alpha-chain of the interleukin-3 receptor (IL-3RA; CD123), with potential immunostimulating and antineoplastic activities. Upon intravenous infusion, anti-CD123/CD3 BiTE antibody SAR440234 binds to both CD3 expressed on T cells and CD123 expressed on tumor cells. This activates and redirects cytotoxic T lymphocytes (CTLs) to CD123-expressing tumor cells, leading to enhanced CTL-mediated elimination of CD123-expressing tumor cells. CD123 is overexpressed in a variety of hematological malignancies; its expression is low or absent in normal hematopoietic progenitors and stem cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD123-pyrrolobenzodiazepine dimer antibody drug conjugate SGN-CD123A
An antibody-drug conjugate (ADC) consisting of an anti-CD123 humanized monoclonal antibody conjugated, via a stable maleimidocaproyl-valine-alanine dipeptide protease-cleavable linker, to the cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of anti-CD123 ADC SGN-CD123A, the antibody moiety targets the cell surface antigen CD123. Upon antibody/antigen binding, internalization, and lysosome uptake, the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of CD123-overexpressing tumor cells. CD123, the alpha subunit of the IL-3 receptor, regulates the proliferation, survival and differentiation of hematopoietic cells. CD123 is overexpressed on a variety of cancers, including myeloid leukemia, and increased expression of CD123 on leukemic stem cells is associated with poor prognosis. Cysteine engineering of the monoclonal antibody (EC-mAb) allows for a site-specific, stable conjugation and uniform loading of the PBD agent to the antibody. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD133-CAR vector-transduced allogeneic T lymphocytes
A preparation of allogeneic peripheral blood T lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) specific for the chimeric CD (cluster of differentiation) 133 antigen receptor, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD133-CAR vector-transduced allogeneic T lymphocytes specifically recognize and kill CD133-expressing tumor cells. CD133, a tumor associated antigen (TAA), is overexpressed on a variety of tumor cell types. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD133-PE38-KDEL fusion protein
A fusion protein consisting of an anti-single-chain variable fragment (scFv) peptide sequence targeting the extracellular domain of human CD133 (prominin-1) (anti-CD133scFV) and a deimmunized truncated form of Pseudomonas exotoxin A (38-kDa derivative of PE; PE38) where the five C-terminal amino acid residues have been replaced with the endoplasmic reticulum (ER) retention signal, KDEL, with potential antineoplastic activity. Upon administration of the anti-CD133-PE38-KDEL fusion protein, the anti-CD133 scFV moiety targets and binds to CD133, which is expressed on a variety of tumor cells. Upon internalization of the receptor-fusion protein complex, the KDEL sequence targets the fusion protein to the ER, where the PE38 exotoxin portion then inhibits protein synthesis, which results in a reduction of proliferation of CD133-expressing tumor cells. CD133, a glycoprotein expressed by a variety of cancers and especially by cancer stem cells (CSCs), plays a key role in tumor initiation, proliferation and progression. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD137 agonistic monoclonal antibody ADG106
A human agonistic monoclonal antibody targeting CD137 (4-1BB; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunostimulating activity. Upon administration, anti-CD137 agonistic monoclonal antibody ADG106 binds to and activates CD137 expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer (NK) cells. This enhances CD137-mediated signaling, induces cytokine production and promotes T-cell mediated anti-tumor immune responses. CD137, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD137 agonistic monoclonal antibody AGEN2373
A conditionally-active, fully human immunoglobulin G1 (IgG1) agonistic monoclonal antibody targeting the costimulatory receptor CD137 (4-1BB; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD137 agonistic monoclonal antibody AGEN2373 targets and binds to a non-ligand blocking epitope on CD137, thereby activating CD137 expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer (NK) cells. This enhances CD137-mediated signaling, induces cytotoxic T-lymphocyte (CTL) proliferation, cytokine production and promotes a CTL-mediated anti-tumor immune response as well as induces NK-mediated tumor cell killing and suppresses the immunosuppressive activity of T-regulatory cells (Tregs). CD137, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. In addition, as AGEN2373 engages with CD137 only in the presence of CD137 ligand and/or Fc gamma receptor-expressing antigen-presenting cells (APCs), this agent may have a decreased toxicity profile and improved tolerability compared to other agents that activate CD137 signaling beyond the tumor site in humans. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD137 agonistic monoclonal antibody ATOR-1017
A humanized agonistic immunoglobulin G4 (IgG4) monoclonal antibody targeting the costimulatory receptor CD137 (4-1BB; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD137 agonistic monoclonal antibody ATOR-1017 targets and binds to CD137 expressed on a variety of leukocyte subsets including activated T-lymphocytes and natural killer (NK) cells, and CD137 is activated upon crosslinking to Fc-gamma receptors (FcgRs) on macrophages. This enhances CD137-mediated signaling, induces cytotoxic T-lymphocyte (CTL) proliferation, cytokine production and promotes a CTL-mediated anti-tumor immune response as well as induces NK-mediated tumor cell killing and suppresses the immunosuppressive activity of T-regulatory cells (Tregs). CD137, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. 4-1BB and FcgRs are both highly expressed in the tumor environment (TME) while their co-expression in non-tumor tissues is low. This may prevent systemic adverse effects. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD137 agonistic monoclonal antibody CTX-471
