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NCI Drug Dictionary

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338 results found for: G

G protein-coupled estrogen receptor agonist LNS8801
An orally bioavailable selective agonist of the G protein-coupled estrogen receptor (G protein-coupled estrogen receptor 1; GPER; GPER1; GPR30), with potential immunomodulating and antineoplastic activities. Upon oral administration, LNS8801 targets, binds to and activates GPER. This activates GPER-mediated signaling and suppresses the expression of various tumor-associated genes, such as c-Myc and programmed cell death-ligand 1 (PD-L1). This leads to an inhibition of tumor cell proliferation. GPER activation may also induce immune memory. GPER is a membrane protein and a member of the G-protein coupled receptors (GPCRs) that are widely distributed in various tissues. GPER is a tumor suppressor in a wide range of cell cancer types.
G-quadruplex stabilizer BMVC
A carbazole derivative (3,6-bis[2-(1-methylpyridinium)vinyl]carbazole diiodide) that selectively targets to the G-quadruplex DNA structure, used as a fluorescent probe for cancer cytological diagnosis and with potential antitumor activity. G-quadruplex stabilizer BMVC, preferentially uptaken by cancer cells, binds to and stabilizes the telomeric G-quadruplex structure at the end of DNA; when visualized with fluorescent imaging device, BMVC emits bright fluorescent light and can be used to differentiate tumor cells from normal cells. The BMVC/G-quadruplex complexes also interfere with the activity of telomerase, which is highly active in tumor cells and plays a key role in tumorigenesis while expressed at very low levels in most somatic cells.
G. lucidum/A. blazei/G. frondosa/H. erinaceus/C. sinensis/I. obliquus/P. ostreatus/P. umbellatus/ L. edodes supplement
A dietary supplement composed of fungal extracts of Ganoderma lucidum, Agaricus blazei, Grifola frondosa, Hericium erinaceus, Cordyceps sinensis, Inonotus obliquus, Pleurotus ostreatus, Polyporus umbellatus and Lentinula edodes, with potential anti-inflammatory and immunomodulatory activities. Upon oral administration of G. lucidum/A. blazei/G. frondosa/H. erinaceus/C. sinensis/I. obliquus/P. ostreatus/P. umbellatus/ L. edodes supplement, the fungal polysaccharides in this dietary supplement may modulate the composition of the gut microflora and reduce gut pathogen levels. In addition, the fungal polysaccharides may support the body's immune function and may have anti-inflammatory activities.
G207
A neuroattenuated, replication-competent, recombinant herpes simplex virus-1 (HSV-1) with potential oncolytic activity. Upon intracerebral administration, oncolytic HSV-1 G207 preferentially replicates within glioma cells, which may elicit tumor-specific systemic immune and cytotoxic T lymphocyte (CTL) responses in addition to direct cytopathic effects. Derived from wild-type HSV-1 strain F, this agent has been neuroattenuated by deletions in both copies of the gamma34.5 gene, the major determinant of HSV neurovirulence. In addition, the HSV-1 gene UL39, encoding the viral ribonucleotide reductase large subunit infected cell protein 6 (ICP6), has been inactivated through the insertion of the Escherichia coli lacZ gene. By inactivating UL39, viral ribonucleotide reductase activity is disrupted, resulting in the inhibition of nucleotide metabolism and viral DNA synthesis in nondividing cells but not in dividing cells.
G250 peptide vaccine
A cancer vaccine containing of a synthetic form of the renal cell carcinoma (RCC)-associated antigen G250 with potential antineoplastic activity. Vaccination with G250 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the G250 antigen, resulting in decreased tumor growth. Found in the majority of renal cell carcinomas, G250 is a cell surface tumor-associated antigen (TAA) that contains an HLA-A2.1-restricted epitope that is recognized by CTLs.
Ga-68-labeled F(ab') 2- trastuzumab
A radioimmunoconjugate consisting of a trastuzumab fragment labeled with the positron-emitting radioisotope gallium Ga 68 with radioisotopic and antibody activities. Upon administration, Ga-68-labeled F(ab')2-trastuzumab may bind to HER2-positive tumor cells, allowing radioimmunolocalization with positron emission tomography (PET). Trastuzumab is a recombinant humanized monoclonal antibody that selectively binds to the extracellular domain of human epidermal growth factor receptor 2 (HER2), overexpressed by many adenocarcinomas, particularly breast adenocarcinomas.
gabapentin
A synthetic analogue of the neurotransmitter gamma-aminobutyric acid with anticonvulsant activity. Although its exact mechanism of action is unknown, gabapentin appears to inhibit excitatory neuron activity. This agent also exhibits analgesic properties.
Gablofen
(Other name for: baclofen)
Gadavist
(Other name for: gadobutrol)
gadobenate dimeglumine
A gadolinium-based paramagnetic contrast agent. When placed in a magnetic field, gadobenate dimeglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI.
gadobutrol
A gadolinium-based, hydrophilic, macrocyclic, electrically neutral contrast agent used in contrast-enhanced MRI (CE-MRI). Gadobutrol is a non-ionic, paramagnetic complex consisting of gadolinium (Gd3+) chelated with the macrocyclic compound dihydroxy-hydroxymethylpropyl-tetraazacyclododecane-triacetic acid (butrol). Following intravenous administration, gadobutrol may increase MRI sensitivity for the detection of tumors and inflammatory and demyelinating diseases of the central nervous system (CNS) which are associated with areas with blood-brain barrier defects due to altered perfusion or an enlarged extracellular space. This agent is eliminated in an unchanged form via the kidneys; extra-renal elimination is negligible.
gadodiamide
A paramagnetic gadolinium-based contrast agent (GBCA), with imaging activity upon magnetic resonance imaging (MRI). When placed in a magnetic field, gadodiamide generates a large local magnetic field, which can enhance the relaxation rate of nearby protons. This change in proton relaxation dynamics, iincreases the MRI signal intensity of tissues in which gadodiamide has accumulated; therefore, visualization of those tissues is enhanced.
gadofosveset trisodium
The trisodium salt form of gadofosveset, an injectable, intravascular, amphiphilic gadolinium-based contrast agent (GBCA) used with magnetic resonance angiography (MRA) imaging. Gadofosveset is a stable gadolinium diethylenet triaminepentaacetic acid (Gd-DTPA) chelate derivative with a diphenylcyclohe xylphosphate group. Upon injection, gadofosveset binds reversibly to endogenous serum albumin which increases its intravascular retention time compared to non-protein binding contrast agents. The serum albumin binding also increases T1-relaxivity of gadofosveset. This produces an increase in signal intensity of blood, thereby enhancing the visualization of blood vessels upon MRA and may aid in the diagnosis of certain blood vessels and heart disorders.
gadolinium-based contrast agent BAY1747846
A gadolinium (Gd)-based contrast agent (GBCA) that can potentially be used for contrast-enhanced MRI (CE-MRI). Upon intravenous administration of GBCA BAY1747846, and upon placement in a magnetic field, this agent produces a large magnetic moment and creates a large local magnetic field, which can enhance the relaxation rate of nearby protons. This change in proton relaxation dynamics increases the MRI signal intensity of tissues in which this agent has accumulated due to abnormal vascularity and altered perfusion. This allows for enhanced contrast and visualization of those tissues compared to unenhanced MRI.
gadolinium-chelate
A coordination complex consisting of a gadolinium ion bound to a hexadentate organic chelating agent such as diethylenetriaminepentaacetic acid. Chelates of gadolinium are frequently utilized as magnetic resonance imaging (MRI) contrast agents and can be used to track nanoparticle-mediated drug delivery.
gadopentetate dimeglumine
A gadolinium complex of diethylenetriamine pentaacetic acid with ionic paramagnetic properties. Gadopentetate dimeglumine may provide contrast enhancement during magnetic resonance imaging (MRI) of intracranial lesions with abnormal vascularity or of abnormalities in the blood-brain barrier (BBB).
gadopiclenol
A gadolinium-based paramagnetic contrast agent, with potential imaging enhancing activity upon magnetic resonance imaging (MRI). Upon administration of gadopiclenol and placement in a magnetic field, this agent produces a large magnetic moment and creates a large local magnetic field, which can enhance the relaxation rate of nearby protons. This change in proton relaxation dynamics, increases the MRI signal intensity of tissues in which this agent has accumulated; therefore, contrast and visualization of those tissues is enhanced compared to unenhanced MRI.
gadoterate meglumine
A gadolinium chelate paramagnetic contrast agent. When placed in a magnetic field, gadoterate meglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI.
Gadovist
(Other name for: gadobutrol)
Gadoxetate Disodium
A paramagnetic contrast agent consisting of the disodium salt of the gadolinium ion chelated with the lipophilic moiety ethoxybenzyl (EOB) bound to diethylenetriamine pentaacetic acid (DTPA). When placed in a magnetic field, gadolinium produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because this agent is excreted in the bile, it may be used to visualize the biliary system using MRI.
Gag:267-274 peptide vaccine
A peptide vaccine containing the amino acids 267 through 274 of the human immunodeficiency virus type 1 (HIV-1) gag core protein (gag:267-274), with potential immunostimulating activity. Upon vaccination, the immune system may exert a potent cytotoxic T-lymphocyte (CTL) response against the xenoantigen gag:267-274 and produces pro-inflammatory cytokines. The concomitant administration of a cancer peptide vaccine may benefit from an already activated immune system and may augment an immune response against the administered tumor associated antigen(s). Gag:267-274 peptide is highly immunogenic and may potentially be used as a cancer immunoadjuvant.
galacto-oligosaccharide prebiotic supplement
A nutritional supplement containing fibers and galacto-oligosaccharides (GOS), with potential immunomodulating and prebiotic activities. Upon oral administration of the GOS prebiotic supplement, the GOS stimulates the proliferation of beneficial bifidobacteria in the gastrointestinal (GI) tract. This modulates the GI flora ecosystem and protects against harmful viruses and bacteria. The bacterial metabolites, such as the short chain fatty acid (SCFA) butyrate, may be essential for normal differentiation of regulatory immune cells in the intestine. In addition, the GOS prebiotic supplement may inhibit inflammation by increasing the level of anti-inflammatory cytokines and decreasing the level of proinflammatory cytokines.
galactomannan derivative
A carbohydrate polymer composed of mannose and galactose, with chemotherapeutic enhancing activity. Galactomannan derivative binds to galectins on cell surfaces and may promote the transport of certain chemotherapeutics, such as 5-fluorouracil (5-FU), into tumor cells. This may increase the antineoplastic effect of 5-FU when administered concomitantly. Galectins are carbohydrate-binding proteins, upregulated on the surface of certain types of tumor cells, and may mediate cell association, survival and metastasis.
galactose
A hexose which is almost identical to glucose except that orientation of -H and -OH on carbon 4 are exchanged, making it an epimer at C-4 of glucose (in Fisher projection).
galantamine hydrobromide
The hydrobromide salt form of galantamine, a tertiary alkaloid obtained synthetically or naturally from the bulbs and flowers of Narcissus and several other genera of the Amaryllidaceae family with anticholinesterase and neurocognitive-enhancing activities. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). In addition, galantamine is a ligand for nicotinic acetylcholine receptors, which may increase the presynaptic release of Ach and activate postsynaptic receptors. This agent may improve neurocognitive function in mild and moderate Alzheimer' s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse.
galectin-1 inhibitor OTX008
A calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteosomal degradation through a not yet fully elucidated mechanism, and eventually downregulates Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses.
galeterone
An orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.
galinpepimut-S
A peptide cancer vaccine comprised of four peptide chains derived from the Wilms’ tumor gene 1 (WT1) protein, with potential immunomodulating and antineoplastic activities. Upon administration, galinpepimut-S, which is comprised of one WT1-derived peptide (WT-A1) that may stimulate CD8-positive T-cell responses; two WT1 peptides (WT1-427 long, WT1-331 long) that may stimulate CD4-positive T-cell responses; and one modified peptide (WT1-122A1 long) that may stimulate both CD4-positive and CD8-positive T cells, may elicit a targeted innate immune response against WT1-expressing tumor cells. WT1 protein, a zinc finger DNA-binding protein and transcription factor, is overexpressed in leukemic cells and in many non-hematological solid tumors.
galiximab
A humanized IgG1 monoclonal antibody directed against CD80, the natural ligand for the T-cell antigen CD28 which mediates T-cell and B-cell adhesion. Galiximab binds to CD80 expressed on the cell surfaces of follicular lymphomas, resulting in antibody-dependent cell-mediated cytotoxicity (ADCC). CD80 is expressed on activated B-cells and gamma-interferon-stimulated monocytes and is often expressed at low levels on the surfaces of follicular lymphoma cells and other lymphoid malignancies.
gallium citrate Ga 67
The citrate salt of the radioisotope gallium Ga 67. Although the mechanism is unknown, gallium Ga 67 concentrates in lysosomes and is bound to a soluble intracellular protein in certain viable primary and metastatic tumors and focal sites of inflammation, allowing scintigraphic localization. Ga-67 scintigraphy (GS) cannot differentiate between tumor and acute inflammation.
gallium Ga 68 AIP-301
A radioconjugate composed of AIP-301, a molecule targeting the tumor-associated antigen (TAA) epidermal growth factor receptor 2 (HER2, EGFR2, ERBB2), that is linked to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68 AIP-301, the AIP-301 moiety targets and binds to HER2-expressing tumor cells. This facilitates both the detection of HER2-expressing tumor cells and the assessment of responses to AIP-303 and other HER2-targeted chemotherapeutic agents during PET/CT. HER2, a tyrosine kinase, is overexpressed on the cell surfaces of various tumor cell types.
gallium Ga 68 EB-ss-CPT
A radioconjugate composed of the amphiphilic camptothecin (CPT) prodrug EB-ss-CPT, labeled with the radioisotope gallium Ga 68, with potential use as a tracer for tumor cells during positron emission tomography (PET). EB-ss-CPT is composed of CPT conjugated, via a redox-responsive disulfide linker, to an albumin-binding Evans blue (EB) derivative. Upon administration of gallium Ga 68 EB-ss-CPT, the EB-ss-CPT moiety binds to endogenous albumin and the resulting albumin-bound nanocomplex accumulates in tumor cells. This allows the detection and visualization of tumor cells upon PET imaging.
gallium Ga 68 FAP-2286
A radioconjugate composed of FAP-2286, a fibroblast activation protein (FAP)-targeted peptide, attached to a linker and tetraazacyclododecane tetraacetic acid chelator, conjugated to the radioisotope gallium Ga 68, with potential use as a tracer for FAP-expressing cancer-associated fibroblasts (CAFs) during positron emission tomography (PET). Upon administration of gallium Ga 68 FAP-2286, the FAP-2286 moiety targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing cells can be detected during PET imaging. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
gallium Ga 68 FAP-CHX
A radioconjugate composed of FAP-CHX, a fibroblast activation protein (FAP)-targeted tracer, labeled with the radioisotope gallium Ga 68, with potential use as a tracer for FAP-expressing cancer-associated fibroblasts (CAFs) during positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68 FAP-CHX, the FAP-CHX moiety targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing cells can be detected during PET/CT imaging. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
gallium Ga 68 FAPi-46
A radioconjugate composed of FAPi-46, a quinoline-based fibroblast activation protein (FAP)-targeted tracer belonging to the group of FAP inhibitors (FAPi), conjugated to the radioisotope gallium Ga 68, with potential use as a tracer for FAP-expressing tumors during positron emission tomography (PET). Upon administration of gallium Ga 68 FAPi-46, the FAPi-46 moiety targets and binds to FAP-expressing tumor cells. Upon binding, FAP-expressing tumor cells can be detected during PET imaging. FAP, a cell surface protein, is overexpressed in a wide variety of cancer cell types.
gallium Ga 68 FF58
A radiopharmaceutical agent comprised of FF58, a non-arginine-glycine-aspartic acid (Arg-Gly-Asp/RGD) small molecule targeting the transmembrane receptors integrin alpha V beta 3 (avb3) and 5 (avb5), labeled with gallium Ga 68, with potential avb3/5 imaging activity during positron emission topography (PET)/computed tomography (CT). After intravenous administration of gallium Ga 68 FF58, the FF58 moiety selectively targets and binds to avb3/5 on the tumor cell membrane. Upon PET/CT imaging, avb3/5-expressing tumor cells can be visualized and their expression levels can be quantified. avb3/5, members of the integrin receptor family, are overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells; they play key roles in angiogenesis, tumor proliferation and survival.
gallium Ga 68 gozetotide
A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting ligand, Glu-urea-Lys(Ahx) (Glu-NH-CO-NH-Lys(Ahx)), conjugated, via the acyclic radiometal chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'-diacetic acid (HBED-CC), to the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68 gozetotide, the Glu-urea-Lys(Ahx) moiety targets and binds to PSMA-expressing tumor cells. Upon internalization, PSMA-expressing tumor cells can be detected during PET imaging. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
gallium Ga 68 labeled PSMA-targeting radiodiagnostic agent HRS-9815
A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting agent labeled with the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET)/computed tomography (CT)). Upon intravenous administration, gallium Ga 68 labeled PSMA-targeting radiodiagnostic agent HRS-9815 targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells can be detected during PET/CT imaging. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
gallium Ga 68 N188
A radioconjugate composed of a nectin-4 (poliovirus receptor-like 4; PVRL4)-targeting moiety, labeled with gallium Ga 68, with potential nectin-4 imaging activity during positron emission topography (PET)/computed tomography (CT). After intravenous administration of gallium Ga 68 N188, the nectin-4-targeting moiety selectively targets and binds to nectin-4 expressed on tumor cells. Upon PET/CT imaging, nectin-4-expressing tumor cells can be visualized. Nectin-4, a tumor-associated antigen (TAA) belonging to the nectin family, is overexpressed in a variety of cancers, but has a restricted distribution in normal tissue.
gallium Ga 68 NNS309
A radioconjugate composed of NNS309, which targets an as of yet unelucidated target on tumor cells, that is conjugated to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68 NNS309, the NNS309 moiety targets and binds to tumor cells expressing the target. This allows the assessment of binding of NNS309 to tumor cells and the possible therapeutic response to NNS309 conjugated to a radionuclide delivering cytotoxic radiation, such as lutetium Lu 177 (Lu177).
gallium Ga 68 NODAGA-CBP8
A radiotracer composed of CBP8, a collagen-targeting peptide, linked via a tris(tert-butyl) ester-protected 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA) chelator, to the radioisotope gallium Ga 68, with potential imaging activity upon positron emission tomography/computed tomography (PET/CT). Upon administration, gallium Ga 68 NODAGA-CBP8 selectively binds with high affinity to collagen type 1. Upon PET/CT imaging, gallium Ga 68 NODAGA-CBP8 can be used to detect lung fibrosis, which is characterized by excess deposition of collagens, primarily type 1 collagen, and other extracellular matrix proteins in the parenchyma.
gallium Ga 68 NY104
A radioconjugate composed of NY104, a small molecule carbonic anhydrase IX (CAIX; carbonic anhydrase 9; CA9; G250)-targeting tracer comprised of an acetazolamide core, a hydrophilic spacer and the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), labeled with the radionuclide gallium Ga 68, with potential use as a tracer for CAIX-expressing tumor cells during positron emission tomography (PET). Upon administration of gallium Ga 68 NY104, the NY104 moiety targets and binds to CAIX-expressing tumor cells. Upon binding, CAIX-expressing tumor cells can be detected during PET. CAIX, a member of the carbonic anhydrase family and a tumor-associated antigen (TAA), is found in a majority of renal cell carcinomas while absent in most normal tissues.
gallium Ga 68 P3
A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting ligand, P3, labeled with the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET). Upon intravenous administration of gallium Ga 68 P3, the P3 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells can be detected during PET imaging. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
gallium Ga 68 R8760
A radioconjugate composed of a melanocortin 2 receptor (MC2R; adrenocorticotropic hormone receptor; ACTHR)-binding ligand, conjugated to the radioisotope gallium Ga 68, with potential use as a tracer for MC2R-expressing tumors during positron emission tomography (PET). Upon administration of gallium Ga 68 R8760, the MC2R-targeting moiety targets and binds to MC2R-expressing tumor cells. Upon binding, MC2R-expressing tumor cells can be detected during PET imaging. MC2R, a member of the melanocortin receptor subfamily of type 1 G protein-coupled receptors, plays a key role in adrenal steroidogenesis and is overexpressed in adrenocortical carcinoma.
gallium Ga 68 satoreotide tetraxetan
A radioconjugate consisting of the somatostatin antagonistic peptide satoreotide that is linked via the chelating agent tetraxetan (dodecanetetraacetic acid; DOTA), to the beta-emitting radioisotope gallium Ga 68, with potential imaging activity during positron emission topography/computed tomography (PET/CT). Upon administration, gallium Ga 68 satoreotide tetraxetan binds to somatostatin receptors (SSTRs), with high affinity for SSTR2, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate can be used to quantify tumor uptake of satoreotide using PET/CT. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most normal tissues express low levels of SSTRs.
gallium Ga 68 satoreotide trizoxetan
A radioconjugate consisting of the somatostatin antagonistic peptide OPS202 that is labeled with the positron-emitting radionuclide gallium Ga 68, which may be used as a somatostatin receptor (SSTR) imaging agent in conjunction with positron emission tomography (PET) to image neuroendocrine tumors (NETs). Gallium Ga 68 satoreotide trizoxetan binds to SSTR subtype 2 present on the cell membranes of many types of NETs. This allows for visualization of SSTR-positive cells upon imaging. SSTR subtypes have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTR subtypes.
gallium Ga 68-citrate
A radiopharmaceutical citrate salt form of the positron-emitting radioisotope gallium Ga 68, with potential imaging activity upon positron emission tomography (PET). Upon administration of Gallium Ga 68-citrate, the gallium Ga 3+ ion dissociates from the weak citrate chelator. As Ga3+ is very similar to iron (Fe3+) in chemical properties, this ion acts as an iron analogue. Ga3+ binds to the iron-binding protein transferrin, distributes in blood, and enters and accumulates in the extracellular fluid space of inflamed or tumor-bearing tissue. In turn, the Ga3+-transferrin complex binds to transferrin receptors and is taken up by tumor cells. Tumor cells can then be imaged upon PET. Compared to healthy cells, tumor cells have increased iron metabolism and transferrin receptor expression. Increased Ga3+ uptake is seen in inflamed and infected tissues as well.
gallium Ga 68-DOTA-5G
A radioconjugate composed of 5G, an agent targeting an as of yet undisclosed target, conjugated, via the bifunctional, macrocyclic chelating agent 1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetra-acetic acid (DOTA), to the radioisotope gallium Ga 68, with potential use as a tracer for certain tumors during positron emission tomography (PET). Upon administration of the gallium Ga 68-DOTA-5G, the 5G moiety targets and binds to a specific target on tumor cells. Upon binding, the tumor cells can be detected during PET imaging.
gallium Ga 68-DOTA-exendin-4
A radiopharmaceutical composed of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the positron-emitting radionuclide gallium Ga 68, with potential use in diagnostic imaging upon positron emission tomography (PET). Upon administration of gallium Ga 68-DOTA-exendin-4, the exendin-4 moiety binds to GLP-1R and is subsequently internalized. The radionuclide moiety can be detected using PET and GLP-1R-expressing tumors can be localized. GLP-1R, located on beta cells, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors.
gallium Ga 68-DOTA-FAPI-04
A radioconjugate composed of FAPI-04, a quinoline-based fibroblast activation protein (FAP)-targeted tracer belonging to the group of FAP inhibitors (FAPi), conjugated, through the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), to the radioisotope gallium Ga 68, with potential use as a tracer for FAP-expressing cancer-associated fibroblasts (CAFs) during positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-DOTA-FAPI-04, the FAPI-04 moiety targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing cells can be detected during PET/CT imaging. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
gallium Ga 68-DOTA-MGS5
A radioconjugate consisting of the minigastrin analog, MGS5, conjugated, via the bifunctional, macrocyclic chelating agent 1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetra-acetic acid (DOTA), to the radioisotope gallium Ga 68, with potential use as a tracer for cholecystokinin receptor subtype 2 (CCK2R)-epressing tumor cells during positron emission tomography (PET)/computed tomography (CT). Upon intravenous administration, gallium Ga 68-DOTA-MGS5 targets and binds to tumor cells expressing CCK2R and these cells can be detected upon PET/CT imaging. CCK2R is expressed on a variety of tumor cell types, such as medullary thyroid carcinoma (MTC), and gastroenteropancreatic and bronchopulmonary neuroendocrine tumors (NETs).
gallium Ga 68-DOTA-siglec-9
A radiopharmaceutical composed of the sialic acid binding Ig-like lectin 9 (siglec-9) linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the positron-emitting radionuclide gallium Ga 68, with potential use in diagnostic imaging upon positron emission tomography (PET). Upon administration of gallium Ga 68-DOTA-siglec-9, the siglec-9 moiety binds to the ligand vascular adhesion protein-1 (VAP-1; amine oxidase, copper containing 3; AOC3) in vasculature. VAP-1 is a homodimeric sialylated glycoprotein with enzymatic activity that is expressed on the endothelium of human tissues such as skin, brain, lung, liver and heart in both normal and inflammatory conditions; it mediates leukocyte migration from the bloodstream to sites of inflammation and can also be found in certain cancers. Siglec-9 is primarily expressed on neutrophils, monocytes, macrophages, and dendritic cells. Detection of siglec-9 binding to VAP-1 using PET may serve as a surrogate marker for inflammation and the presence of cancer cells.
gallium Ga 68-DOTANOC
A gallium Ga 68-radiolabeled analogue of somatostatin that may be used in conjunction with positron emission tomography (PET) to image neuroendocrine tumors and metastases. Gallium Ga 68-DOTANOC is a conjugate of the somatostatin analogue 1-Nal3-octreotide (NOC) and gallium Ga 68-labeled 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA). The somatostatin analogue NOC has a high affinity for somatostatin receptor subtypes 2, 3, and 5; these receptor subtypes have been shown to be present in large numbers on neuroendocrine tumors and their metastases, while most other normal tissues express low levels of these somatostatin receptor subtypes.
gallium Ga 68-DOTATATE
A radioconjugate consisting of the somatostatin analogue tyrosine-3-octreotate (Tyr3-octreotate or TATE) labeled with the positron emission tomography (PET) tracer gallium Ga 68 via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA), which may be used as a somatostatin receptor (SSTR) imaging agent in conjunction with PET to image neuroendocrine tumors (NETs). Gallium Ga 68-DOTATATE binds to SSTRs, with a much higher affinity for type 2 SSTR, present on the cell membranes of many types of NETs. This allows for visualization of SSTR-positive cells upon imaging. SSTR subtypes have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTR subtypes.
gallium Ga 68-edotreotide
A radioconjugate consisting of the octreotide derivative edotreotide labeled with gallium 68 (Ga-68) with potential application in somatostatin receptor (SSTR) imaging in conjunction with positron emission tomography (PET). Similar to octreotide, gallium Ga 68-edotreotide binds to SSTRs, especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells and their metastases, thereby allowing for imaging of SSTR-expressing cells upon PET. Gallium Ga 68-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide (Tyr3-octreotide or TOC) and chelating the substituted octreotide to Ga-68 via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA).
gallium Ga 68-EVS459
A radioconjugate composed of EVS459, a folate receptor alpha (FRa; FolRa; FOLR1)-targeting moiety, radiolabeled with gallium Ga 68 (68Ga), with potential imaging activity upon positron emission tomography/computed tomography (PET/CT) or PET/magnetic resonance imaging (MRI). Upon administration of gallium Ga 68-EVS459, the FOLR1-targeting moiety targets and binds to FOLR1 expressed on tumor cells. Upon PET/CT or PET/MRI imaging, FOLR1-expressing tumor cells can be visualized. FOLR1 is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues.
gallium Ga 68-HA-DOTA-TATE
A radioconjugate consisting of consisting of the high affinity somatostatin analogue iodo-tyrosine-3-octreotate (HA-TATE), labeled with the positron emission tomography (PET) tracer gallium Ga 68 via the macrocyclic chelating agent 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetra-acetic acid (DOTA), which may be used as a human somatostatin receptor (SSTR) imaging agent in conjunction with PET to image neuroendocrine tumors (NETs). Gallium Ga 68-HA-DOTATATE binds to SSTRs, with high affinity for SSTR2, present on the cell membranes of many types of NETs. This allows for visualization of SSTR-positive cells upon imaging. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTRs. HA-TATE is an octreotide derivative in which phenylalanine at position 3 is substituted with iodo-tyrosine and threoninol at position 8 is replaced by threonine. The iodo addition in Gallium Ga 68-HA-DOTA-TATE may allow for higher affinity for the SSTRs when compared to gallium Ga 68-DOTA-TATE.
gallium Ga 68-HBED-CC-exendin-4
A radiopharmaceutical composed of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 linked by the acyclic radiometal chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'-diacetic acid (HBED-CC) to the positron-emitting radionuclide gallium Ga 68, with potential imaging activity upon positron emission tomography (PET)/computed tomography (CT). Upon administration of gallium Ga 68-HBED-CC-exendin-4, the exendin-4 moiety binds to GLP-1R. The radionuclide moiety can be detected using PET/CT and GLP-1R-expressing tumors can be localized. GLP-1R, located on beta cells, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors.
gallium Ga 68-ICAM-1pep
A radioconjugate composed of ICAM-1pep, an intercellular adhesion molecule-1 (ICAM-1; CD54)-targeted tracer, labeled with the radioisotope gallium Ga 68, with potential use as a tracer for ICAM-1 during positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-ICAM-1pep, the ICAM-1pep moiety targets and binds to ICAM-1. Upon binding, ICAM-1pep expression can be detected during PET/CT imaging. ICAM-1, an inducible glycoprotein of the immunoglobulin superfamily (IgSF) normally expressed on leukocytes and endothelial cells, may be overexpressed in a variety of cancers. Its expression may also be up-regulated in nonirradiated tumors that are responsive to radiation therapy.
gallium Ga 68-labeled affibody ABY-025
A radioconjugate composed of an optimized affibody conjugated, via its C-terminal cysteine, to maleimide-DOTA, and linked to the radioisotope gallium Ga 68, with potential use as a tracer for human epidermal growth factor receptor type 2 (HER2; ErbB2)-expressing tumors using positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68-labeled affibody ABY-025, the affibody targets HER2-expressing tumor cells. This facilitates both detection of HER2-expressing tumor cells and assessment of responses to HER2-targeting chemotherapeutic agents during PET imaging. The affibody is an optimized antibody mimetic based on a 6.5-kDa 3-helical bundle Z domain derived from the staphylococcal protein A (Z her2:342); the nonbinding surface of the Z domain is reengineered (Z her2:2891) to increase binding affinity for HER2 and to improve tumor imaging. HER2 is overexpressed in many cancer cell types.
gallium Ga 68-labeled alphaVbeta6 binding peptide RAD 301
A radiotracer composed of RAD301, which comprises an integrin alphaVbeta6 (aVb6) binding peptide (BP) and is radiolabeled with the radionuclide gallium Ga 68, with potential integrin aVb6 imaging activity using positron emission tomography (PET). Upon administration of gallium Ga 68-labeled alphaVbeta6 binding peptide RAD301, the aVb6-binding peptide moiety selectively targets and binds to integrin aVb6-positive cancer cells. During PET, aVb6-expressing tumor cells can be visualized and the degree of tumor growth can be determined. Integrin aVb6, a cell adhesion and signaling receptor, is upregulated in certain cancer cell types and has been associated with increased proliferation, migration and invasion of tumor cells.
gallium Ga 68-labeled BNOTA-PRGD2
A radiopharmaceutical agent comprised of a pegylated arginine-glycine-aspartic acid dimer (PRGD2) labeled with gallium Ga 68, with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET) or single photon emission computed tomography (SPECT). This radiopharmaceutical is prepared by conjugating PRGD2 with chelator S-2-(4-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (BNOTA) which is capable of forming a six-coordinate complex with Ga 68. After intravenous administration, gallium Ga 68-labeled BNOTA-PRGD2 binds to alphaVbeta3 integrin on the cell membrane via the cyclic tri-amino acids RGD motif. Upon PET imaging, alphaVbeta3 integrin-expressing tumor cells can be visualized and expression levels can be quantified. Compared to other radiolabeled RGD-containing peptides, this agent shows increased affinity to alphaVbeta3 integrin, enhanced tumor uptake as well as improved pharmacokinetics. alphaVbeta3 integrin is overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells and plays a key role in angiogenesis, tumor proliferation and survival.
gallium Ga 68-labeled DOTA Di-HSG peptide IMP-288
A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide gallium (Ga) 68 with potential use in diagnostic imaging. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor-associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered gallium Ga 68-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; Ga-68 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized upon positron emission tomography (PET).
gallium Ga 68-labeled DX600
A radioconjugate composed of an angiotensin converting enzyme 2 (ACE2)-specific inhibitor DX600 labeled with the radioisotope gallium Ga 68, with potential imaging activity upon positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-labeled DX600, DX600 targets and binds to ACE2. Upon PET/CT imaging, ACE2 expression can be assessed. ACE2 plays an important role in the renin-angiotensin system (RAS), and may be involved in malignancies, diabetes, and liver, cardiovascular and lung diseases. ACE2 is also the main host cell receptor of human pathogenic coronaviruses including severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and plays a key role in viral entry and viral infection. 
gallium Ga 68-labeled MLN6907
A radioconjugate containing a monoclonal antibody directed against guanylyl cyclase C (GCC) labeled with the radioisotope gallium Ga 68, with positron emission tomography (PET) imaging activity. The monoclonal antibody moiety of MLN6907 selectively binds to GCC, a transmembrane receptor normally found on intestinal cells and dopaminergic neurons in the brain, that is also overexpressed on the surface of a variety of cancer cells. Upon internalization of the agent and PET, tumors expressing GCC can be visualized.
gallium Ga 68-labeled NODAGA-MJ9
A radiopharmaceutical agent comprised of a peptide targeting the gastrin releasing peptide receptor (GRPR) chelated with 1,4,7-triazacyclononane,1-glutaric acid-4,7 acetic acid (NODAGA) and radiolabeled with gallium Ga 68, with potential tumor imaging activity upon positron emission tomography (PET). After administration of gallium Ga 68-labeled-NODAGA-MJ9, the MJ9 moiety binds to GRPR located on tumor cells. Upon PET imaging, GRPR-expressing tumor cells can be visualized and expression levels can be quantified. GRPR is overexpressed on certain tumor cells and plays a key role in tumor proliferation and survival.
gallium Ga 68-labeled RM2
A radioconjugate containing a synthetic bombesin receptor antagonist targeting the gastrin-releasing peptide receptor (GRPR), that is linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68 GRPR antagonist BAY86-7548, the peptide moiety targets and binds to GRPR. Upon PET/CT, GRPR-expressing tumor cells can then be visualized. GRPR, also called bombesin receptor 2 (BB2), is a G protein-coupled seven-transmembrane receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers.