A fully human immunoglobulin G4 (IgG4) agonistic monoclonal antibody targeting CD137 (4-1BB; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD137 agonistic monoclonal antibody CTX-471 binds to and activates CD137 expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer (NK) cells. This enhances CD137-mediated signaling, induces cytokine production and promotes T-cell mediated anti-tumor immune responses. CD137, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD137 agonistic monoclonal antibody LVGN6051
A humanized agonistic monoclonal antibody targeting the costimulatory receptor CD137 (4-1BB; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD137 agonistic monoclonal antibody LVGN6051 targets and binds to CD137, thereby activating CD137 expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer (NK) cells. This enhances CD137-mediated signaling, induces cytotoxic T-lymphocyte (CTL) proliferation, cytokine production and promotes a CTL-mediated anti-tumor immune response as well as induces NK-mediated tumor cell killing and suppresses the immunosuppressive activity of T-regulatory cells (Tregs). CD137, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD157 monoclonal antibody MEN1112
A humanized, Fc-engineered, de-fucosylated monoclonal immunoglobulin G1 (IgG1) antibody directed against the bone marrow stromal cell antigen 1 (BST1/CD157), with potential antineoplastic activity. Upon intravenous infusion, anti-CD157 monoclonal antibody MEN1112 specifically binds to and induces an antibody-dependent cell cytotoxic (ADCC) response against CD157-expressing tumor cells. CD157, also known as ADP-ribosyl cyclase 2, is a glycosyl-phosphatidylinositol (GPI)-anchored transmembrane protein belonging to the ADP-ribosyl-cyclase family and is overexpressed on certain cancer cell types. Fc-optimization of MEN1112, which involves the removal of fucose residues from its Fc domain, allows for enhanced Fc-gamma receptor binding on effector cells, such as natural killer (NK) cells, and further enhances tumor cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD166 probody-drug conjugate CX-2009
A probody drug conjugate (PDC) composed of a recombinant antibody targeting the tumor-associated antigen (TAA) CD166, which is masked by a cleavable masking peptide, and conjugated to the cytotoxic agent maytansinoid DM4, with potential antineoplastic activity. Upon administration of CX-2009 and migration to the tumor microenvironment (TME), the cleavable masking peptide, which prevent anti-CD166 antibody binding to the CD166 expressed on both normal cells and tumor cells, is proteolytically cleaved by tumor-associated proteases that are specifically present in the TME. This enables the anti-CD166 antibody moiety of CX-2009 to selectively bind to, be internalized by, and deliver DM4 into CD166-expressing tumor cells. Following internalization, DM4 is released, binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CD166-expressing tumor cells. The masking peptide prevents binding of the anti-CD166 antibody to CD166 in normal tissues, thereby minimizing toxicities. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19 antibody-T-cell receptor-expressing T cells ET019003
A preparation of T lymphocytes that have been engineered by incorporating an as of yet undisclosed co-stimulatory molecule into T cells expressing an anti-CD19 antibody T-cell receptor (AbTCR) structure (ET190L1), with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19 AbTCR-expressing T cells ET019003 targets and binds to CD19-expressing tumor cells. This results in cytotoxic T-lymphocyte (CTL)-mediated elimination of CD19-positive tumor cells. The binding to CD19-expressing tumor cells may also activate the undisclosed costimulatory domain, leading to further T-cell proliferation. CD19 antigen is a B-cell specific cell surface antigen overexpressed in B-cell lineage malignancies. ET019003 is able to match the anticancer activity of chimeric antigen receptor (CAR) T cells, while they are less likely to stimulate cytokine release syndrome (CRS) and less likely to cause cytokine-related toxicities. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19 CAR-T cells XLCART001
A preparation of T lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) targeting the tumor-associated antigen (TAA) CD19 and containing, as of yet undisclosed co-stimulatory signaling domains, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19 CAR-T cells XLCART001 targets and binds to CD19-expressing tumor cells, thereby inducing selective toxicity in CD19-expressing tumor cells. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19 fully human monoclonal antibody MDX-1342
A fully human anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential antineoplastic activity. Anti-CD19 monoclonal antibody MDX-1342 binds to CD19, depleting and eliminating CD19-expressing B-cells. CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19 monoclonal antibody DI-B4