gallium Ga 68-labeled tilmanocept
A radioconjugate composed of tilmanocept, a macromolecule consisting of multiple units of mannose and the chelating agent diethylenetriaminepentaacetic acid (DTPA) each covalently attached to a 10 kDa dextran backbone, labeled with the radioisotope gallium Ga 68, with potential use as a tracer for cancer sentinel lymph node (SLN) upon positron emission tomography (PET)/computed tomography (CT). Upon administration, the mannose moiety of gallium Ga 68-labeled tilmanocept selectively binds to macrophage mannose receptor 1 (mannose receptor; MR; CD206) expressed on the surface of macrophages and dendritic cells (DCs) in lymphatic tissue. Upon PET/CT imaging, SLN may be imaged and mapped. Tilmanocept exhibits rapid clearance from the injection site, rapid uptake and high retention within the first draining lymph node, and low uptake by the remaining lymph nodes. CD206, a member of the C-type lectin (CLEC) family that binds mannose or fucose carbohydrate residues, such as those found on the surfaces of many pathogens, is expressed on the surface of macrophages and DCs in lymphatic tissue.
gallium Ga 68-NEB
A radiotracer composed of a truncated form of the azo dye Evans blue (EB) conjugated, via a 1,4,7-triazacyclononane-N,N',N"-triacetic acid (NOTA) linker (NEB), to the radioisotope gallium Ga 68, with potential blood pool imaging activity for use in positron emission tomography (PET). Upon administration of gallium Ga 68-NEB, the NEB moiety, which has high affinity for serum albumin, targets and forms a complex with albumin. Upon PET, the lymph nodes (LN) and lymphatic vessels as well as other desired tissues can be visualized.
gallium Ga 68-NeoB
A radioconjugate consisting of a gastrin-releasing peptide receptor (GRPR) antagonist linked via the chelating agent, dodecanetetraacetic acid (DOTA), to the beta-emitting radioisotope gallium Ga 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration, gallium Ga 68-NeoB binds to GRPRs present on cancer cells. Upon binding, this radioconjugate can be used to quantify tumor uptake of NeoBOMB1 using PET/CT. GRPR, also known as bombesin receptor subtype 2, is a G protein-coupled receptor that is overexpressed in some cancer types.
gallium Ga 68-NODAGA-Ac-Cys-ZEGFR:1907
A radiolabeled recombinant EGFR-specific affibody molecule composed of an epidermal growth factor receptor (EGFR)-targeting protein, the anti-EGFR affibody ZEGFR:1907 with an acetylated cysteine (Ac-Cys) at the N terminal of the affibody, and conjugated to the radioisotope gallium Ga 68, via the chelating agent NODAGA (1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid), with potential use for imaging EGFR-expressing tumor cells upon positron emission tomography (PET). Upon administration of gallium Ga 68-NODAGA-Ac-Cys-ZEGFR:1907, the ZEGFR:1907 affibody molecule moiety targets and binds to the extracellular domain (ECD) of EGFR expressed on various tumor cell types. Upon PET, EGFR-expressing tumor cells can be visualized. EGFR, frequently overexpressed in cancers, plays important roles in cell proliferation, survival, adhesion, migration, and differentiation. The affibody protein scaffold is based on the Z-domain, which is derived from one of the immunoglobulin (Ig) G-binding domains of staphylococcal protein A.
gallium Ga 68-NODAGA-E(c[RGDyK])2
A radiopharmaceutical agent composed of a dimeric cyclic arginine-glycine-aspartic acid (RGD)-based peptide (c[RGDyK]) and labeled, via the chelating agent 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA), with gallium Ga 68, with potential alphaVbeta3 (aVb3) integrin imaging activity upon positron emission topography (PET) or single photon emission computed tomography (SPECT). After intravenous administration of gallium Ga 68-NODAGA-E(c[RGDyK])2, the cyclic RGD moiety targets and binds to aVb3 integrin which is expressed on the cell membrane of tumor cells and tumor-resident endothelial cells. Upon imaging, aVb3 integrin-expressing cells can be visualized and expression levels can be quantified. This can be used to assess response to anti-angiogenic treatment. aVb3 integrin is overexpressed on certain tumor cells and tumor-resident endothelial cells, while minimally or not expressed on healthy, normal cells; aVb3 integrin plays a key role in angiogenesis, tumor proliferation and survival.
gallium Ga 68-NODAGA-LM3
A radiopharmaceutical agent comprised of LM3, a human somatostatin receptor (SSTR) antagonist, chelated with 1,4,7-triazacyclononane,1-glutaric acid-4,7 acetic acid (NODAGA) and radiolabeled with gallium Ga 68, that may be used as an imaging agent for SSTR-expressing tumor cells upon positron emission tomography (PET). Upon administration of gallium Ga 68 NODAGA-LM3, the LM3 moiety targets and binds to SSTRs that are present on the cell membranes of many types of neuroendocrine tumors (NETs). This allows for visualization of SSTR-positive cells upon PET imaging. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTRs.
gallium Ga 68-NODAGA-ZIGF-1R:4：40
A radiolabeled recombinant insulin-like growth factor 1 receptor (IGF-1R; IGF1R)-specific affibody ligand composed of an IGF1R-targeting protein, the anti-IGF1R affibody ZIGF-1R:4:40 with an acetylated cysteine (Ac-Cys) at the N terminal of the affibody, that is site-specifically conjugated with the chelating agent NODAGA (1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid), and labeled with the radioisotope gallium Ga 68, with potential use for imaging IGF1R-expressing tumor cells upon positron emission tomography (PET). Upon administration of gallium Ga 68-NODAGA-ZIGF-1R:4:40, the ZIGF-1R:4:40 affibody molecule moiety targets and binds to IGF1R expressed on various tumor cell types. Upon PET, IGF1R-expressing tumor cells can be visualized. IGF1R, frequently overexpressed in cancers, plays important roles in cell proliferation, survival, adhesion, migration, and differentiation. The affibody protein scaffold is based on the Z-domain, which is derived from one of the immunoglobulin (Ig) G-binding domains of staphylococcal protein A.
gallium Ga 68-NOTA-3PTATE-RGD
A radiopharmaceutical agent composed of a modified form of the somatostatin analogue octreotate (TATE), linked, via a glutamate linker, to the cyclic tri-amino acid arginine-glycine-aspartic acid (RGD) motif (3PTATE-RGD), and labeled, via the macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) with the radioisotope gallium Ga 68, with potential somatostatin receptor type 2 (SSTR2) and alphaVbeta3 (aVb3) integrin imaging activity upon positron emission topography (PET) or single photon emission computed tomography (SPECT). After intravenous administration, gallium Ga 68-NOTA-3PTATE-RGD simultaneously binds to SSTR, with its TATE moiety (with a preference for SSTR2), and to the integrin receptor aVb3 with its RGD moiety. Both SSTR2 and aVb3 are expressed on the membrane of certain tumor cells while minimally or not expressed on healthy, normal cells. Upon PET imaging, SSTR2- and aVb3 integrin-expressing tumor cells can be visualized and expression levels can be quantified. SSTR2 and aVb3 play key roles in tumor proliferation and survival.
gallium Ga 68-NOTA-Aca-BBN(7-14)
A radioconjugate containing the bombesin (BBN) fragment BBN(7-14) comprised of the amino acid sequence of Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2, which targets the gastrin-releasing peptide receptor (GRPR), bound to aminocaproic acid (Aca), and linked by the macrocyclic chelating agent, 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-Aca-BBN(7-14), the peptide moiety targets and binds to GRPR. Upon PET/CT, GRPR-expressing tumor cells can then be visualized. GRPR, also called bombesin receptor 2 (BB2), is a seven-transmembrane G protein-coupled receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers.
gallium Ga 68-NOTA-AE105
A radiotracer composed of AE105, an urokinase-type plasminogen activator receptor (uPAR) peptide antagonist, conjugated with the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and labeled with the radionuclide gallium Ga 68, with potential imaging activity using positron emission tomography (PET). Upon administration, the AE105 moiety of gallium Ga 68-NOTA-AE105 targets and binds, with high affinity, to uPAR expressed on tumor cells. Upon PET imaging, uPAR-expressing tumor cells can be visualized and the degree of tumor aggressiveness can be assessed. uPAR expression is correlated with increased tumor invasiveness and aggressiveness, as well as a poor prognosis.
gallium Ga 68-NOTA-anti-HER2 nanobody VHH1
A radioconjugate composed of a nanobody directed against human epidermal growth factor receptor 2 (HER2, EGFR2, ERBB2) that is linked, through the macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-anti-HER2 nanobody VHH1, the anti-HER2 antibody moiety targets and binds to HER2-expressing cells. This facilitates both detection of HER2-expressing tumor cells and assessment of responses to HER2-targeted chemotherapeutic agents during PET/CT. HER2, a tyrosine kinase is overexpressed on the cell surfaces of various tumor cell types.
gallium Ga 68-NOTA-anti-MMR-VHH2 nanobody
A radiotracer composed of a nanobody against the macrophage mannose receptor (MMR, CD206) conjugated with the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and labeled with the radionuclide gallium Ga 68, with potential imaging activity using positron emission tomography (PET). Upon administration, the nanobody moiety of gallium Ga 68-NOTA-anti-MMR-VHH2 nanobody binds to MMR on tumor-associated macrophages (TAMs). Upon PET imaging, MMR-expressing TAMs can be visualized. MMR-expressing TAMs play a role in tumor growth and metastasis as well as immunotherapy resistance.
gallium Ga 68-NOTA-BBN-RGD
A radioconjugate containing the bombesin (BBN) fragment BBN(7-14) comprised of the amino acid sequence Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2, which targets the gastrin-releasing peptide receptor (GRPR), and linked, via a glutamate linker, to the cyclic arginine-glycine-aspartic acid (RGD) sequence-based peptide cyclo[Arg-Gly-Asp-D-Tyr-Lys] (c(RGDyK)), which targets integrin alphaVbeta3 (aVb3), and labeled with the radionuclide gallium (Ga) 68 through the macrocyclic chelating agent, 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-BBN(7-14)-RGD, the BBN peptide moiety of the RGD-BBN heterodimer specifically targets and binds to GRPR while the RGD moiety specifically binds to the aVb3. Upon PET/CT, GRPR- and/or aVb3-expressing tumor cells can be visualized and expression levels can be quantified. GRPR, also called bombesin receptor 2 (BB2), is a seven-transmembrane G protein-coupled receptor belonging to the bombesin receptor family. aVb3, an integrin receptor, plays a key role in angiogenesis, tumor proliferation and survival. Both are overexpressed in certain types of cancers.
gallium Ga 68-NOTA-exendin-4
A radiopharmaceutical composed of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 linked by the macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) to the positron-emitting radionuclide gallium Ga 68, with potential imaging activity upon positron emission tomography (PET)/computed tomography (CT). Upon administration of gallium Ga 68-NOTA-exendin-4, the exendin-4 moiety binds to GLP-1R. The radionuclide moiety can be detected using PET/CT and GLP-1R-expressing tumors can be localized. GLP-1R, located on beta cells, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors.
gallium Ga 68-NOTA-FAPI-04
A radioconjugate composed of FAPI-04, a quinoline-based fibroblast activation protein (FAP)-targeted tracer belonging to the group of FAP inhibitors (FAPi), conjugated with the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and labeled with the radionuclide gallium Ga 68, with potential use as a tracer for FAP-expressing cancer-associated fibroblasts (CAFs) during positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-FAPI-04, the FAPI-04 moiety targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing cells can be detected during PET/CT imaging. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
gallium Ga 68-NOTA-hGZP
A radiotracer composed of hGZP, a biotinylated human granzyme B peptide, conjugated with the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and labeled with the radionuclide gallium Ga 68, with potential imaging activity using positron emission tomography (PET). Upon administration, the hGZP moiety of gallium Ga 68-NOTA-hGZP targets and binds to granzyme B, a cytotoxic serine protease released by cytotoxic T lymphocytes (CTLs), in tumors. Upon PET imaging, tumoral granzyme B expression can be visualized, and CTL activation and activity can be assessed.
gallium Ga 68-NOTA-MAL-Cys39-exendin-4
A radiopharmaceutical tracer composed of the glucagon-like peptide-1 receptor (GLP-1R) agonist exendin-4 in which the serine residues (ser39) are replaced with cysteine (cys39) linked by the macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), which is linked to maleimide (MAL), to the positron-emitting radionuclide gallium Ga 68, with potential use in diagnostic imaging upon positron emission tomography (PET)/computed tomography (CT). Upon administration of gallium Ga 68-NOTA-MAL-Cys39-exendin-4, the exendin-4 moiety binds to GLP-1R. The radionuclide moiety can be detected using PET/CT and GLP-1R-expressing tumors can be localized and visualized. GLP-1R, which is located on beta cells and regulates insulin secretion, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors (NETs).
gallium Ga 68-NOTA-NFB
A radioconjugate composed of a derivative of the CXCR4 peptide antagonist T140, in which the N-terminal 4-fluoro-benzoyl group (NFB) is substituted with the chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and radiolabeled with gallium Ga 68, with potential CXCR4 imaging activity during positron emission topography (PET). Upon administration, gallium Ga 68-NOTA-NFB selectively binds to CXCR4 and CXCR4-expressing tumor cells can then be visualized upon PET imaging. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis, and is upregulated in several tumor cell types. CXCR4 expression is correlated with tumor aggressiveness and high metastatic potential. Unmodified T140 binds non-specifically to red blood cells (RBCs); replacing the fluoro-benzoyl group with NOTA (NOTA-NFB) prevents the RBC binding almost entirely, while only minimally reducing the binding to CXCR4-positive tumor cells.
gallium Ga 68-NOTA-RM26
A radioconjugate containing RM26, a synthetic bombesin analogue and antagonist of the gastrin-releasing peptide receptor (GRPR), that is linked, through the macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-RM26, the peptide moiety targets and binds to GRPR. Upon PET/CT, GRPR-expressing tumor cells can then be visualized. GRPR, also called bombesin receptor subtype 2 (BB2), is a G protein-coupled seven-transmembrane receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers.
gallium Ga 68-NOTA-Sgc8
A radioconjugate consisting of Sgc8, a 41 oligonucleotides long single-stranded DNA aptamer and protein tyrosine kinase-7 (PTK7; colon carcinoma kinase-4; CCK4)-targeting ligand, linked via the bi-functional agent 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), to the beta-emitting radioisotope gallium Ga 68, with potential imaging activity during positron emission topography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-Sgc8, the Sgc8 aptamer moiety targets and binds to PTK7 expressed on certain tumor cells. Upon PET/CT imaging, this radioconjugate can be used to detect and quantify PTK7-expressing tumor cells. PTK7, a member of the receptor tyrosine kinase (RTK) superfamily, is overexpressed in many different tumor cell types and plays an important role in tumor cell proliferation, migration and invasion.
gallium Ga 68-NOTA-SNA002
A radiotracer composed of SNA002, a targeting agent for programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), conjugated to the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), and radiolabeled with the radionuclide gallium Ga 68, with potential PD-L1 imaging activity using positron emission tomography (PET). Upon administration of gallium Ga 68-NOTA- SNA002, the SNA002 moiety targets and binds to PD-L1 expressed on certain tumor cells. Upon uptake and PET imaging, the radioisotope moiety can be visualized and the extent of PD-L1 expression can be assessed. SNA002 binds PD-L1 on a different epitope than most PD-L1 inhibitors.
gallium Ga 68-P15-041
A radiotracer composed of a bone targeting agent P15-041 linked to the radioisotope gallium Ga 68, with potential imaging activity upon positron emission tomography (PET)/computed tomography (CT). Upon administration, the P15-041 moiety targets, through an as of yet unknown mechanism of action, a certain target expressed by bone and, upon PET/CT, bone metastases can be imaged.
gallium Ga 68-P16-093
A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting ligand (P16-093) conjugated to the radioisotope gallium Ga 68, via the acyclic radiometal chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'-diacetic acid (HBED-CC), with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68 P16-093, the P16-093 moiety targets and binds to PSMA-expressing tumor cells. During PET imaging, PSMA-expressing tumor cells can be detected. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
gallium Ga 68-pentixafor
A radioconjugate composed of a synthetic, cyclic pentapeptide analog of stromal-cell derived factor-1 (SDF-1 or CXCL12), which is a ligand for chemokine receptor C-X-C chemokine receptor type 4 (CXCR4), that is radiolabeled, via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA), with the radioisotope gallium Ga 68 (Ga68; 68Ga), with potential use for imaging CXCR4-expressing cells upon positron emission tomography (PET)/computed tomography (CT). Upon administration of 68Ga-pentixafor, the pentixafor moiety targets and binds to CXCR4-expressing cancer cells. Upon PET/CT, CXCR4-expressing cancer cells can be visualized and the expression status of the receptor can be assessed. CXCR4, a marker of poorly differentiated cells, is overexpressed on various cancer cells, and plays a key role in tumor growth, progression, invasiveness and metastasis.
gallium Ga 68-PNT6555
A radioconjugate composed of PNT6555, a fibroblast activation protein (FAP)-targeting moiety linked to the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), radiolabeled with gallium Ga 68 (68Ga), with potential use as a tracer for FAP-expressing cancer-associated fibroblasts (CAFs) and FAP-expressing tumor cells during positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-PNT6555, the FAP-targeting moiety targets and binds to FAP-expressing CAFs and tumor cells. Upon binding, FAP-expressing CAFs and tumor cells can be detected during PET/CT imaging. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME) and certain tumor cells.
gallium Ga 68-PSMA-617
A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET)/computed tomography (CT). Upon intravenous administration of 68Ga-PSMA-617, the PSMA-617 moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells can be detected during PET/CT imaging. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
gallium Ga 68-PSMA-R2
A radioconjugate composed of PSMA-R2, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope gallium Ga 68, with potential imaging activity during positron emission topography/computed tomography (PET/CT). Upon administration of gallium Ga 68-PSMA-R2, the PSMA-R2 moiety targets and binds to PSMA-expressing tumor cells. This allows for visualization of PSMA-expressing cells upon imaging. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on the majority of prostate tumor cells.
gallium Ga 68-R10602
A radioconjugate containing a small molecule radioligand targeting an as of yet undisclosed hormone receptor and labeled with the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-R10602, the radioligand moiety targets and binds to the hormone receptor. Upon PET/CT, tumor cells expressing the hormone receptor can then be visualized.
gallium Ga 68-RGD
A radiopharmaceutical agent comprised of a cyclic arginine-glycine-aspartic acid (Arg-Gly-Asp/RGD) peptide labeled with gallium Ga 68, with potential alphaVbeta3 integrin (avb3) imaging activity during positron emission topography (PET). After intravenous administration, gallium Ga 68-RGD selectively binds to avb3 on the cell membrane via the cyclic RGD motif. Upon PET imaging, avb3-expressing tumor cells can be visualized and their expression levels can be quantified. avb3, a member of the integrin receptor family, is overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells; it plays a key role in angiogenesis, tumor proliferation and survival.
gallium Ga 68-THP-PSMA
A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting agent conjugated, via the tris(hydroxypyridinone) (THP) chelator, to the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68-THP-PSMA, the PSMA moiety targets and binds to PSMA-expressing tumor cells. Upon PET imaging, PSMA-expressing tumor cells can be detected. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
gallium Ga 68-VMT02
A radioconjugate composed of the melanocyte-stimulating hormone receptor (MSHR; melanocortin-1 receptor; MC1R; melanin-activating peptide receptor; melanotropin receptor)-targeting moiety, VMT02, labeled with the radioisotope gallium Ga 68, with potential imaging activity using positron emission tomography (PET). Upon administration of gallium Ga 68-VMT02, VMT02 targets and binds to MC1R-expressing tumor cells. Upon PET imaging, MC1R-expressing tumor cells can be detected. MC1R, a G protein-coupled receptor expressed by melanocytes that binds to melanocortins, is involved in regulating mammalian skin and hair color. It is upregulated on the surface of metastatic melanoma cells.
gallium Ga 68-WL12
A radiotracer composed of the programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274)-binding peptide WL12 radiolabeled with the radionuclide gallium Ga 68, with potential PD-L1 imaging activity using positron emission tomography (PET). Upon administration of gallium Ga 68-WL12, the WL12 moiety targets and binds to PD-L1 expressed on certain tumor cells. Upon uptake and PET imaging, the radioisotope moiety can be visualized and the extent of PD-L1 expression can be assessed. This may be used to predict the therapeutic response to PD-L1-targeting agents.
gallium Ga 68/copper Cu 64-labeled FAPI-XT117
A radioconjugate composed of FAPI-XT117, a fibroblast activation protein inhibitor (FAPi), labeled with the radionuclides gallium Ga 68 and copper Cu 64, with potential use as a tracer for FAP-expressing cancer-associated fibroblasts (CAFs) during positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68/copper Cu 64-labeled FAPI-XT117, the FAPI-XT117 moiety targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing cells can be detected during PET/CT imaging. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
gallium Ga-labeled PSMA-11-gadoxetate
A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting ligand, Glu-urea-Lys(Ahx) (Glu-NH-CO-NH-Lys(Ahx)) conjugated to both the paramagnetic contrast enhancer gadoxetate and the radioisotope gallium Ga 68, the latter is conjugated via an acyclic radiometal chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'-diacetic acid (HBED-CC), with potential use as a tracer for PSMA-expressing tumors during magnetic resonance imaging (MRI) and positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68-labeled PSMA-11-gadoxetate, the Glu-urea-Lys(Ahx) moiety targets and binds to PSMA-expressing tumor cells. PSMA-expressing tumor cells can be detected during PET imaging and MRI. The dual imaging capabilities of this agent may improve both visualization of PSMA-expressing tumor cells and tumor assessment. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as on some other tumor cell types.
gallium maltolate
An orally bioavailable form of the element gallium (Ga) composed of a trivalent gallium cation (Ga3+) coordinated to three maltolate ligands, with anti-inflammatory, anti-proliferative, antineoplastic, analgesic, antiresorptive and antibacterial activities. Upon administration of gallium maltolate, Ga3+, which is structurally similar to the ferric ion (Fe3+), competes with and replaces Fe3+ in many vital Fe 3+-mediated biological reactions.. Unlike Fe3+, Ga3+ cannot be reduced, cannot participate in redox reactions and cannot mimic Fe3+ functions. In rapidly proliferating cells, such as cancer cells, high amounts of iron are needed for DNA synthesis. The incorporation of Ga3+ inactivates the Fe3+-dependent enzyme ribonucleotide reductase (RR), an enzyme essential for DNA synthesis, leading to an inhibition of DNA synthesis and induction of cell death in rapidly proliferating cells. Gallium similarly reduces bacterial cell growth. In addition, Ga3+ is able to suppress inflammation through the down-regulation of pro-inflammatory cells and the inhibition of pro-inflammatory cytokine secretion. Gallium also exerts analgesic effects due to the inhibition of Fe3+-dependent enzymes involved in inflammation and may interfere with the activity of certain metalloproteinases and neuropeptides that are implicated in pain. Also, gallium is able to inhibit bone resorption by osteoclasts, may inhibit metastasis to bone and may prevent the destruction of bone by tumors.
gallium nitrate
A hydrated nitrate salt of the group IIIa element gallium with potential use in the treatment of malignancy-associated hypercalcemia. Gallium nitrate localizes preferentially to areas of bone resorption and remodeling and inhibits osteoclast-mediated resorption by enhancing hydroxyapatite crystallization and reduction of bone mineral solubility. This agent also increases calcium and phosphorous deposition into bone and may increase collagen synthesis.
gallium-based bone resorption inhibitor AP-002
An orally bioavailable gallium (Ga)-based small molecule agent with potential anti-bone resorption and antineoplastic activities. Upon oral administration, AP-002 selectively inhibits osteoclast differentiation and bone resorption, and may promote the growth of osteoblasts thereby improving the skeletal sequelae of bony metastases which include pain, spinal cord compression, fractures and hypercalcemia of malignancy. Additionally, AP-002 may, through an as of yet undescribed mechanism of action, directly target and kill bone tumor cells.
galunisertib
An orally available, small molecule antagonist of the tyrosine kinase transforming growth factor-beta (TGF-b) receptor type 1 (TGFBR1), with potential antineoplastic activity. Upon administration, galunisertib specifically targets and binds to the kinase domain of TGFBR1, thereby preventing the activation of TGF-b-mediated signaling pathways. This may inhibit the proliferation of TGF-b-overexpressing tumor cells. Dysregulation of the TGF-b signaling pathway is seen in a number of cancers and is associated with increased cancer cell proliferation, migration, invasion and tumor progression.
gamboge resin extract TSB-9-W1
An orally bioavailable extract from the yellow to brown gum-resin of the gamboge tree (genus Garcinia) belonging to the Clusiaceae (or Guttiferae) family, with potential anti-inflammatory and antineoplastic activities. Gamboge resin extract TSB-9-W1 contains various active ingredients, including gambogic acid, formoxanthone A, betulin, betulinic acid, morellic acid, isomorellic acid, isogambogic acid, isomorellinol and desoxymorellin. Upon oral administration, the various active components of the gamboge resin extract TSB-9-W1 may bind to and inhibit the activity of a variety of cancer-related proteins, may induce apoptosis, and may exert cytotoxic activity on tumor cells, thereby inhibiting tumor cell proliferation. TSB-9 is derived from TSB-14, which is the acetone-extract of gamboge resin, and pulverized into powder form; TSB-9 is 90% extract and 10% brown sugar. TSB-9-W1 is a milled form of TSB-9 with a particle size of 5 micrometers.
Gamifant
(Other name for: emapalumab-lzsg)
Gamimune N
(Other name for: therapeutic immune globulin)
gamitrinib
A resorcinolic-based mitochondrial-targeted heat shock protein 90 (Hsp90) family inhibitor, with potential antineoplastic activity. Upon administration, gamitrinib targets and inhibits the activity of Hsp90 heat shock proteins, such as TNF receptor-associated protein-1 (TRAP1). This induces the accumulation of the mitochondrial kinase PINK1 and the cytosolic E3 ubiquitin (Ub) ligase Parkin, ubiquitylates substrate proteins, and induces PINK1/Parkin-dependent mitophagy. Gamitrinib induces acute mitochondrial dysfunction, loss of membrane potential and membrane rupture leading to the induction of apoptosis in susceptible tumor cells. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins.
gamma-delta tocotrienol
An orally available nutritional supplement containing the gamma and delta forms of the vitamin E family member tocotrienol, with hypocholesterolemic, antithrombotic, antioxidant, and potential antineoplastic activity. Upon oral administration, gamma-delta tocotrienol accumulates in cancer cells and may exert their anti-cancer activity in part through 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase downregulation and/or degradation, cell cycle arrest, and induction of caspase-mediated apoptosis. In addition, this agent may inhibit angiogenesis partially through the blockage of vascular endothelial growth factor receptor (VEGFR) and the inhibition of tumor cell-induced vessel formation. Altogether, this may result in the inhibition of tumor cell growth. Further, this agent prevents free radical formation and inhibits lipid peroxidation. Tocotrienols contain 3 double bonds, absent in tocopherols, on its farnesyl isoprenoid side chain that likely contribute to its anti-cancer activities.
gamma-secretase/Notch signalling pathway inhibitor RO4929097
An orally bioavailable, small-molecule gamma secretase (GS) inhibitor with potential antitumor activity. Gamma secretase inhibitor RO4929097 binds to GS and blocks activation of Notch receptors, which may inhibit tumor cell proliferation. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth.
gamma-tocopherol
The orally bioavailable gamma form of the naturally-occurring fat-soluble vitamin E, found in certain nuts and seeds, with potential antioxidant activity. Although the exact mechanism of action of this tocopherol has yet to be fully identified, gamma-tocopherol appears to have the ability to scavenge free radicals, thereby protecting against oxidative damage.
Gammacorten
(Other name for: dexamethasone)
Gammagard
(Other name for: human immunoglobulin G)
Gammagard S/D
(Other name for: therapeutic immune globulin)
Gammar-P
(Other name for: therapeutic immune globulin)
Gamunex-C
(Other name for: human immunoglobulin G)
ganaxolone
An orally bioavailable synthetic analog of the neuroactive steroid allopregnanolone and positive allosteric modulator of the gamma-aminobutyric acid (GABA)-A receptor, with anxiolytic, sedative, antidepressant and anticonvulsant activities. Upon oral administration, ganaxolone specifically targets and binds to the allosteric sites of the synaptic and extrasynaptic GABA-A receptor-chloride ionophore complex in the central nervous system (CNS). This leads to an increase in the opening of chloride channels, membrane hyperpolarization, increases the inhibitory effect of GABA on the CNS, and inhibits neurotransmission. This blocks seizure propagation and elevates seizure thresholds.
ganciclovir
A synthetic guanine derivative with antiviral activity. As the active metabolite of ganciclovir, ganciclovir-5-triphosphate (ganciclovir-TP) appears to inhibit viral DNA synthesis by competitive inhibition of viral DNA polymerases and incorporation into viral DNA, resulting in eventual termination of viral DNA elongation.
gandotinib
An orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. JAK2V617F has a substitution of phenylalanine for valine at amino acid position 617 and plays a key role in tumor cell proliferation and survival.
ganetespib
A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Ganetespib binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.
Ganite
(Other name for: gallium nitrate)
ganitumab
A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Ganitumab binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R is a tyrosine kinase and a member of the insulin receptor family. IGF-1R activation stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis.
Ganoderma lucidum spores powder capsule
An orally available powder-based nutritional supplement containing the spores of the mushroom Ganoderma lucidum (Ganoderma l.), a traditional Chinese medicine, with potential protective, sedative, anti-oxidant, immunomodulating, and antineoplastic activities. The spores contain various bioactive components including polysaccharides, triterpenoids, peptidoglycans, amino acids, fatty acids, vitamins, and minerals. Upon oral administration of the Ganoderma lucidum spores powder capsule, the active ingredients may modulate the immune system, may activate dendritic cells, natural killer cells, and macrophages and may modulate the production of certain cytokines, such as tumor necrosis factor-alpha (TNFa), interleukin (IL) 1-beta (IL-1b), IL-2, IL-6 and IL-8. This supplement may improve cancer-related fatigue and may be used as a sleep aid; it may also have a beneficial effect on the heart, lung, liver, pancreas, kidney, and the central nervous system.
Gardasil
(Other name for: recombinant human papillomavirus quadrivalent vaccine)
Gardasil 9
(Other name for: recombinant human papillomavirus nonavalent vaccine)
garetatug rezetecan
An antibody-drug conjugate (ADC) composed of garetatug, an immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) Claudin 18.2 (CLDN18.2; A2 isoform of claudin-18) conjugated, via a cleavable linker, to rezetecan, an exatecan derivative and topoisomerase 1 inhibitor, with potential antineoplastic activity. Upon administration of garetatug rezetecan, the anti-CLDN18.2 monoclonal antibody moiety specifically targets and binds to CLDN18.2 expressed on tumor cells. Upon binding, internalization and linker cleavage, rezetecan is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing CLDN18.2. CLDN18.2, a tight junction protein and stomach-specific isoform of claudin-18, is expressed on a variety of tumor cells. Its expression in healthy tissues is strictly confined to short-lived differentiated epithelial cells of the gastric mucosa.
garlic
A bulbous herb isolated from the plant Allium sativum with potential antineoplastic activity. Garlic contains a number of different organosulfur compounds, some of which have displayed antineoplastic activity.
garlic extract
The alcoholic extract of the bulb or whole garlic plant Allium sativum (Liliaceae) with potential antineoplastic activity. The garlic plant has long been considered a beneficial plant for health and has been used as an antihelmintic, a rubefacient, an anti-infective, and an antihypertensive. Fresh or aged, garlic extracts contain compounds such as diallyl and allyl propyl disulfides with potent antioxidant, cholesterol-lowering properties; regular ingestion may be preventative for atherosclerosis and cardiovascular diseases.
garsorasib
An orally available inhibitor of the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration, garsorasib selectively targets the KRAS G12C mutant and inhibits KRAS G12C mutant-dependent signaling. KRAS, a member of the RAS family of oncogenes, serves an important role in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.
Gastrimmune
(Other name for: gastrin immunotoxin)
gastrin immunotoxin
An immunotoxin containing an epitope of human gastrin conjugated to diphtheria toxin, with antineoplastic activity. The gastrin epitope in this vaccine is chemically identical or similar to the endogenous gastrin-17 (G-17), a 17-amino acid peptide hormone that stimulates secretion of gastric acid by the stomach. Diphtheria toxin inhibits protein synthesis via modifying translation elongation factor 2 (EF-2). Vaccination with this immunotoxin may elicit production of antibodies against gastrinoma cells overexpressing gastrin, in addition to the toxic effects on protein synthesis exerted by the diphtheria toxin moiety.
GastroMARK
(Other name for: ferumoxsil oral suspension)
gataparsen sodium
A second-generation antisense oligonucleotide directed against survivin mRNA with potential antitumor activity. Gataparsen sodium hybridizes to survivin mRNA, thereby blocking translation of survivin protein, a member of the inhibitor of apoptosis (IAP) family. Silencing the expression of survivin may result in the restoration of the apoptotic process in tumor cells, facilitating chemotherapeutic treatment. Survivin, expressed during embryonal development, is upregulated in a variety of human cancers while absent in most normal adult cells; its expression in tumors is associated with a more aggressive phenotype, shorter survival times, and a decreased response to chemotherapy.
gatipotuzumab
A humanized monoclonal antibody recognizing the tumor-specific epitope of mucin-1 (TA-MUC1), with potential antineoplastic activity. Gatipotuzumab targets and binds to the TA-MUC1 epitopes expressed on the cell surface of tumor cells, thereby potentially activating the immune system to induce an antibody-dependent cellular cytotoxicity (ADCC) against the TA-MUC1-expressing tumor cells. TA-MUC1 is designated to MUC1 epitopes with O-glycosylated carbohydrate-induced conformational structures that are tumor-specific, thereby enabling gatipotuzumab to differentiate between tumor MUC1 and non-tumor MUC1 epitopes.
gavilimomab
A murine IgM monoclonal antibody (MoAb) developed for the potential treatment of graft versus host disease (GvHD). Gavilimomab recognizes human CD147 antigen, weakly expressed on human leukocytes and up-regulated on activated lymphocytes. This MoAb is capable of neutralizing inflammatory reactions via a complement-dependent cytotoxic mechanism. However, gavilimomab does not offer an improvement over antithymocyte globulin in the treatment of acute steroid resistant GVHD.
gavocabtagene autoleucel
A preparation of autologous T lymphocytes that have been genetically engineered to express a single-domain antibody that recognizes human mesothelin, fused to the N-terminus of the CD3-epsilon T-cell receptor (TCR) subunit which, upon expression is incorporated into the endogenous TCR complex, with potential antineoplastic activity. Upon administration, gavocabtagene autoleucel specifically target and bind to mesothelin-expressing tumor cells. This leads to T-cell activation and T-cell mediated lysis of mesothelin-expressing tumor cells. Mesothelin, a cell surface glycoprotein involved in cell adhesion, is overexpressed in a variety of cancer cell types. Compared to chimeric antigen receptor (CAR) T cells, TRuCs may be associated with less pro-inflammatory cytokine secretion and fewer adverse effects without compromising therapeutic efficacy.