A low-fucosylated, humanized, IgG1 isotype, monoclonal antibody directed against the B-cell-specific membrane protein CD19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody DI-B4 binds to CD19, which may result in a strong antibody-dependent cellular cytotoxicity (ADCC) directed at CD19-expressing B-cells but with minimal complement dependent cytotoxicity. DI-B4 contains low levels of fucose, which contributes to its enhanced ADCC activity. CD19 is a B-cell specific membrane antigen that is widely expressed during B-cell development and in all B-cell lineage malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19/CD20/CD22/CD30 CAR-T cells
A preparation of human T lymphocytes engineered to express a chimeric antigen receptor (CAR) specific for the tumor-associated antigens (TAAs) cluster of differentiation 19 (CD19), CD20, CD22 and CD30, with potential immunostimulating and antineoplastic activities. Upon administration, the anti-CD19/CD20/CD22/CD30 CAR-T cells target and bind to CD19, CD20, CD22 and CD30 expressed on the surface of certain tumor cells. This induces selective toxicity in tumor cells expressing these TAAs. The TAAs are overexpressed in certain hematologic malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19/CD22 bispecific ligand-directed toxin DT2219ARL
An immunotoxin consisting of two scFv ligands recognizing human CD19 and CD22 linked to the first 389 amino acids of diphtheria toxin (DT), DT 390, with potential antineoplastic activity. The VH and VL regions of anti-CD22 (sFv) and anti-CD19 are reversed and linked by an aggregration stabilizing linker (ARL) consisting of a 20 amino acid segment of human muscle aldolase (hma) and an Xho1 -compatible restriction site; the CDR3 region of the VH of anti-CD22 sFv is mutated to enhance its affinity. The anti-CD19 and anti CD-22 portions of the immunotoxin specifically bind to CD19 and CD22 receptors on tumor B cells. Upon internalization, DT catalyzes ADP ribosylation of elongation factor 2 (EF-2) which may result in the irreversible inhibition of protein synthesis and cell death in CD19- and CD22-expressing tumor cells. CD19 and CD22 transmembrane proteins upregulated on malignant B cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19/CD3 BiTE antibody AMG 562
A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the B-cell-specific membrane protein CD19, and another that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19/CD3 BiTE antibody AMG 562 binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and the CD19 antigen expressed on malignant B cells. This activates and redirects CTLs to CD19-expressing tumor cells, resulting in CTL-mediated killing of tumor cells. CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19/CD3 tetravalent antibody AFM11
An anti-CD19/anti-CD3 bispecific tetravalent antibody with potential immunostimulatory and antineoplastic activities. Anti-CD19/CD3 tetravalent antibody AFM11 possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD19, a tumor-associated antigen (TAA) overexpressed on the surface of B-cells. Upon bolus infusion of AFM11, this bispecific antibody binds to CD3-expressing T-cells and CD19-expressing cancer cells, thereby crosslinking CD19-expressing tumor B-cells and cytotoxic T-lymphocytes (CTLs). This may result in a potent CTL-mediated cell lysis of CD19-expressing B-lymphocytes. CD19, a B-cell specific membrane antigen, is expressed during both B-cell development and B-cell malignant growth. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-CAR FMC63-28Z retroviral vector-transduced allogeneic T lymphocytes
Allogeneic T-lymphocytes derived from peripheral blood mononuclear cells (PBMC) transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) consisting of both the light and heavy chain variable regions of anti-CD19 monoclonal antibody FMC63, coupled to the molecule CD28 and the signaling domain of the zeta chain of the T-cell receptor (TCR) (FMC63-28Z), with potential immunomodulating and antineoplastic activities. Upon transfusion, the anti-CD19-CAR FMC63-28Z retroviral vector-transduced allogeneic T lymphocytes specifically recognize and kill CD19-expressing tumor cells. CD19 antigen is a B-cell specific cell surface antigen, which is expressed in all B-cell lineage malignancies and normal B-cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-CAR retroviral vector-transduced autologous T cells
A preparation of autologous peripheral blood T-lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment); an extracellular portion of human CD28 and the entire transmembrane and cytoplasmic portion of human CD28; and the cytoplasmic portion of the human TCR-[zeta] molecule with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19-CAR retroviral vector-transduced autologous T cells may stimulate host cytotoxic T lymphocyte (CTL) and antibody responses against CD19-expressing tumor cells, resulting in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. CD28 is essential for CD4+ T-cell proliferation, interleukin-2 production, and T-helper type-2 (Th2) development. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-CAR-CD28/CD20-CAR-4-1BB-expressing autologous T lymphocytes Hu1928-Hu20BB
A preparation of autologous human T lymphocytes that have been genetically modified to express the CAR construct Hu1928-Hu20BB that consists of two chimeric antigen receptor (CAR) constructs: one encoding a fully-human anti-CD19 CAR with a co-stimulatory domain of CD28, Hu19-CD828, and one encoding a human anti-CD20 CAR with a co-stimulatory domain of 4-1BB (CD137), Hu20BB, with potential immunostimulating and antineoplastic activities. Upon re-infusion, the anti-CD19-CAR-CD28/CD20-CAR-4-1BB-expressing autologous T lymphocytes Hu1928-Hu20BB recognize and kill CD19- and/or CD20-expressing tumor B cells. This results in a cytotoxic T-lymphocyte (CTL) response against CD19- and/or CD20-expressing tumor cells, thereby causing tumor cell lysis. Both the tumor-associated antigens (TAAs) CD19 and CD20 are B-cell-specific cell surface antigens overexpressed in B-cell lineage malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-CAR-CD3zeta-4-1BB-expressing natural killer cells
Allogeneic natural killer (NK) cells transduced with an mRNA expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), coupled to the signaling domain of 4-1BB (CD137), with potential immunomodulating and antineoplastic activities. NK cells from haploidentical donors are expanded in culture and electroporated with the CAR mRNA. Upon transfusion of the transduced cultured cells, CD19CAR-CD3zeta-4-1BB-expressing allogeneic NK cells bind to and induce selective cytotoxicity in CD19-expressing tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19. Its inclusion may also increase antitumor activity, when compared to the inclusion of the CD3-zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes
Autologous T lymphocytes that have been transduced with a lentiviral vector to express a chimeric antigen receptor (CAR) consisting of a single chain variable fragment (scFv) of anti-CD19 in tandem with an anti-CD20 scFv, and coupled to the cytoplasmic portion of the zeta chain of the human T-cell receptor (CD3zeta), and the co-stimulatory molecule 4-1BB (CD137), with potential immunostimulating and antineoplastic activities. Upon transfusion, anti-CD19-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes recognize and direct T cells to CD19- or CD20-expressing tumor B cells. This results in a cytotoxic T-lymphocyte (CTL) response against CD19- or CD20-expressing tumor cells, and causes tumor cell lysis. Both CD19 and CD20 are B-cell-specific cell surface antigens overexpressed in B-cell lineage malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-CD28-zeta modified CAR CD3+ T lymphocytes JCAR015
Genetically modified CD3-positive-enriched autologous T lymphocytes transduced with a replication incompetent gamma retroviral vector expressing a chimeric T-cell antigen receptor (CAR) consisting of an anti-CD19 single chain variable fragment (scFv), fused to the extracellular, transmembrane and intracellular signaling domains of the T-cell co-stimulatory receptor CD28 and the cytoplasmic signaling domain of the zeta chain of the TCR/CD3 complex (CD3-zeta) (CAR19-28z), with potential antineoplastic activities. Upon intravenous administration, autologous CD19-28z CAR-expressing CD3+ T lymphocytes are directed to CD19-expressing tumor cells, and, upon binding to the T cells, induce selective toxicity in CD19-expressing tumor cells. CD19 antigen is a B-cell-specific cell surface antigen expressed in all B-cell lineage malignancies. The CD28 co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19. The inclusion of the CD28 signaling domain may increase proliferation of T cells and antitumor activity compared to the inclusion of the CD3-zeta chain alone. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD19-DM4 immunoconjugate SAR3419
An immunoconjugate consisting of an anti-CD19 monoclonal antibody conjugated to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-CD19-DM4 conjugate SAR3419 targets the cell surface antigen CD19, found on a number of B-cell-derived cancers. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CD19-expressing tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 B9E9 scFv-streptavidin fusion protein
An Escherichia coli periplasm-expressed tetrameric fusion protein composed of four single-chain variable regions (scFv) of the murine immunoglobulin (Ig) G2a anti-CD20 monoclonal antibody B9E9 fused to the streptavidin (SA) gene of Streptomyces avidinii (scFv-SA), with potential use in pretargeted radioimmunotherapy (PRIT). Upon intravenous administration of the anti-CD20 B9E9 scFv-SA fusion protein, this agent targets and binds to CD20-expressing tumor cells. Subsequently, a biotinylated N-acetylgalactosamine-containing clearing agent is administered, which binds to the streptavidin moiety of the unbound fusion protein and promotes its hepatic excretion. In turn, radiolabeled DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid)-biotin is administered and, due to its small size, quickly distributes. The biotin moiety efficiently binds to the SA moiety of the bound fusion protein, which localizes the biotin-conjugated radionuclide to the tumor site. CD20, a tumor-associated antigen (TAA), is overexpressed on B-cell malignancies. PRIT increases both tumor uptake and renal elimination of the radionuclide conjugate as compared to conventional radioimmunotherapy (RIT), where the radioisotope is bound to the antibody before administration; this increases the dose of radionuclide delivered to the tumor while limiting radiation exposure for normal, healthy tissues. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 monoclonal antibody B001
A recombinant humanized monoclonal antibody directed against human CD20 with potential antineoplastic activity. Upon intravenous administration, anti-CD20 monoclonal antibody B001 specifically binds to CD20 on the surfaces of B cells. Although the exact mechanisms through which B001 exert its effects have not been elucidated, B001 may induce a B-cell-directed cell-mediated immune response against CD20-expressing B cells and/or prevent CD20-medaited signaling. This induces tumor cell apoptosis and inhibits proliferation. CD20 is a non-glycosylated cell surface phosphoprotein which is exclusively expressed on B cells during most stages of B-cell development and which is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 monoclonal antibody BAT4306F