Gavreto
(Other name for: pralsetinib)
Gazyva
(Other name for: obinutuzumab)
GBM antigens and alloantigens immunotherapeutic vaccine
An orally bioavailable, immunotherapeutic vaccine composed of hydrolyzed and formulated glioblastoma multiforme (GBM) antigens and alloantigens derived from a pool of patients’ cancer cells in the blood and samples of tumor tissues, with potential immunomodulating and antineoplastic activities. Upon oral administration of the GBM antigens and alloantigens immunotherapeutic vaccine, the GBM antigens and alloantigens may stimulate the host immune system via antigen-presenting cells (APCs) lining the gut to mount an immune response against tumor cells expressing these antigens. This may lead to tumor cell death.
GCN2 inhibitor APL-4098
An orally bioavailable inhibitor of the serine/threonine protein kinase general control nonderepressible 2 (GCN2; eukaryotic translation initiation factor 2-alpha kinase 4; GCN2 EIF2alpha kinase; eIF-2-alpha kinase GCN2), with potential antineoplastic and immunomodulating activities. Upon oral administration, GCN2 inhibitor APL-4098 specifically targets, binds to and inhibits the activity of GCN2. This prevents GCN2-mediated signaling and may induce apoptosis in tumor cells that rely on GCN2 signaling for survival. In addition, as GCN2 signaling reduces anti-tumor immunity, preventing GCN2 signaling may enhance anti-tumor immune responses. GCN2 plays a key role in the activation of the integrated stress response (ISR) pathway in response to amino acid deprivation and in hypoxic tumors.
GCN2 modulator HC-7366-K
An immediate release (IR) capsule formulation of the potassium salt monohydrate form of HC-7366, a modulator of the serine/threonine protein kinase general control nonderepressible 2 (GCN2), with potential antineoplastic and immunomodulating activities. Upon oral administration, the base moiety HC-7366 of the GCN2 modulator HC-7366-K targets and binds to GCN2. This prevents GCN2 activity and GCN2-mediated signaling. This may induce apoptosis in tumor cells that rely on GCN2 signaling for survival. In addition, as GCN2 signaling reduces anti-tumor immunity, preventing GCN2 signaling may enhance anti-tumor immune responses. GCN2 plays a key role in the activation of the integrated stress response (ISR) pathway in response to amino acid deprivation and in hypoxic tumors.
GD2 lactone/GD3 lactone-KLH conjugate bivalent vaccine
A cancer vaccine, containing epitopes of the gangliosides GD2 and GD3 conjugated with the immunostimulant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with GD2 lactone/GD3 lactone-KLH conjugate bivalent vaccine may elicit antibodies against tumor cells expressing either epitope, resulting in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC). Located primarily in the nervous system, gangliosides, such as GD2 and GD3, are cell membrane components involved in cellular recognition and cell-cell communication.
GD2-CAR-expressing autologous T-lymphocytes
Genetically modified, autologous T-lymphocytes transduced with a retroviral vector encoding a 14g2a.zeta chimeric antigen receptor (CAR) directed against the disialoganglioside GD2, with potential immunomodulating and antineoplastic activities. Upon intravenous administration, the activated T-lymphocytes target the GD2 antigen on tumor cells and selectively kill those cells. The tumor-associated antigen GD2 is overexpressed on the surface of almost all tumors of neuroectodermal origin.
gebasaxturev
A preparation of naturally occurring, oncolytic enterovirus, with potential antineoplastic activity. Upon administration, gebasaxturev targets and binds to intracellular adhesion molecule 1 (ICAM-1) and decay acceleration factor (DAF), both cell surface molecules that are overexpressed on certain malignant cells. After entering the cells, gebasaxturev replicates in these cancer cells, thereby causing cancer cell lysis. This results in a reduction of tumor cell growth.
gedatolisib
An agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Upon intravenous administration, gedatolisib inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K.
gefitinib
An anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis.
gefurulimab
A humanized bispecific VHH antibody directed against terminal complement protein C5 and albumin, with potential anti-inflammatory and immunomodulatory activities. Upon administration, gefurulimab, with its anti-C5 antibody moiety, targets and binds to terminal complement protein C5, thereby blocking the terminal complement pathway of complement activation. This inhibits complement-mediated inflammation and cell lysis. Excessive complement activation plays a key role in various inflammatory and autoimmune diseases, and leads to tissue destruction. The binding of gefurulimab to albumin, with its albumin binding domain, increases its half-life.
Gelclair
(Other name for: polyvinylpyrrolidone-sodium hyaluronate gel)
Gelfoam
(Other name for: absorbable gelatin sponge)
Gelnique
(Other name for: oxybutynin chloride)
gelonin
A class I ribosome-inactivating protein (RIP) and toxin derived from the seeds of the plant Gelonium multiflorum. Gelonin (rGel) exerts N-glycosidase activity on the 28S ribosomal RNA (rRNA) unit of eukaryotic ribosomes by cleaving out adenine at the 4324 site, which depurinates rRNA, inactivates ribosomes, inhibits protein synthesis, and results in cell death. Used as the toxin moiety of certain immunotoxins and linked to antibodies specific for a tumor-associated antigen (TAA), gelonin can be targeted to and induce specific cytotoxicity in tumor cells expressing the TAA.
GEM640
(Other name for: AEG35156)
gemcitabine 5'-elaidic acid ester
A lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. Due to its lipophilicity, gemcitabine 5'-elaidic acid ester exhibits an increased cellular uptake and accumulation, resulting in an increased conversion to active metabolites, compared to gemcitabine. In addition, this formulation of gemcitabine may be less susceptible to deamination and deactivation by deoxycytidine deaminase.
gemcitabine hydrochloride
The hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
gemcitabine hydrochloride emulsion
An orally available nanoparticle-based formulation containing the hydrochloride salt form of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue, with antineoplastic activity. The formulation consists of an oil-in-water emulsion in which gemicitabine is solubilized in the excipient matrix containing a mixture of oil and (co)surfactants. Upon oral administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA, resulting in premature termination of DNA replication and the induction of apoptosis. Further, dFdCDP inhibits ribonucleotide reductase and reduces the deoxynucleotide pool available for DNA synthesis. Compared to gemcitabine alone, the emulsion allows for increased oral bioavailability and decreases its susceptibility to deamination and deactivation by cytidine deaminase.
gemcitabine liposome FF-10832
A liposomal formulation in which gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue, is encapsulated in liposomes, with potential antineoplastic activity. Upon administration of gemcitabine liposome FF-10832, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA, resulting in premature termination of DNA replication and the induction of tumor cell apoptosis. In addition, dFdCDP inhibits ribonucleotide reductase (RNR) and reduces the deoxynucleotide pool available for DNA synthesis. This inhibits tumor cell proliferation.
gemcitabine prodrug LY2334737
An orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity. Upon administration, gemcitabine prodrug LY2334737 is hydrolyzed by carboxylesterase 2 (CES2) and releases gemcitabine systemically over a period of time consistent with formation rate-limited kinetics. In turn, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate and triphosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP is incorporated into DNA, resulting in premature termination of DNA replication and eventually the induction of apoptosis. Compared to gemcitabine, this prodrug is able to avoid hydrolysis in enterocytes and the portal circulation thus avoiding first pass metabolism and increasing systemic gemcitabine availability. In addition, the slow release of gemcitabine may enhance efficacy while lowering toxicity. CES2, a serine ester hydrolase, is expressed in certain tumors which may allow for increased conversion of gemcitabine at the tumor site, thus increasing cytotoxicity.
gemcitabine-erlotinib regimen
A first-line chemotherapy regimen consisting of gemcitabine and erlotinib used for the treatment of locally advanced and metastatic pancreatic cancer.
gemcitabine-oxaliplatin regimen
A regimen consisting of gemcitabine and oxaliplatin used for the treatment of biliary adenocarcinoma, pancreatic cancer, hepatocellular cancer, and testicular cancer. This regimen is currently being studied in a variety of other cancers.
gemcitabine-releasing intravesical system
A controlled-release intravesical system consisting of a small flexible tube-like device with a solid core composed of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue, with antineoplastic activity. Upon placement of the gemcitabine-releasing intravesical system (GemRIS) into the bladder, gemcitabine is gradually and continuously released from the system over an extended period of time before being removed from the bladder. Upon release, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA, resulting in premature termination of DNA replication and the induction of apoptosis of bladder tumor cells. In addition, dFdCDP inhibits ribonucleotide reductase (RNR) and reduces the deoxynucleotide pool available for DNA synthesis.
gemfibrozil
A fibric acid derivative with hypolipidemic effects. Gemfibrozil interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III results in subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).
gemigliptin
An orally bioavailable inhibitor of the serine protease dipeptidyl peptidase 4 (DPP-4), with hypoglycemic and potential renoprotective activities. Upon administration, gemigliptin binds to DPP-4 and inhibits the breakdown of the incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This prolongs incretin activity, increases postprandial insulin secretion from pancreatic beta cells, decreases glucagon secretion, delays gastric emptying and lowers blood glucose levels. In addition, gemigliptin exerts a renoprotective effect, probably through enhanced GLP-1 signaling, may prevent apoptosis and acute kidney injury induced by nephrotoxic agents, and may protect against diabetic nephropathy.
gemogenovatucel-T
Autologous tumor cells transfected with a plasmid expressing recombinant human granulocyte macrophage-colony stimulating factor (rhGM-CSF) and bifunctional short hairpin RNA (bi-shRNA) against furin, with potential immunostimulatory and antineoplastic activities. Upon intradermal vaccination of gemogenovatucel-T, the expressed GM-CSF protein, a potent stimulator of the immune system, recruits immune effectors to the site of injection and promotes antigen presentation. The furin bifunctional shRNA blocks furin protein production. Decreased levels of furin lead to a reduction in the conversion of transforming growth factor (TGF) beta into TGF beta1 and beta2 protein isoforms. In turn, as part of the negative feedback mechanism, reduced furin protein levels inhibit TGFbeta1 and TGFbeta2 gene expression, thereby further decreasing TGF levels. As TGFs are potent immunosuppressive cytokines, reducing their levels may activate the immune system locally and this may eventually cause a cytotoxic T-lymphocyte (CTL) response against the tumor cells.
GemRIS
(Other name for: gemcitabine-releasing intravesical system)
gemtuzumab ozogamicin
A recombinant, humanized anti-CD33 monoclonal antibody attached to the cytotoxic antitumor antibiotic calicheamicin. In this conjugate, the antibody binds to and is internalized by tumor cells expressing CD33 antigen (a sialic acid-dependent glycoprotein commonly found on the surface of leukemic blasts), thereby delivering the attached calicheamicin to CD33-expressing tumor cells. Calicheamicin binds to the minor groove of DNA, causing double strand DNA breaks and resulting in inhibition of DNA synthesis.
Gemzar
(Other name for: gemcitabine hydrochloride)
Genasense
(Other name for: oblimersen sodium)
Gencept
(Other name for: ethinyl estradiol/norethindrone)
gene-edited autologous neoantigen-targeted NeoTCR-P1 T cells
A preparation of autologous CD4- and CD8-positive T lymphocytes that have been engineered with site-specific nucleases to suppress the expression of most endogenous forms of the T-cell receptor (TCR) and promote expression of a single, native TCR targeting a neoepitope that is presented on the surface of a patient's tumor cells, with potential immunostimulating and antineoplastic activities. Upon reintroduction into the patient, the gene-edited autologous neoantigen-targeted NeoTCR-P1 T cells recognize and bind to tumor cells expressing the targeted neoantigen, resulting in a cytotoxic T-lymphocyte (CTL)-mediated immune response against the patient's tumor cells.
gene-modified HIV-protected hematopoietic stem cells
Autologous hematopoietic stem cells (HSCs) genetically modified to be resistant to infection by human immunodeficiency virus (HIV). Allogeneic human autologous HSCs are isolated and transduced ex vivo with three different anti-HIV genes. Upon infusion into the HIV-infected lymphoma patient, the gene-modified HIV-protected HSCs are resistant to HIV entry and replication thereby preventing HIV infection in these proliferating stem cells and any differentiated cells that they give rise to. This results in the formation of immune cells resistant to HIV which also may be able to destroy HIV-infected cells.
genetically modified interleukin-12 transgene-encoding Bifidobacterium longum
A live, genetically modified probiotic bacteria Bifidobacterium longum (B. longum) engineered to deliver genetic material encoding the human pro-inflammatory transgene interleukin-12 (IL-12), with potential immunoactivating activity. Upon administration of genetically modified IL-12 transgene-encoding B. longum, the bacteria selectively colonize hypoxic tumor tissues and deliver plasmid DNA encoding the IL-12 transgene within the tumor microenvironment (TME). IL-12 is translated in cells and activates the immune system by promoting the activation of natural killer cells (NK cells), inducing secretion of interferon-gamma and promoting cytotoxic T-cell responses against tumor cells. This may result in both immune-mediated tumor cell death and the inhibition of tumor cell proliferation.
genetically-modified anti-HER2-CAR-CD28zeta-expressing allogeneic NK-92/5.28.z cells
A preparation of genetically-modified natural killer (NK) cells derived from the allogeneic NK-92 cell line that are transduced with a lentiviral vector expressing a codon-optimized chimeric antigen receptor (CAR) consisting of a single chain variable fragment (scFv) of the anti-human epidermal growth factor 2 (HER2; ErbB2) monoclonal antibody FRP5, and fused, via hinge and transmembrane regions, to the intracellular domain of the costimulatory molecule CD28, and the intracellular signaling domain of the T-cell antigen receptor complex zeta chain (CD3-zeta), with potential cytolytic, immunomodulating and antineoplastic activities. Upon infusion of the genetically modified anti-HER2-CAR-CD28zeta-expressing allogeneic NK-92/5.28.z cells, the NK cells recognize and bind to HER2 expressed on tumor cells. This leads to the secretion and release of perforins, granzymes, cytokines and chemokines, which results in selective tumor cell lysis in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase (RTK) mutated or overexpressed in many tumor cell types, plays a significant role in tumor cell proliferation and tumor vascularization. The NK-92 cells are derived from a human cytotoxic cell line composed of allogeneic, activated, interleukin-2-(IL-2) dependent-NK cells from a 50-year old male patient with rapidly progressive non-Hodgkin lymphoma. As NK-92 cells are devoid of killer inhibitory receptors (KIRs; also called killer cell immunoglobulin-like receptors), which are negative regulators of NK cell activity, cancer cells are unable to suppress the cancer cell killing ability of the NK-92 cells.
genetically-modified MAGE-A3-expressing MG1 Maraba virus vaccine
A vaccine consisting of the attenuated, genetically-modified, oncolytic form of the Maraba virus, MG1, which has been engineered to express a gene encoding the cancer testis antigen melanoma antigen family A3 (MAGE-A3), with potential antineoplastic activity. Upon administration of genetically-modified MAGE-A3-expressing MG1 Maraba virus vaccine, the attenuated Maraba virus selectively and rapidly replicates in cancer cells; however, it is unable to replicate in normal, healthy cells. This induces a selective Maraba virus-mediated cytotoxicity in those cancer cells, and leads to cancer cell lysis. In addition, the expression of MAGE-A3 further stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing MAGE-A3. The tumor-associated antigen MAGE-A3 is overexpressed by a variety of cancer cell types. The attenuated virus is a double mutant strain with single amino acid substitutions occurring in both G protein (Q242R) and M protein (L123W).
Genexol-PM
(Other name for: paclitaxel polymeric micelle formulation NANT-008)
Gengraf
(Other name for: cyclosporine)
genistein
A soy-derived isoflavone and phytoestrogen with antineoplastic activity. Genistein binds to and inhibits protein-tyrosine kinase, thereby disrupting signal transduction and inducing cell differentiation. This agent also inhibits topoisomerase-II, leading to DNA fragmentation and apoptosis, and induces G2/M cell cycle arrest. Genistein exhibits antioxidant, antiangiogenic, and immunosuppressive activities.
genolimzumab
An immunoglobulin G4 (IgG4) humanized monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1; PD1; PDCD1; CD279), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, genolimzumab binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands programmed cell death-1 ligand 1 (PD-L1) or 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
Genotropin
(Other name for: somatotropin)
gentuximab
A recombinant, humanized monoclonal antibody directed against the vascular endothelial growth factor receptor 2 (VEGFR-2), with potential anti-angiogenic and antineoplastic activities. Upon intravenous injection, gentuximab specifically binds to VEGFR-2, preventing the binding of its ligand, vascular endothelial growth factor (VEGF). Inhibition of VEGFR-2 signaling may potentially inhibit tumor angiogenesis and decrease nutrient supply to tumor cells, resulting in tumor cell death. VEGFR-2 is a type V receptor tyrosine kinase (RTK) expressed on endothelial cells and some tumor cells that regulates endothelial migration and proliferation.
Geopen
(Other name for: carbenicillin)
geranylgeranyltransferase I inhibitor
A substance that inhibits protein geranylgeranyltransferase type 1 (GGTase-I), with potential antineoplastic activity. GGTase-I is involved in the posttranslational modification of a number of oncogenic GTPases, including K-Ras, N-Ras, RhoA, RhoC, Cdc42, RalA, RalB and Rac1. Inhibition of the prenylation of these oncogenic proteins inhibits both their oncogenic activity and membrane localization. This may result in cell cycle arrest and apoptosis. Protein geranylgeranylation, catayzed by GGTase-I, plays a critical role in malignant transformation and cancer cell proliferation, migration and invasion.
gevokizumab
An IgG2 humanized monoclonal antibody against the pro-inflammatory cytokine interleukin 1 beta (IL-1b) with anti-inflammatory activity. Gevokizumab binds to IL-1b, thereby preventing IL-1b-mediated inflammatory responses. This antibody has a long half life and allows for once a month dosing intervals.
ghrelin peptide analogue
A ghrelin peptide analogue with potential anti-cachexia activity. Upon subcutaneous administration, ghrelin peptide analogue binds to and stimulates the G protein-coupled growth hormone secretagogue receptor (GHSR) in the central nervous system (CNS), thereby mimicking the appetite-stimulating and growth hormone-releasing effects of endogenous ghrelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play direct roles in cancer-related loss of appetite. Ghrelin, naturally secreted by gastric endocrine cells, is a 28 amino acid peptide and an endogenous ligand for GHSR.