A recombinant, glycosylation-modified monoclonal antibody directed against the human B-cell-specific cell surface antigen CD20, with potential antineoplastic and immunomodulating activities. Upon administration of anti-CD20 monoclonal antibody BAT4306F, the antibody specifically targets and binds to CD20. This induces antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B cells, which leads to B-cell apoptosis and the inhibition of tumor cell proliferation. CD20, a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B-cell development, is often overexpressed in B-cell malignancies. The complete defucosylation of BAT4306F may result in enhanced ADCC. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 monoclonal antibody MIL62
A glyco-engineered recombinant humanized monoclonal antibody directed against the human B-cell-specific cell surface antigen CD20, with potential antineoplastic and immunomodulating activities. Upon administration of anti-CD20 monoclonal antibody MIL62, the antibody specifically targets and binds to CD20. This induces antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B cells, which leads to B-cell apoptosis and the inhibition of tumor cell proliferation. In addition, MIL62 inhibits CD20-mediated signaling which further induces apoptosis in and inhibits proliferation of CD20-expressing tumor cells. CD20, a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B-cell development, is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 monoclonal antibody SCT400
A chimeric monoclonal antibody directed against human CD20, with potential antineoplastic activity. Anti-CD20 monoclonal antibody SCT400 binds to the B cell-specific cell surface antigen CD20, which triggers an immune response against CD20-positive B-cells, leading to apoptosis. CD20, a non-glycosylated cell surface phosphoprotein, is exclusively expressed on B-cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 monoclonal antibody TL011
A monoclonal antibody directed against human CD20 with potential antineoplastic activity. Anti-CD20 monoclonal antibody TL011 specifically binds to the B cell-specific cell surface antigen CD20 antigen (MS4A1; membrane-spanning 4-domains, subfamily A, member 1), thereby potentially triggering an immune response against CD20-positive B cells, leading to B cell apoptosis. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development and is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20 monoclonal antibody-interferon alpha fusion protein IGN002
A humanized monoclonal antibody directed against the human B-cell-specific cell surface antigen CD20 and fused to the recombinant cytokine, interferon-alpha (IFN-a), with potential antineoplastic and immunomodulating activities. Upon administration of anti-CD20 monoclonal antibody-interferon alpha fusion protein IGN002, the antibody moiety specifically targets and binds to CD20. In turn, the IFN-a moiety binds to the IFN receptor, and activates IFN-mediated signal transduction, which induces the transcription and translation of genes whose protein products mediate anticancer effects. This results in the induction of both G2 cell cycle arrest and apoptosis in CD20-expressing tumor cells. In addition, IGN002 causes the induction of complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B-cells, which leads to B-cell apoptosis and the inhibition of tumor cell proliferation. CD20, a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B-cells during most stages of B-cell development, is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20/anti-CD3 bispecific IgM antibody IGM2323
An engineered immunoglobulin M (IgM) bispecific antibody, with potential antineoplastic activity. Anti-CD20/CD3 bispecific IgM antibody IGM2323 contains ten high affinity binding domains for the tumor-associated antigen (TAA) CD20, and one binding domain for CD3, a T-cell surface antigen. Upon administration, IGM2323 binds to both T cells and CD20-expressing B-lineage tumor cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against the CD20-expressing tumor B cells. Additionally, IGM-2323 induces complement-dependent cytotoxicity (CDC) to a greater extent than anti-CD20/anti-CD3 IgG bispecific antibodies, thereby further enhancing the killing CD20-expressing tumor cells. The extra binding units of IGM-2323 may bind cancer cells that express relatively low amounts of CD20. Also, compared to IgG format bispecific T-cell engaging antibodies, IGM2323 appears to induce less cytokine release, which may reduce the risk of cytokine release syndrome (CRS). CD20 is exclusively expressed on B-cells during most stages of B cell development and is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20/CD3 monoclonal antibody REGN1979
A bispecific, human monoclonal antibody with potential antineoplastic activity. Anti-CD20/CD3 monoclonal antibody REGN1979 contains two antigen-recognition sites: one for human CD3, a T cell surface antigen, and one for human CD20, a tumor-associated antigen that is exclusively expressed on B-cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Upon administration, REGN1979 binds to both T-cells and CD20-expressing tumor B-cells, which cross-links the T-cells to tumor cells, and may result in a potent cytotoxic T-lymphocyte (CTL) response against CD20-expressing tumor B-cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20/CD3 monoclonal antibody XmAb13676
A bispecific, Fc domain-containing, monoclonal antibody with potential antineoplastic activity. Anti-CD20/CD3 monoclonal antibody XmAb13676 contains two antigen-recognition sites: one for human CD3, a T-cell surface antigen, and one for human CD20, a tumor-associated antigen (TAA) that is exclusively expressed on B cells during most stages of B-cell development and is often overexpressed in B-cell malignancies. Upon administration, XmAb13676 binds to both T cells and CD20-expressing B-lineage tumor cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against the CD20-expressing tumor B-cells. Inclusion of an Fc domain on the antibody prolongs the half-life of the bispecific antibody and enhances T-cell-mediated tumor cell killing because the agent is able to bind to Fc receptors. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD205 antibody-drug conjugate OBT076
An antibody-drug conjugate (ADC) comprised of an anti-CD205 (lymphocyte antigen 75; Ly75) humanized immunoglobin G1 (IgG1) monoclonal antibody conjugated to DM4, a maytansinoid microtubule disruptor, via a cleavable N-succinimidyl-4-(2-pyridyldithio) butanoate (SPDB) linker, with potential antineoplastic activity. Upon intravenous administration, anti-CD205 ADC OBT076 specifically targets and binds to CD205, a receptor involved in antigen capture and endocytosis, expressed on tumor cells. Following rapid internalization of the ADC/CD205 complex, OBT076 releases its DM4 payload due to cleavage of the SPDB linker by intracellular proteases. Then the DM4 binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in the inhibition of both cell division and cell growth of CD205-expressing tumor cells. CD205, a type I transmembrane surface glycoprotein belonging to the C-type lectin receptor family, is normally expressed on various antigen-presenting cells (APCs) and some leukocyte sub-populations but it is overexpressed in multiple cancer types where it plays a key role in facilitating metastatic invasion. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes
A preparation of autologous blood T-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD20 scFv (single chain variable fragment); the cytoplasmic portion of the human TCR-[zeta] molecule; and the co-stimulatory molecule 4-1BB (CD137), with potential immunostimulating and antineoplastic activities. Upon transfusion, anti-CD20-CAR-CD3zeta-4-1BB-expressing autologous T-lymphocyte cells direct T-cells to CD20-expressing tumor cells. This results in cytotoxic T lymphocyte (CTL) and antibody responses against CD20-expressing tumor cells, causing tumor cell lysis. The CD20 antigen, a non-glycosylated cell surface phosphoprotein, is a B-cell specific cell surface antigen expressed in B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD20; the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone.
anti-CD20-engineered toxin body MT-3724
An engineered toxin body (ETB) composed of the single-chain variable fragment (ScFv) from an antibody targeting CD20 that is linked to a modified form of the ribosome-inactivating alpha subunit of Shiga-like toxin 1 (Shiga-like Toxin-1 A or SLT-1A), with antineoplastic activity. Upon administration, the ScFv moiety of anti-CD20-engineered toxin body MT-3724 targets and binds to the CD20 antigen expressed on tumor cells. Upon internalization, the SLT-1A moiety is released and acts as an N-glycosidase, which binds to and cleaves an adenine nucleobase in the 28S RNA component of the 60S subunit of ribosomes and prevents ribosome activity. This inhibits protein synthesis and eventually leads to apoptosis of CD20-expressing tumor cells. CD20, a B-cell specific transmembrane protein and tumor-associated antigen (TAA), is expressed during most stages of B-cell development and is often overexpressed in B-cell malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD22 ADC TRPH-222
An antibody-drug conjugate (ADC) composed of an anti-CD22 humanized monoclonal antibody site-specifically conjugated, via formylglycine (FG) residues and a protease insensitive 4AP linker, to a cytotoxic microtubule-targeting maytansinoid payload, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of TRPH-222 binds to B-cell-specific CD22 receptors and is rapidly internalized, thereby delivering the payload intracellularly. Upon proteolytic cleavage, the maytansinoid payload binds to tubulin, disrupting microtubule assembly/disassembly dynamics, inhibiting both cell division and tumor cell proliferation. CD22, a cell surface sialoglycoprotein, is expressed on mature B-cells and on most malignant B-cells. The site specific and stable conjugation to the payload allows for a higher drug-to-antibody ratio (DAR) and an enhanced therapeutic index. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD22 CAR-expressing T lymphocytes
A preparation of human T lymphocytes transduced with a recombinant viral vector encoding a chimeric T-cell receptor (chimeric antigen receptor or CAR) consisting of one or more binding domains targeting the tumor-associated antigen (TAA) CD22 and fused to one or more co-stimulatory, TCR-signaling domains, with potential immunostimulating and antineoplastic activities. Upon administration, the anti-CD22 CAR-expressing T lymphocytes, express anti-CD22-CAR on their cell surfaces and bind to the CD22 antigen on tumor cell surfaces. Subsequently, CD22-expressing B cells are lysed. CD22, a B-lineage-restricted, transmembrane phosphoglycoprotein, is expressed on malignant B cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD22 monoclonal antibody-MMAE conjugate DCDT2980S
An antibody-drug conjugate (ADC) composed of MCDT2219A , a humanized IgG1 anti-CD22 monoclonal antibody covalently linked, via a protease-cleavable peptide linker, to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DCDT2980S binds to B-cell-specific CD22 receptors and is rapidly internalized, thereby delivering MMAE intracellularly. Upon proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. CD22, a cell surface glycoprotein, is expressed on mature B-cells and on most malignant B-cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD22 scFv TCRz:41BB-CAR lentiviral vector-transduced autologous T lymphocytes