GI-4000 vaccine
A vaccine containing a heat-killed recombinant Saccharomyces cerevisiae yeast transfected with mutated forms of Ras, an oncogene frequently found in solid tumors, with potential immunostimulant and antitumor activity. Upon administration, GI-4000 vaccine elicits an immune response by stimulating a specific cytotoxic T-cell response against the mutated forms of Ras. This may lead to a destruction of cancer cells expressing a Ras mutation.
Gilotrif
(Other name for: afatinib dimaleate)
gilteritinib
An orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-like tyrosine kinase 3 (FLT3; STK1; FLK2), AXL (UFO; JTK11), anaplastic lymphoma kinase (ALK; CD246), and leukocyte receptor tyrosine kinase (LTK), with potential antineoplastic activity. Upon administration, gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL, ALK and LTK. This may result in an inhibition of FLT3-, AXL-, ALK-, and LTK-mediated signal transduction pathways and reduced proliferation in cancer cells that overexpress these RTKs. FLT3, AXL, ALK, and LTK, which are overexpressed or mutated in a variety of cancer cell types, play key roles in tumor cell growth and survival.
gilteritinib fumarate
The fumarate salt form of gilteritinib, an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-like tyrosine kinase 3 (FLT3; STK1; FLK2), AXL (UFO; JTK11), anaplastic lymphoma kinase (ALK; CD246), and leukocyte receptor tyrosine kinase (LTK), with potential antineoplastic activity. Upon administration, gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL, ALK and LTK. This may result in an inhibition of FLT3-, AXL-, ALK-, and LTK-mediated signal transduction pathways and reduced proliferation in cancer cells that overexpress these RTKs. FLT3, AXL, ALK, and LTK, which are overexpressed or mutated in a variety of cancer cell types, play key roles in tumor cell growth and survival.
gimatecan
An orally bioavailable, semi-synthetic lipophilic analogue of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic and antiangiogenic activities. Gimatecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Although the mechanism of its antiangiogenic activity has yet to be full elucidated, this agent may inhibit endothelial cell migration, tumor neovascularization, and the expression of proangiogenic basic fibroblast growth factor (bFGF).
gimeracil
A pyridine derivative with antitumor activity. Gimeracil enhances the antitumor activity of fluoropyrimidines by competitively and reversibly inhibiting the enzyme dihydropyrimidine dehydrogenase causing decreased degradation of the fluoropyrimidines.
ginger extract
An extract of the rhizome of the perennial plant Zingiber officinale with potential antineoplastic activity. Ginger extract contains a number of different phenolic compounds, some of which have displayed antineoplastic, anti-inflammatory, and antioxidant activities. This agent also exhibits antiemetic properties.
ginseng compound
A compound containing the traditional Chinese medicine (TCM) ginseng, a herb belonging to the Araliaceae family, with potential antioxidant, chemopreventive, anti-inflammatory and antineoplastic activities. Upon administration of the ginseng compound, the active ingredients, mainly ginsenosides, inhibit various signal transduction pathways that play key roles in carcinogenesis and inflammation. This leads to the induction of apoptosis in and inhibits proliferation of tumor cells. In addition, ginsenosides enhance the activity of various antioxidant enzymes, induce nitric oxide (NO) formation, inhibit the formation of reactive oxygen species (ROS) and protect against free radical-induced DNA damage. Ginseng also modulates various components of the immune system, including the activation of dendritic cells (DCs).
ginseng/lingzhi mushroom/Cordyceps sinensis/rose oral liquid
An orally available supplement containing ginseng, lingzhi mushroom, Cordyceps sinensis, and rose with potential immunostimulating activities. Upon oral administration, ginseng/lingzhi mushroom/Cordyceps sinensis/rose oral liquid may, through a not yet elucidated mechanism, enhance immune responses and relieve fatigue.
ginsenoside Rg3 capsule
A capsule containing the steroidal saponin ginsenoside Rg3 isolated from the root of Panax ginseng, with potential cancer preventive and anti-angiogenic activities. Upon oral administration, ginsenoside Rg3 appears to inhibit endothelial cell proliferation, migration and tubular formation, and promotes cancer cell apoptosis. This agent also modulates the activities of certain growth factors, such as vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), and matrix metalloproteinases (MMPs), on tumor angiogenesis. In addition, ginsenoside Rg3 may be able to sensitize cancer cells to some chemotherapeutic agents.
ginsenosides supplement
An oral and herbal supplement containing sixteen ginsenosides derived from ginseng and including the ginsenoside monomers Rg3(R, S), Rh1(S, R), Rh2(R, S), Rk1, Rk3, Rg5, Rh3, Rh4, Rk2, aPPD(S, R) and aPPT(S, R), that may potentially be used to reduce fatigue. Ginseng contains a complex mixture of ginsenosides, and ginsenosides may have different mechanisms of actions and pharmacological activities due to their structural differences. They may have anti-inflammatory, antioxidant, and cortisol-modulating activities, modulate various metabolic pathways, and are believed to act on the central nervous system (CNS), which may enhance vital energy and result in anti-fatigue effects.
Gintemetostat
An orally available small molecule inhibitor of the histone-lysine N-methyltransferase nuclear receptor-binding SET domain protein 2 (NSD2; MMSET; WHSC1), with potential antineoplastic activity. Upon oral administration, gintemetostat selectively targets and binds to NSD2, and inhibits its catalytic activity and the mono- and di-methylation of histone H3 lysine 36 (H3K36). This modulates the expression of genes involved in cellular processes including cellular proliferation, which may lead to decreased growth of cancer cells. NSD2, a member of the NSD family of histone lysine methyltransferase enzymes that catalyzes the mono- and di-methylation of H3K36, is overexpressed and dysregulated in many types of cancers.
giredestrant
An orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, giredestrant specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells.
girentuximab
A chimeric monoclonal antibody directed against G250, a cell surface antigen found in the majority of renal cell carcinomas. Following binding, girentuximab may be internalized by G250 antigen-expressing renal carcinoma cells; mAb G250 may be useful as a carrier for radioisotopes and other antineoplastic therapeutic agents.
GITRL RNA-transfected autologous dendritic cell vaccine
An autologous dendritic cell (DC) cancer vaccine with potential immunostimulatory activity. GITRL RNA-transfected autologous DC vaccine is prepared by transfecting DCs with RNAs encoding tumor necrosis factor (ligand) superfamily, member 18 (TNFSF18 or GlTRL); expression of GlTRL results in modulating T lymphocyte survival in peripheral tissues. Co-vaccination of this vaccine with melanoma antigen specific vaccine may eliminate the adverse effects associated with systemic administration of immune modulators, while also enhancing vaccine-induced immune responses.
givinostat
An orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Givinostat inhibits class I and class II HDACs, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. Givinostat has also been shown to activate the intrinsic apoptotic pathway, inducing apoptosis in hepatoma cells and leukemic cells. This agent may also exhibit anti-angiogenic activity, inhibiting the production of angiogenic factors such as IL-6 and vascular endothelial cell growth factor (VEGF) by bone marrow stromal cells.
givosiran
A proprietary enhanced stabilization chemistry (ESC)-stabilized conjugate composed of the liver-targeted ligand N-acetylgalactosamine (GalNAc) conjugated to small-interfering RNAs (siRNAs) directed against the liver-expressed enzyme aminolevulinic acid synthase 1 (delta-aminolevulinate synthase 1; ALAS1; ALAS-1) that can potentially be used in the treatment of acute hepatic porphyrias (AHPs). Upon subcutaneous administration of givosiran, the GalNAc moiety targets and binds with high affinity to asialoglycoprotein receptors (ASGPRs) expressed on hepatocytes. Once inside the cell, the siRNAs bind to and silence ALAS1 mRNA and inhibit both the translation and expression of the ALAS1 protein. This prevents delta-aminolevulinic acid (ALA) formation, decreases 5-ALA levels and prevents the production of porphyrins and hemes, such as porphobilinogen (PBG). AHPs are a group of metabolic disorders caused by deficiencies of specific enzymes that are responsible for hemoglobulin biosynthesis within the liver, which leads to the accumulation of toxic intermediates, such as ALA and PBG. ALAS1, a liver-expressed, rate-limiting enzyme in the heme biosynthesis pathway, is responsible for the formation of ALA from succinyl-CoA and glycine. ESC enables the subcutaneous dosing of givosiran with increased efficacy, durability and a wide therapeutic index as compared to non-ESC GalNAc-siRNA conjugates.
glasdegib maleate
The maleate salt form of glasdegib, an orally bioavailable small-molecule, smoothened (SMO) receptor inhibitor, with potential antineoplastic activity. Upon oral administration, glasdegib targets, binds to and inhibits the activity of SMO. This inhibits the activity of the Hedgehog (Hh) signaling pathway and inhibits the growth of tumor cells in which this pathway is aberrantly activated. SMO, a transmembrane protein, is involved in Hh signal transduction. The Hh signaling pathway plays an important role in cellular growth, differentiation, repair, and cancer stem cell (CSC) survival. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies and is associated with uncontrolled cellular proliferation in a variety of cancers.
Glassia
(Other name for: alpha-1-proteinase inhibitor human)
glecaprevir/pibrentasvir
A fixed dose combination of glecaprevir, an inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease, and pibrentasvir, an inhibitor of the HCV non-structural protein 5A (NS5A), with activity against HCV genotypes 1-6. Upon oral administration of glecaprevir/pibrentasvir, glecaprevir inhibits the HCV NS3/4A serine protease enzyme, thereby disrupting the cleavage of the virally encoded polyprotein into mature proteins and preventing the formation of the viral replication complex. Pibrentasvir inhibits the activity of the NS5A protein, leading to disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of certain cancers.
glecirasib
An orally available inhibitor of the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration, glecirasib selectively targets, binds to and inhibits the activity of the KRAS G12C mutant, thereby inhibiting KRAS G12C mutant-dependent signaling. KRAS, a member of the RAS family of oncogenes, serves an important role in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.
Gleevec
(Other name for: imatinib mesylate)
glembatumumab vedotin
An antibody-drug conjugate, consisting of the fully human monoclonal antibody CR011 directed against glycoprotein NMB (GPNMB) and conjugated via a cathepsin B-sensitive valine-citrulline (vc) linkage to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the monoclonal antibody CR011 moiety binds to glycoprotein nmb (GPNMB), expressed on the surfaces of a variety of cancer cell types; upon endocytosis, the synthetic dolastin analogue MMAE is released via enzymatic cleavage into the tumor cell cytosol, where it binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and apoptosis. The vc linkage system is highly stable in serum, rendering the cytotoxicity of glembatumumab vedotin specific for GPNMB-positive cells. GPNMB is a transmembrane protein overexpressed on the surfaces of various cancer cell types, including melanoma, breast, and prostate cancer cells.
Gleolan
(Other name for: oral aminolevulinic acid hydrochloride)
Gleostine
(Other name for: lomustine)
glesatinib
An orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. Glesatinib binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON). Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs.
Gliadel Wafer
(Other name for: carmustine implant)
Gliadel Wafers
(Other name for: carmustine implant)
GliAtak
(Other name for: aglatimagene besadenovec)
gliclazide
A short-acting, relatively high-potency, second-generation sulfonylurea compound with hypoglycemic activity. Gliclazide also increases peripheral insulin sensitivity. This agent is metabolized by CYP2C9.
glimepiride
A long-acting, third-generation sulfonylurea with hypoglycemic activity. Compared to other generations of sulfonylurea compounds, glimepiride is very potent and has a longer duration of action. This agent is metabolized by CYP2C9 and shows peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity.
glioblastoma cancer vaccine ERC1671
A cancer vaccine composed of a combination of autologous glioblastoma (GBM) tumor cells, allogeneic GBM tumor cells, generated from three different GBM donor cancer patients, and the lysates of all of these cells, with potential antineoplastic activity. Upon intradermal administration of GBM cancer vaccine ERC1671, the mixture of the autologous and allogeneic cells and lysates stimulates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GBM-associated antigens, which leads to the destruction of glioblastoma cells.
glioblastoma multiforme multipeptide vaccine IMA950
A cancer vaccine comprising 11 peptides associated with glioblastoma multiforme (GBM), with potential immunomodulating and antineoplastic activities. Vaccination with glioblastoma multiforme multi-antigen vaccine IMA950 stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response as well as a T-helper (Th) immune response against tumor cells expressing these peptides, potentially resulting in decreased tumor growth of GBM. Peptides in IMA950 comprise the following: brevican (BCAN); chondroitin sulfate proteoglycan 4 (CSPG4); fatty acid binding protein 7, brain (FABP7); insulin-like growth factor 2 mRNA binding protein 3 (IGF2BP3); neuroligin 4, X-linked (NLGN4X); neuronal cell adhesion molecule (NRCAM); protein tyrosine phosphatase, receptor-type, Z polypeptide 1 ( PTPRZ1); tenascin C (TNC); Met proto-oncogene (MET); baculoviral IAP repeat-containing 5 (BIRC5); and hepatitis B virus core antigen.
glioma lysate vaccine GBM6-AD
An allogeneic cell lysate-based vaccine derived from the glioma stem cell line GBM6-AD, which was isolated from the brain tumor of a patient diagnosed with glioblastoma multiforme (GBM), with potential immunostimulatory and antineoplastic activities. Upon subcutaneous administration, the glioma lysate vaccine GBM6-AD exposes the immune system to an undefined amount of glioma-associated antigens (GAAs), and stimulates the immune system to mount a specific anti-tumoral, cytotoxic T-lymphocyte (CTL)-mediated response against the GAA-expressing cells, resulting in glioma cell lysis.
glioma-associated antigen peptide-pulsed autologous dendritic cell vaccine
A cancer vaccine comprised of autologous dendritic cells pulsed with synthetic glioma-associated antigen (GAA) peptides with potential antineoplastic activity. Upon administration, this vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against GAA peptide-expressing glioma cells, resulting in tumor cell lysis.
glioma-associated peptide-loaded dendritic cell vaccine SL-701
A cell-based cancer vaccine comprised of dendritic cells (DCs) pulsed with various synthetic glioma-associated antigen (GAA) peptides, with potential antineoplastic activity. Upon subcutaneous administration, the glioma-associated peptide-loaded DC vaccine SL-701 exposes the immune system to various GAA peptides. This may stimulate both anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against the GAA-expressing glioma cells, which may result in tumor cell lysis.
glipizide
A short-acting, second-generation sulfonylurea with hypoglycemic activity. Glipizide is rapidly absorbed, has a very quick onset of action and a short half-life. This agent is extensively metabolized in the liver and the metabolites as well as the unchanged form are excreted in the urine.
gliquidone
A potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.
glisoxepide
A second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, glisoxepide exerts greater binding affinity than the first-generation compounds. Glisoxepide shows peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity, has a short half-life and is excreted in both the bile and urine.
Globo H-DT vaccine OBI-833
A carbohydrate-based vaccine comprised of the Globo H hexasaccharide 1 (Globo H) antigen conjugated to DT-CRM197, a non-toxic, mutated form of diphtheria toxin (DT), with potential immunostimulating and antineoplastic activities. Upon administration of Globo H-DT vaccine OBI-833, the carbohydrate antigen Globo H may stimulate a cytotoxic T-lymphocyte (CTL) response against Globo H-expressing tumor cells, thereby decreasing tumor cell proliferation. The hexasaccharide Globo H is a tumor-associated antigen (TAA) commonly found on a variety of tumor cells. DT-CRM197 is used to increase the immunogenicity of the Globo H carbohydrate antigen.
Globo-H-GM2-Lewis-y-MUC1-32(aa)-sTn(c)-TF(c)-Tn(c)-KLH conjugate vaccine
A heptavalent vaccine consisting of the tumor-associated carbohydrate antigens globohexaosylceramide (globo-H), GM2, Lewis-y, MUC1-32(aa), sTn(c), TF(c), and Tn(c) conjugated with keyhole limpet hemocyanin (KLH), an immunomodulator. This vaccine may induce the production of IgG and IgM antibodies and an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumors expressing these antigens.
globulin component macrophage-activating factor
A recombinant form of naturally-occurring GC (group-specific component) protein-derived macrophage-activating factor (GC-MAF). GC, also known as vitamin D binding protein (VDBP). GC-MAF promotes macrophage activation.
glofitamab-gxbm
A bispecific monoclonal antibody, with potential antineoplastic activity. Glofitamab 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, glofitamab-gxbm 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.
Glosso-Sterandryl
(Other name for: methyltestosterone)
glucarpidase
A zinc-dependent enzyme isolated from a strain of the bacterium Pseudomonas. Because glucarpidase rapidly hydrolyzes methotrexate into inactive metabolites, it may be useful as a rescue agent for methotrexate-induced nephrotoxicity. In antibody-directed enzyme prodrug therapy (ADEPT), this agent is conjugated with an antibody that binds to a specific tumor cell type, allowing for glucarpidase-catalyzed activation of a co-administered prodrug at the site of the tumor.
Glucidex
(Other name for: maltodextrin)
glucocorticoid receptor antagonist ORIC-101
A mifepristone-based steroidal glucocorticoid receptor (GR) antagonist with potential antineoplastic activity. Upon oral administration, ORIC-101 selectively binds to GRs, thereby inhibiting the activation of GR-mediated proliferative and anti-apoptotic gene expression pathways. The GR, a member of the nuclear receptor superfamily of ligand-dependent transcription factors, is overexpressed in certain tumor types and may be associated with tumor cell proliferation and treatment resistance. Inhibition of GR activity may potentially slow tumor cell growth and disease progression in certain cancers. Due to its reduced androgen receptor (AR) agonistic activity and improved cytochrome P450 2C8 (CYP2C8) and 2C9 (CYP2C9) inhibition profile, ORIC-101 may be useful in the treatment of AR-positive tumors with reduced potential for drug-drug interactions.