Autologous human T lymphocytes transduced with a recombinant lentiviral vector encoding a chimeric T cell receptor consisting of an anti-CD22 single chain variable fragment (scFv) and the co-stimulatory domain 4-1BB (CD137) coupled to the zeta chain of the TCR/CD3 complex (CD3-zeta), with potential immunostimulating and antineoplastic activities. Autologous peripheral blood lymphocytes (PBLs) from a patient with CD22-positive cancer are transduced with this lentiviral vector that encodes the CAR gene specific for CD22. After isolation, transduction, expansion in culture and reintroduction into the patient, the anti-CD22 scFv TCRz:41BB-CAR lentiviral vector-transduced autologous T lymphocytes express anti-CD22-CAR on their cell surfaces and bind to the CD22 antigen on tumor cell surfaces. Subsequently, CD22-expressing tumor cells are lysed. CD22, a B-lineage-restricted, transmembrane phosphoglycoprotein, is expressed on malignant B cells. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD228/MMAE antibody-drug conjugate SGN-CD228A
An antibody-drug conjugate (ADC) composed of a humanized antibody targeting the cell surface antigen cluster of differentiation (CD228; melanotransferrin; MFI2; MELTF) that is conjugated, via a beta-glucuronidase-cleavable linker, to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Following administration, the antibody moiety of anti-CD228/MMAE ADC SGN-CD228A targets and binds to CD228 on the surface of tumor cells. Following internalization of SGN-CD228A and release of MMAE, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in CD228-expressing tumor cells. CD228, a cell-surfaced, glycosylphosphatidylinoitol (GPI)-anchored glycoprotein, belongs to the transferrin family of iron-binding proteins. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD22-CAR m971-BBz lentiviral vector-transduced autologous T lymphocytes
Autologous human T-lymphocytes transduced with a recombinant lentiviral vector encoding a chimeric T-cell receptor (chimeric antigen receptor or CAR) consisting of an anti-CD22 single chain variable fragment (scFv) derived from the monoclonal antibody (moAb) 971 (m971), and the co-stimulatory domain 4-1BB (CD137) coupled to the zeta chain of the TCR/CD3 complex (CD3-zeta), with potential immunostimulating and antineoplastic activities. Autologous peripheral blood lymphocytes (PBLs) from a patient with CD22-positive cancer are transduced with this lentiviral vector that encodes the CAR gene specific for CD22. After expansion in culture and reintroduction into the patient, the anti-CD22-CAR m971-BBz lentiviral vector-transduced autologous T-lymphocytes express anti-CD22-CAR on their cell surfaces and bind to the CD22 antigen on tumor cell surfaces. Subsequently, CD22-expressing tumor cells are lysed. CD22, a B-lineage-restricted, transmembrane phosphoglycoprotein, is expressed on malignant B-cells. m971 binds to a membrane proximal epitope on CD22 and has a higher binding affinity compared to any other anti-CD22 moAb. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD25 monoclonal antibody RO7296682
A monoclonal antibody against CD25 (IL-2R alpha), with potential antineoplastic activity. Upon administration, the anti-CD25 monoclonal antibody RO7296682 targets and binds to CD25 expressed on tumor-infiltrating regulatory T (Treg) cells. This may deplete Treg cells and prevent immunosuppression, thereby enhancing anti-tumor immune responses. CD25, the alpha chain of the interleukin (IL)-2 receptor, is highly expressed on Treg cells but not on effector T (Teff) cells in tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD26 monoclonal antibody YS110
A humanized, immunoglobulin G1 (IgG1) monoclonal antibody directed against the extracellular domain of dipeptidyl peptidase 4 (CD26; DPP4; DPP IV), with potential antineoplastic activity. Upon administration of anti-CD26 monoclonal antibody YS110, this antibody targets and binds to CD26 expressed on tumor cells. This inhibits CD26 activity and causes internalization of CD26-YS110. This leads to cell cycle arrest, lysis and inhibition of growth in CD26-positive tumor cells. YS110 also induces antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) against CD26-expressing tumor cells. CD26, a 110-kDa, type II transmembrane glycoprotein, is overexpressed in a variety of cancer cell types while absent in normal, healthy cells and plays a key role in tumor cell growth, migration, invasion and survival. It also plays a major role in the regulation of T-cell activity. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD27 agonistic monoclonal antibody MK-5890
A humanized agonistic monoclonal antibody targeting the cell surface antigen CD27, with potential immunostimulatory and antineoplastic activities. Upon administration, anti-CD27 agonistic monoclonal antibody MK-5890 targets and binds to CD27 on a variety of immune cell types, including most T lymphocytes. This induces CD27-dependent signaling pathways and enhances T-cell-mediated responses, including the expansion of antigen-activated T cells and the cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. CD27, a co-stimulatory molecule and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T-lymphocytes, memory B cells and natural killer (NK) cells. It plays an important role in NK cell-mediated cytolytic activity and T- and B-lymphocyte proliferation and activation. It is overexpressed in certain tumor cell types. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD27L antibody-drug conjugate AMG 172