Glucodry
(Other name for: maltodextrin)
Glucophage
(Other name for: metformin hydrochloride)
Glucophage ER
(Other name for: metformin hydrochloride)
Glucophage XR
(Other name for: extended release metformin hydrochloride)
glucosamine sulfate/chondroitin sulfate tablet
An oral tablet formulation of a dietary supplement containing the sulfate salts of the amino sugar glucosamine and the glucosaminoglycan chondroitin with potential analgesic, anti-inflammatory, and anti-arthritic activities. Both glucosamine and chondroitin are naturally occurring substances that play a key role in cartilage formation and repair. Glucosamine is an essential substrate for glycosaminoglycans and hyaluronic acid, needed for formation of the joint proteoglycan structural matrix, and may prevent chondrocytic catabolic activity and inhibit production of inflammatory mediators. Chondroitin is the major glycosaminoglycan in cartilage, responsible for the elasticity of cartilage; it may reduce the IL-1beta-induced nuclear factor-kappaB (NF-kB) translocation in chondrocytes, inhibiting NF-kB-mediated inflammatory processes.
Glucotrol
(Other name for: glipizide)
glucuronic acid
A carboxylic acid with structural similarity to glucose with detoxifying activity. The xenobiotic metabolism of various substances such as drugs, pollutants, bilirubin, androgens, estrogens, mineralocorticoids, glucocorticoids, fatty acid derivatives, retinoids, and bile acids involves glucuronidation, a process in which water-soluble, excretable glucuronides of these substances are formed via glycosidic linkages to glucuronic acid. UDP-glucuronic acid, formed in the liver through the linkage of glucuronic acid to uridine diphosphate (UDP) via a glycosidic bond, is an intermediate in the process of glucuronidation.
Glumetza
(Other name for: extended release metformin hydrochloride)
Glumetza
(Other name for: metformin hydrochloride)
glutamic acid
A non-essential alpha-amino acid and excitatory neurotransmitter. Glutamic acid can serve as a precursor for the synthesis of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA).
glutaminase inhibitor CB-839 hydrochloride
The hydrochloride salt form of CB-839, an orally bioavailable inhibitor of glutaminase, with potential antineoplastic and immunostimulating activities. Upon oral administration, CB-839 selectively and reversibly binds to and inhibits human glutaminase, an enzyme that is essential for the conversion of the amino acid glutamine into glutamate. Blocking glutamine metabolism inhibits proliferation in rapidly growing tumor cells and leads to an induction of cell death. Unlike normal healthy cells, glutamine-dependent tumors heavily rely on the intracellular conversion of exogenous glutamine into glutamate and glutamate metabolites to both provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival. In addition, CB-839 causes accumulation of glutamine in tumor cells and increases glutamine concentration in the tumor microenvironment (TME) upon cell death. As glutamine is essential for T-cell generation, CB-839 may also enhance T-cell proliferation and activation in the TME, which may lead to further killing of tumor cells.
glutaminase-1 inhibitor IACS-6274
An orally bioavailable inhibitor of the metabolic enzyme glutaminase-1 (GLS1), with potential antineoplastic and immunostimulating activities. Upon oral administration, IACS-6274 selectively targets, binds to and inhibits human GLS1, an enzyme that is essential for the conversion of the amino acid glutamine into glutamate. Blocking glutamine metabolism inhibits proliferation in rapidly growing tumor cells and leads to an induction of cell death. Unlike normal healthy cells, glutamine-dependent tumors heavily rely on the intracellular conversion of exogenous glutamine into glutamate and glutamate metabolites to provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival.
glutamine
A nonessential amino acid. Glutamine can donate the ammonia on its side chain to the formation of urea (for eventual excretion by the kidneys) and to purines (necessary for the synthesis of nucleic acids). Glutamic acid-to-glutamine conversion, in which an ammonia group is added to glutamic acid (catalyzed by glutamine synthase), is of central importance in the regulation of toxic levels of ammonia in the body. This agent is a substrate for the production of both excitatory and inhibitory neurotransmitters (glutamate and GABA) and is also an important source of energy for the nervous system. Glutamine may become a conditionally essential amino acid during certain catabolic states.
Glutapak-10
(Other name for: glutamine)
GlutaSolve
(Other name for: glutamine)
glutathione
A tripeptide comprised of three amino acids (cysteine, glutamic acid, and glycine) present in most mammalian tissue. Glutathione acts as an antioxidant, a free radical scavenger and a detoxifying agent. Glutathione is also important as a cofactor for the enzyme glutathione peroxidase, in the uptake of amino acids, and in the synthesis of leukotrienes. As a substrate for glutathione S-transferase, this agent reacts with a number of harmful chemical species, such as halides, epoxides and free radicals, to form harmless inactive products. In erythrocytes, these reactions prevent oxidative damage through the reduction of methemoglobin and peroxides. Glutathione is also involved in the formation and maintenance of disulfide bonds in proteins and in the transport of amino acids across cell membranes.
glutathione disulfide NOV-002
A stabilized formulation of disodium glutathione disulfide (GSSG; oxidized glutathione) and cisplatin (1000:1) with potential chemoprotective and immunomodulating activities. Mimicking endogenous GSSG, glutathione disulfide NOV-002 acts as a competitive substrate for gamma-glutamyl-transpeptidase (GGT), which may result in the S-glutathionylation of proteins, predominantly actin, a redox stress on endoplasmic reticulum (ER), and ER stress-induced apoptosis; S-glutathionylation may be stimulated by reactive oxygen species (ROS) liberated by a glutathione disulfide NOV-002-induced increase in GGT activity. Glutathione disulfide NOV-002 may also induce phosphorylation of proteins such as ERK and p38, two kinases that play critical regulatory roles in cell proliferation and apoptosis. The cisplatin component of this agent does not provide an effective therapeutic concentration of cisplatin in vivo.
glutathione pegylated liposomal doxorubicin hydrochloride formulation 2B3-101
A glutathione (GSH) pegylated, liposome-encapsulated preparation of the hydrochloride salt form of the anthracycline antineoplastic antibiotic doxorubicin, with potential anetineoplastic activity. Upon administration, the glutathione pegylated liposomal formulation 2B3-101 specifically delivers doxorubicin into the brain. Doxorubicin intercalates between DNA base pairs and interferes with topoisomerase II activity, which inhibits both DNA replication and RNA synthesis, resulting in cancer cell death and tumor regression. Doxorubicin also generates reactive oxygen species, which causes cell membrane lipid peroxidation leading to cytotoxicity. The pegylated liposomal delivery of doxorubicin improves drug penetration into tumors and prolongs circulation time, thereby increasing doxorubicin's efficacy and decreasing its toxicity. Conjugation of GSH to the PEG molecules directs the liposomes to the GSH transporters on the blood brain barrier (BBB) and improves the delivery of doxorubicin into the brain.
gluten-free compact nutritional supplement drink
A gluten-free, calorie-dense, milkshake-like nutritional supplement drink containing all essential vitamins, minerals, and trace elements, as well as protein, fat and carbohydrates. Upon oral intake, gluten-free compact nutritional supplement drink may aid in the prevention of malnutrition and weight loss. The drink is provided in a reduced volume (125 ml) but with the same complete nutrition as the standard drink (200 ml); the reduced volume may increase patient compliance.
gluten-free DHA/EPA/GLA/antioxidant-rich nutritional liquid
A gluten- and lactose-free, energy-rich, calorie-dense, non-complete liquid nutritional supplement enriched with eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), gamma-linolenic acid (GLA) and antioxidants, with potential anti-cachexic and anti-inflammatory activities. The nutritional liquid also contains protein, in the form of sodium and calcium caseinates, carbohydrates, as maltodextrin and sucrose, fat, as canola, borage, and marine oils, L-carnitine, taurine, and several other vitamins and minerals. Upon oral intake of the gluten-free DHA/EPA/GLA/antioxidant-rich nutritional liquid, the essential omega-3 polyunsaturated fatty acids EPA and DHA, derived from refined marine oil, and GLA, derived from borage oil, are incorporated into cell membranes and affect the production of pro-inflammatory mediators, which elicits an anti-inflammatory effect and may also prevent infections. The antioxidants, including ascorbic acid, beta-carotene, and tocopherols, neutralize free radicals, thereby protecting tissues and organs from oxidative damage. Medium chain triglycerides (MCT) and large chain triglycerides (LCT) in this supplement enhance fat absorption and increase calorie intake. Additionally, this nutritional supplement may prevent malnutrition and weight loss.
gluten-free/fiber enriched compact nutritional supplement drink
A gluten-free, calorie-dense, fiber-enriched milkshake-like nutritional supplement drink containing all essential vitamins, minerals, and trace elements, as well as protein, fat and carbohydrates. Upon oral intake, gluten-free, fiber-enriched compact nutritional supplement drink may aid in the prevention of malnutrition and weight loss. The drink is provided in a reduced volume (125 ml) but with the same complete nutrition as the standard drink (200 ml); the reduced volume may increase patient compliance. The fiber, acting as a prebiotic, promotes beneficial bacterial growth in the gastrointestinal (GI) tract, increases digestive health and may reduce the incidence of constipation and/or diarrhea.
glyburide
A sulfonamide urea derivative with antihyperglycemic activity that can potentially be used to decrease cerebral edema. Upon administration, glyburide binds to and blocks the sulfonylurea receptor type 1 (SUR1) subunit of the ATP-sensitive inwardly-rectifying potassium (K(ATP)) channels on the membranes of pancreatic beta cells. This prevents the inward current flow of positively charged potassium (K+) ions into the cell, and induces a calcium ion (Ca2+) influx through voltage-sensitive calcium channels, which triggers exocytosis of insulin-containing granules. In addition, glyburide also inhibits the SUR1-regulated nonselective cation (NC) Ca-ATP channel, melastatin 4 (transient receptor potential cation channel subfamily M member 4; (TRPM4)), thereby preventing capillary failure and brain swelling. SUR1-TRPM4 channels are formed by co-assembly of SUR1 with TRPM4 in neurons, astrocytes, and capillary endothelium during cerebral ischemia. Upon ischemia-induced ATP depletion, channels open which results in sodium influx, cytotoxic edema formation, capillary fragmentation and necrotic cell death. SUR1-TRPM4 is not expressed in normal, uninjured tissues.
glycerin enema
An enema solution containing 5% glycerin, a trihydroxy alcohol with osmotic laxative activity. Upon rectal administration, glycerin enema creates an osmotic gradient thereby attracting water into the rectum. This increases volume, increases peristalsis, stimulates evacuation, and relieves constipation.
glycine
A non-essential, non-polar, non-optical, glucogenic amino acid. Glycine, an inhibitory neurotransmitter in the CNS, triggers chloride ion influx via ionotropic receptors, thereby creating an inhibitory post-synaptic potential. In contrast, this agent also acts as a co-agonist, along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is an important component and precursor for many macromolecules in the cells.
glyco-engineered anti-CD20 monoclonal antibody CHO H01
A glyco-engineered monoclonal antibody directed against the human B-cell-specific cell surface antigen CD20, with potential antineoplastic and immunomodulating activities. Upon administration of glyco-engineered anti-CD20 monoclonal antibody CHO H01, 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, CHO H01 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. The Fc-glycans are homogenously engineered onto the antibody and increase ADCC, anti-tumor activity and the half-life of the antibody.
glycocyamine
A naturally-occurring derivative of glycine and a metabolic precursor of creatine. Glycocyamine, also known as guanidinoacetic acid (GAA), is catalyzed by guanidinoacetate N-methyltransferase to form creatine. Creatine, in phosphate form, helps supply energy to muscle cells for contraction. After intense effort, when adenosine triphosphate (ATP) deposits are depleted, creatine phosphate donates phosphate groups toward the fast synthesis of ATP. Dietary supplementation with GAA may improve muscle wasting associated with cancer and other chronic diseases.
glycooptimized trastuzumab-GEX
A glycoengineered form of a monoclonal antibody directed against the human epidermal growth factor receptor-2 (HER2), with potential antineoplastic activity. Glycooptimized trastuzumab-GEX specifically binds to the extracellular domain of HER2, thereby inducing an antibody-dependent cell-mediated cytotoxicity (ADCC) against HER2-expressing tumor cells. This eventually results in apoptosis and growth inhibition of tumor cells. HER2, a member of the receptor tyrosine kinase EGFR superfamily, is overexpressed on the cell surfaces of various solid tumors. This agent has a specific glycosylation profile that may enhance its ADCC response against HER2-expressing tumor cells.
glycopeptide antibiotic
One of a class of antibiotics originally isolated from plant and soil bacteria with structures containing either a glycosylated cyclic or polycyclic nonribosomal peptide. These antibiotics inhibit the cell wall structure of susceptible organisms (principally Gram-positive cocci) by inhibiting peptidoglycan synthesis. First-generation glycopeptide antibiotics include vancomycin, teicoplanin, and ramoplanin; second-generation semi-synthetic glycopeptide antibiotics include oritavancin, dalbavancin, and telavancin.
glycopyrrolate
A synthetic quaternary ammonium that is an anticholinergic agent with antispasmodic activity. Glycopyrrolate competitively binds to peripheral muscarinic receptors in the autonomic effector cells of, and inhibits cholinergic transmission in smooth muscle, cardiac muscle, the sinoatrial (SA) node, the atrioventricular (AV) node, exocrine glands and in the autonomic ganglia. Blockage of cholinergic transmission, in smooth muscle cells located in the gastrointestinal tract and the bladder, causes smooth muscle relaxation and prevents the occurrence of painful spasms. In addition, glycopyrrolate inhibits the release of gastric, pharyngeal, tracheal, and bronchial secretions.
glycosaminoglycan
Linear polysaccharides composed of disaccharide repeating units of glycosamine-glycans, two monosaccharide units (hexosamine and the repeating disaccharide of either hexuronate or galactose) located on the surface of cells or in the extracellular matrix contributing to adhesion, elasticity, and viscosity of extracellular substances.
glycosylated recombinant human G-CSF AVI-014
A glycosylated form of a recombinant agent that is chemically identical to or similar to endogenous human granulocyte colony-stimulating factor (G-CSF) and is produced using transgenic biotechnology. Transgenic hens carrying recombinant human G-CSF cDNA express the naturally glycosylated recombinant human protein in egg albumen from which glycosylated recombinant human G-CSF AVI-014 is isolated. Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions.
glycosylated recombinant human interleukin-7
A glycosylated recombinant protein which is chemically identical to or similar to endogenous human interleukin-7 (IL-7) with hematopoietic and immunopotentiating activities. Naturally produced by bone marrow, thymic stromal, and spleen cells, the cytokine interleukin-7 is a hematopoietic growth factor for progenitor B cells and T cells, stimulating proliferation and differentiation of mature T-cells and natural killer (NK) cells. As with glycosylated endogenous proteins, glycosylation of recombinant proteins may fundamentally affect their biological activity, function, clearance from circulation, and antigenicity; glycosylation of recombinant proteins that are chemically identical to similar to endogenous proteins may render protein structures and biological activities that are more similar to those of glycosylated endogenous proteins.
glymidine
A sulfapyrimidine derivative,also known as glycodiazine, with antihyperglycemic activity. Like sulfonylureas, glymidine is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells and increasing the sensitivity of peripheral tissues to insulin.
Glyset
(Other name for: miglitol)
GlyT2/5HT2a antagonist VVZ-149
An antagonist of both glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with potential anti-nociceptive activity. Upon administration, GlyT2/5HT2A antagonist VVZ-149 binds to and blocks both GlyT2 and 5HT2A. Blockage of GlyT2 prevents the re-uptake of the inhibitory neurotransmitter glycine in the synaptic cleft, thereby potentiating glycine-mediated inhibitory signaling, and inhibiting the firing of neurons, which suppresses the transmission of pain signals to the brain and induces analgesia. Blockage of 5HT2A prevents both the binding of its ligand serotonin and 5HT/5HT2A-mediated signaling. This also suppresses pain signaling and induces analgesia. GlyT2 and 5HT2A play key roles in the induction and transmission of pain signals. GlyT2, a glycine plasma membrane transporter, modulates glycine-mediated inhibition of synaptic transmission in the spinal cord and mediates pain signal transmission to the brain; inhibition of GlyT2 potentiates glycinergic mediated pain signaling. Serotonin and its 5HT2A receptor are involved in both serotonin receptor-mediated signaling and the perception of pain.
GM-CSF-encoding oncolytic adenovirus CGTG-102
A recombinant, oncolytic serotype 5/3 capsid-modified adenovirus encoding the immunostimulatory cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF) with potential antineoplastic activity. Upon administration, the oncolytic adenovirus selectively infects and replicates in tumor cells, which may result in tumor cell lysis. Synergistically, GM-CSF (sargramostim) expressed by the oncolytic adenovirus enhances antigen presentation, promotes natural killer (NK) cell-mediated killing and causes a cytotoxic T cell (CTL) response against tumor cells harboring the oncolytic adenovirus, resulting in an immune-mediated tumor cell death. CGTG-102 is designed to replicate only in cells with defects in the p16/Rb/E2F pathway, attributed to a mutation common in many solid tumors. Replacement of the Ad5 capsid protein knob with a knob domain from serotype 3 causes higher transduction in cancer cells as compared to normal cells.