An immunoconjugate consisting of a human IgG1 monoclonal antibody directed against CD27L conjugated, via a non-cleavable linker, to the cytotoxic agent maytansinoid DM1, with potential antineoplastic activity. The monoclonal antibody moiety of this immunoconjugate binds to CD27L on tumor cell surfaces. After internalization, the DM1 moiety binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting both cell division and proliferation of cancer cells that express CD27L. CD27L, a type II transmembrane protein and member of the tumor necrosis factor family, is a co-stimulatory molecule constitutively expressed on a subset of activated T-cells, B-cells, and dendritic cells, which is overexpressed in certain tumor cell types. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1)
A bivalent recombinant fusion protein immunotoxin derived from the anti-CD3 monoclonal antibody UCHT1 with potential antineoplastic activity. Anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1) consists of 1-390 amino acid residues of chain A diphtheria toxin (DT) joined via a spacer to the Fv fragment of UCHT1, which is connected to a second UCHT1 Fv fragment via a disulfide bond (hence the "bisFv" designation); the addition of the second Fv fragment overcomes the steric hindrance of immunotoxin binding due to the large N-terminal DT domain. Once inside target T cells, the DT moiety catalyzes the transfer of the ADP-ribose moiety of NAD to diphthamide, a posttranslationally modified histidine residue found in elongation factor 2 (EF-2); inactivation of EF-2, disruption of polypeptide chain elongation, and cell death ensue. CD3 is a complex of five cell-surface polypeptides associated with the T cell receptor (TCR) complex. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD3 x anti-CD20 bispecific antibody-armed activated T cells
Autologous activated T cells that have been coated with bispecific antibodies (BiAb), with potential antineoplastic and immunomodulating activities. In vitro, T cells are activated through exposure to the anti-CD3 murine monoclonal antibody OKT3 and low-dose interleukin 2 (Il-2) for 6-14 days and then armed with anti-CD3 x anti-CD20 bispecific antibody (CD20Bi). Upon administration, anti-CD3 x anti-CD20 bispecific antibody-armed activated T cells (AATC) attach to CD3-expressing T cells and CD20-expressing tumor cells, selectively cross-linking T cells and tumor cells. This may result in the recruitment and activation of cytotoxic T lymphocyte (CTLs), CTL-mediated specific tumor cell lysis, and the secretion of antitumor cytokines and chemokines. CD20, a cell surface phosphoprotein, is found on normal B cells and most B-cell tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD3/5T4 IgG1 bispecific antibody GEN1044
A recombinant immunoglobulin G1 (IgG1) bispecific antibody targeting both the human T-cell surface antigen CD3 and oncofetal antigen 5T4, with potential immunomodulating and antineoplastic activities. Upon administration, anti-CD3/anti-5T4 bispecific antibody GEN1044 simultaneously targets and binds to CD3 expressed on T cells and 5T4 expressed on tumor cells. The resulting cross-linkage may trigger a potent cytotoxic T-lymphocyte (CTL) response against the 5T4-expressing tumor cells. 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types; its expression is correlated with increased invasiveness. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD3/anti-BCMA bispecific monoclonal antibody JNJ-64007957
A bispecific humanized monoclonal antibody against human CD3, a T-cell surface antigen, and human B-cell maturation antigen (BCMA; TNFRSF17), a tumor-associated antigen (TAA) expressed on plasma cells, with potential antineoplastic activity. Upon administration, anti-CD3/anti-BCMA bispecific monoclonal antibody JNJ-64007957 binds to both CD3 on T cells and BCMA expressed on malignant plasma cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against BCMA-expressing plasma cells. BCMA, a member of the tumor necrosis factor receptor superfamily member that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival. Check for active clinical trials using this agent. (NCI Thesaurus)
anti-CD3/anti-BCMA bispecific monoclonal antibody PF-06863135
A bispecific monoclonal antibody against human CD3, a T-cell surface antigen, and human B-cell maturation antigen (BCMA; TNFRSF17), a tumor-associated antigen (TAA) expressed on plasma cells, with potential antineoplastic activity. Upon administration, anti-CD3/anti-BCMA bispecific monoclonal antibody PF-06863135 binds to both CD3 on T cells and BCMA expressed on malignant plasma cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against BCMA-expressing plasma 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.
anti-CD3/anti-CD20 trifunctional bispecific monoclonal antibody FBTA05
A trifunctional bispecific monoclonal antibody with potential antineoplastic activity. FBTA05 contains two antigen-recognition sites: one for human CD3, a T cell surface antigen; and one for human CD20, a tumor-associated antigen that is exclusively expressed on B cells during most stages of B-cell development and often overexpressed in B-cell malignancies. In addition, the modified Fc portion of this antibody binds Fc receptors on antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs). FBTA05 brings T cells, CD20-expressing tumor B-cells and APCs together into tricellular complexes, which may result in a potent cytotoxic T-lymphocyte (CTL) response against CD20-expressing tumor B-cells. Fc-mediated binding of APCs in the tricellular complex potentiates CD20 antigen presentation to T cells and the activation of anti-tumor cytotoxic T cells. Check for active clinical trials using this agent. (NCI Thesaurus)