GM-CSF-secreting MVX-2-loaded capsules/autologous irradiated tumor cell vaccine MVX-ONCO-2
A cancer vaccine composed of autologous irradiated tumor cells and two implantable capsules loaded with MVX-2 cells, which contain allogeneic genetically modified cells that continuously release granulocyte-macrophage colony stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Upon administration of GM-CSF-secreting MVX-2-loaded capsules/autologous irradiated tumor cell vaccine MVX-ONCO-2, the MVX-2-loaded capsules and the autologous irradiated cells isolated from the patient's own tumor are co-localized in the patient's tissue. GM-CSF is released, and the immune system is exposed to the tumor-associated antigens (TAAs) expressed by the autologous irradiated tumor cells at the injection site. GM-CSF recruits and activates antigen-presenting cells (APC), which induces both antibody-dependent cell-mediated cytotoxicity (ADCC) and cytotoxic T-lymphocyte (CTL) responses locally and systemically. This may lead to tumor regression. By using the patient's own irradiated cancer cells as vaccine antigens, the patient's immune system is exposed to the entire repertoire of this individual's TAAs. The encapsulation of MVX-2 cells protects them from the immune responses, thereby ensuring the continuous release of GM-CSF. GM-CSF, a monomeric glycoprotein that functions as a cytokine, is a strong immune booster and plays an important role in the activation of immune system.
GM-K562 cell vaccine
A cell-based vaccine comprised of K562 cells transfected with the granulocyte macrophage-colony stimulating factor (GM-CSF) gene with potential immunopotentiating properties. Vaccination with GM-K562 cells may stimulate the host immune system to produce an antitumoral T-lymphocyte response, thereby inhibiting tumor growth. K562 cells are derived from the human erythroleukemia cell line K562. GM-CSF (also known as sagramostim) expressed by vaccine cells binds to specific cell surface receptors, modulating the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production. GM-CSF also promotes antigen presentation, up-regulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function; it may also augment host antitumoral immunity.
GM.CD40L cell vaccine
A cell-based vaccine composed of irradiated tumor cells transduced with granulocyte-macrophage colony-stimulating factor (GM-CSF) and CD40-ligand (CD40L) genes. Upon administration, this vaccine may stimulate an anti-tumoral dendritic cell-mediated host immune response.
GM2-KLH vaccine
A cancer vaccine consisting of GM2 ganglioside, a melanoma-specific antigen, conjugated with the immunostimulant keyhole limpet hemocyanin. Vaccination with GM2-KLH vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against GM2 ganglioside-expressing melanoma cells, resulting in tumor growth inhibition.
GM2/GD2/GD3 lactone-KLH conjugate trivalent vaccine
A trivalent cancer vaccine containing the ganglioside lactones GM2, GD2 and GD3 conjugated with the immunostimulant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with GM2 lactone/GD2 lactone/GD3 lactone-KLH conjugate trivalent vaccine may elicit antibodies against tumor cells expressing any of these epitopes, resulting in an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing these gangliosides. GM2, GD2 and GD3 are tumor associated antigens (TAAs) that are overexpressed in a variety of tumor cell membranes.
GNAQ/GNA11 antagonist DYP688
An antagonist of guanine nucleotide-binding protein G(q) subunit alpha (GNAQ)/ guanine nucleotide-binding protein subunit alpha-11 (GNA11), with potential antineoplastic activity. Upon administration, GNAQ/GNA11 antagonist DYP688 inhibits the activity of GNAQ/GNA11 and prevents GNAQ/GNA11-mediated signaling. This may prevent proliferation in tumors overexpressing and/or harboring mutations of GNAQ/GNA11. GNAQ and GNA11 are involved in carcinogenesis and are mutated in certain melanomas.
GnRH antagonist SHR7280
An orally bioavailable gonadotropin-releasing hormone (GnRH) receptor antagonist, with potential hormone production inhibitory activity. Upon oral administration, GnRH antagonist SHR7280 competes with GnRH for receptor binding and inhibits GnRH receptor signaling in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. In females, this prevents the production of estrogen by the ovaries and may relieve symptoms from sex-hormone dependent diseases. Since SHR7280 reduces the occurrence of premature LH surge in females, premature ovulation is also prevented.
GnRH antagonist VERU-100
A long-acting depot formulation of a gonadotropin-releasing hormone (GnRH) receptor antagonist decapeptide, with potential hormone production inhibitory activity. Upon subcutaneous administration, GnRH antagonist VERU-100 competes with GnRH for receptor binding and inhibits GnRH receptor signaling in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with hormonally dependent disease states such as hormone-dependent prostate cancer.
golcadomide
A modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and antineoplastic activities. Upon administration, golcadomide specifically binds to cereblon (CRBN), thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces proteasome-mediated degradation of certain transcription factors, some of which are transcriptional repressors in T cells. This leads to modulation of the immune system, including activation of T lymphocytes, and downregulation of the activity of other proteins, some of which play key roles in the proliferation of certain cancer cell types. CRBN, the substrate recognition component of the CRL4-CRBN E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.
gold sodium thiomalate
The sodium salt of gold thiomalic acid, an organogold compound with antirheumatic and potential antineoplastic activities. Gold sodium thiomalate (GST) appears to inhibit the activity of atypical protein kinase C iota (PKCiota) by forming a cysteinyl-aurothiomalate adduct with the cysteine residue Cys-69 within the PB1 binding domain of PKCiota. This prevents the binding of Par6 (Partitioning defective protein 6) to PKCiota, thereby inhibiting PKCiota-mediated oncogenic signaling, which may result in the inhibition of tumor cell proliferation, the promotion of tumor cell differentiation, and the induction of tumor cell apoptosis. Atypical PKCiota, a serine/threonine kinase overexpressed in numerous cancer cell types, plays an important role in cancer proliferation, invasion, and survival; Par6 is a scaffold protein that facilitates atypical PKC-mediated phosphorylation of cytoplasmic proteins involved in epithelial and neuronal cell polarization.
goldenrod
A group of North American weedy herbs belonging to the genus Solidago (family Asteraceae) with potential chemopreventive activities. Goldenrod may also possess anti-inflammatory, antiseptic properties, diuretic and antifungal properties, and may relieve chemotherapy-induced side-effects.
golidocitinib
An orally available inhibitor of Janus-associated kinase 1 (JAK1), with potential antineoplastic activity. Upon oral administration, golidocitinib inhibits JAK-dependent signaling and may lead to an inhibition of cellular proliferation in JAK1-overexpressing tumor cells. The JAK-STAT (signal transducer and activator of transcription) signaling pathway is a major mediator of cytokine activity and is often dysregulated in a variety of tumor cell types. Additionally, JAK1 may be a primary driver of STAT3 phosphorylation and signaling, which plays a role in neoplastic transformation, resistance to apoptosis, tumor angiogenesis, metastasis, immune evasion, and treatment resistance.
golimumab
A human monoclonal antibody directed against the pro-inflammatory cytokine tumor necrosis factor-alpha (TNF-a) with immunosuppressive activity. Golimumab binds to TNF-a, thereby preventing TNF-a-mediated immune responses. TNF-a production is dysregulated in various auto-immune diseases and in cancer.
golnerminogene pradenovec
A recombinant agent consisting of a genetically-modified adenovirus 5 vector encoding the protein cytokine tumor necrosis factor (TNF) alpha. TNF exhibits potent anti-tumor cytolytic properties; the adenovirus 5 vector efficiently infects tumor cells, delivering tumor-specific TNF.
golotimod
An orally bioavailable synthetic peptide containing the amino acids D-glutamine and L-tryptophan connected by a gamma-glutamyl linkage with potential immunostimulating, antimicrobial and antineoplastic activities. Although the exact mechanism of action is unknown, golotimod appears to inhibit the expression of STAT-3, reversing immunosuppression and stimulating an anti-tumor immune response. This agent may stimulate the production of T-lymphocytes (in particular the helper T [Th1] cells), activate macrophages, and increase levels of interleukin 2 and interferon gamma. STAT-3, a transcription factor upregulated in many cancer cell types, is involved in tumor cell growth and survival and immunosuppression.
golvatinib
An orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. Golvatinib binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis.
gonadotrophin releasing hormone analogue
A synthetic analog of the endogenous hormone gonadotropin-releasing hormone (GnRH), with potential antineoplastic activity. Upon administration, GnRH analog mimics endogenous GnRH and strongly binds to and activates pituitary GnRH receptors, which stimulates the synthesis and secretion of the gonadotropic hormones, follicle stimulating hormone (FSH) and luteinizing hormone (LH). Continuous, prolonged activation by the GnRH analog results in pituitary GnRH receptor desensitization and receptor downregulation. This causes inhibition of pituitary gonadotropin secretion of LH and FSH. In males, the inhibition of LH secretion prevents the production and release of testosterone from Leydig cells in the testes and causes a significant decline in testosterone production that is near the levels seen after castration. This may inhibit androgen receptor-positive tumor progression. In females, this results in a decrease in estradiol production. GnRH, also called luteinizing hormone-releasing hormone (LH-RH), is normally synthesized in and secreted by the hypothalamus. Synthetic analogs of GnRH have a stronger receptor binding affinity than the endogenous form.
Goodbelly Probiotic
(Other name for: Lactobacillus plantarum 299v/Lactobacillus acidophilus/Bifidobacterium lactis probiotic supplement)
gorilla-derived adenovirus-expressing HPV-16/18 E6/E7 vaccine
An off-the-shelf (OTS) cancer vaccine comprised of a genetically engineered, replication-deficient gorilla-derived adenovirus encoding human papillomavirus (HPV) types 16 and 18 E6/E7 antigens, with potential immunostimulating and antineoplastic activities. Upon administration of gorilla-derived adenovirus expressing HPV-16/18 E6/E7 vaccine PRGN-2009, the adenovirus infects and expresses the HPV-16/18 E6/E7 proteins. The expressed proteins stimulate the host immune system to produce antigen-specific neutralizing antibodies and to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing HPV-16/18 E6/E7 antigens, thereby inducing tumor cell lysis. HPV oncoproteins play a key role in the development of cervical intraepithelial neoplasia (CIN) and cervical carcinoma.
gorilla-derived adenovirus-expressing HPV-6/11 vaccine PRGN-2012
An off-the-shelf (OTS) cancer vaccine comprised of a genetically engineered, replication-deficient gorilla-derived adenovirus encoding human papillomavirus (HPV) types 6 and 11, with potential immunostimulating and antineoplastic activities. Upon administration of gorilla-derived adenovirus-expressing HPV-6/11 vaccine PRGN-2012, the adenovirus infects and expresses the HPV-6/11 proteins. The expressed proteins stimulate the host immune system to produce antigen-specific neutralizing antibodies and to mount a cytotoxic T-lymphocyte (CTL) response against cells infected with HPV-6/11, thereby inducing tumor cell lysis. HPV6/11 play a key role in the development of recurrent respiratory papillomatosis (RRP).
goserelin acetate
The acetate salt of a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH). Continuous, prolonged administration of goserelin in males results in inhibition of pituitary gonadotropin secretion, leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
goserelin acetate extended-release microspheres LY01005
A long-acting, extended-release microsphere formulation of the acetate form of goserelin, a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH), with potential antineoplastic activity. Upon administration, goserelin binds to and activates pituitary gonadotropin-releasing hormone (GnRH) receptors. Prolonged administration of goserelin inhibits the secretion of pituitary gonadotropin, thereby decreasing levels of testosterone (in males) and estradiol (in females). Administration of this agent in an extended-release formulation may result in the regression of sex hormone-sensitive tumors and a reduction in sex organ size and function.
goserelin acetate extended-release microspheres LY01022
A long-acting, extended-release (ER) microsphere formulation of the acetate form of goserelin, a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH), with potential antineoplastic activity. Upon administration of goserelin acetate ER microspheres LY01022, goserelin is released over an extended period of time and binds to and activates pituitary gonadotropin-releasing hormone (GnRH) receptors. Prolonged administration of goserelin inhibits the secretion of pituitary gonadotropin, thereby decreasing levels of testosterone (in males) and estradiol (in females). Administration of the goserelin ER formulation may result in the regression of sex hormone-sensitive tumors and a reduction in sex organ size and function. LY01022 prolongs the dosing cycle to a three-month period, thereby reducing the frequency of injections and potentially improving compliance.
gossypol
An orally-active polyphenolic aldehyde with potential antineoplastic activity. Derived primarily from unrefined cottonseed oil, gossypol induces cell cycle arrest at the G0/G1 phase, thereby inhibiting DNA replication and inducing apoptosis. This agent also inhibits cell-signaling enzymes, resulting in inhibition of cell growth, and may act as a male contraceptive.
Gotistobart
A humanized, pH-sensitive immunoglobulin (Ig) G1 monoclonal antibody directed against the human T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4; CD152), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, gotistobart targets and binds to CTLA-4 expressed on T-cells and inhibits the CTLA-4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells, thereby killing cancer cells. As gotistobart is dissociated from CTLA-4 under low pH, it does not cause lysosomal degradation of CTLA-4, preserving CTLA-4 and allowing the recycling of CTLA-4. This may result in more efficient and selective CTLA-4-targeted regulatory T-cell (Treg) depletion within the tumor microenvironment (TME) while preserving CTLA-4 functions outside the TME, thereby reducing toxicities. CTLA-4, an inhibitory receptor and member of the immunoglobulin superfamily (IgSF), plays a key role in the downregulation of the immune system.
gozanertinib
An orally bioavailable dual kinase inhibitor of epidermal growth factor receptor (EGFR; ErbB1) and human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2), including EGFR L858R, EGFR T790M and HER2 exon 20 insertion (Ex20ins) mutations, with potential antineoplastic activity. Upon oral administration, gozanertinib targets, binds to and inhibits the activity of EGFR or HER2 insertions or mutations. This prevents EGFR/HER2-mediated signaling, which may induce cell death and inhibit tumor growth in EGFR/HER2-overexpressing tumor cells. The ErbB receptor tyrosine kinase family is involved in key cellular functions, including cell growth and survival. EGFR and HER2 alterations constitutively upregulate kinase activity.
gozetotide
An unlabeled radiotracer composed of the human prostate specific membrane antigen (PSMA)-targeting ligand and linked to the acyclic radiometal chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'-diacetic acid (HBED-CC), that may potentially be used to prevent or reduce salivary gland toxicities of PSMA-targeted radionuclides. Upon administration of gozetotide into the salivary gland, gozetotide may selectively decrease salivary uptake of systemically administered PSMA-targeted radionuclides. This may reduce the salivary gland toxicities of these agents including salivary gland hypofunction and xerostomia.
gp100 antigen
A melanoma-associated antigen. When administered in a vaccine formulation, gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumors that express this antigen, which may result in a reduction in tumor size.
gp100-fowlpox vaccine
A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the melanoma antigen glycoprotein 100 (gp 100) with potential antineoplastic activity. The expression of gp100 may generate a cellular immune response to melanoma cells; this effect is enhanced by the co-administration of interleukin 2 (IL-2).
gp100:154-162 peptide vaccine
A peptide consisting of amino acid residues 154 through 162 of the melanoma-melanocyte antigen gp100. Vaccination with gp100:154-162 peptide may enhance tumor-specific T-cell immunity. gp100 antigen is a self-antigen expressed by melanocytes, pigmented retinal cells, and most melanoma lesions and is recognized via class I and II HLA-restricted mechanisms.
gp100:209-217(210M) peptide vaccine
A synthetic peptide cancer vaccine consisting of amino acid residues 209 through 217 of the glycoprotein 100 (gp100) melanoma antigen, with a methionine substitution at position 210 designed to improve immunogenicity. Vaccination with gp100:209-217(210M) peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing gp100.
gp100:280-288(288V) peptide vaccine
A peptide vaccine consisting of the amino acids 280 through 288 of the melanoma antigen glycoprotein 100 (gp100) with potential antineoplastic activity. gp100:280-288(288V) peptide has a valine substitution at amino acid position 288 to improve immunogenicity. Vaccination with gp100:280-288(288V) peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the gp100 antigen, resulting in decreased tumor growth.
GP2 peptide/GM-CSF vaccine
A vaccine containing a HER2/Neu-derived epitope (amino acids 654-662) (GP2), and combined with granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential antineoplastic and immunoadjuvant activity. Upon vaccination, GP2 may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against HER2/Neu expressing cancer cells. GM-CSF may potentiate a tumor-specific cytotoxic T-lymphocyte (CTL) response against cancer cells expressing the HER2/Neu antigen. HER2/neu, a tumor associated antigen (TAA), is overexpressed in a variety of tumor cell types and is highly immunogenic.
gp96-secreting allogeneic bladder cancer cell vaccine HS-410
An allogeneic urothelial bladder cancer cell vaccine expressing a recombinant secretory form of the immunoadjuvant heat shock protein gp96 fused with an immunoglobulin Fc domain (gp96-Ig) protein, with potential antineoplastic activity. Upon administration of the gp96-Ig-secreting allogeneic bladder cancer cell vaccine HS-410, the live, irradiated tumor cells continuously secrete gp96-Ig along with its chaperoned tumor associated antigens (TAAs). This enhances antigen cross presentation to cytotoxic T-lymphocytes (CTLs) and, upon expansion, leads to the induction of a potent CTL response against the TAAs on the endogenous bladder cancer cells. This vaccine also induces a memory T cell response that could fight recurring cancer cells. gp96-Ig is constructed by replacing the KDEL endoplasmic reticulum (ER) retention sequence of gp96 with the Fc portion of the IgG1 protein. This allows for gp96, normally an ER-resident chaperone peptide, to be released from cells.
GPC3-targeted plasmid DNA vaccine NWRD06
A plasmid DNA therapeutic cancer vaccine encoding glypican-3 (GPC3), with potential immunomodulating and antineoplastic activities. Upon intramuscular administration of GPC3-targeted plasmid DNA vaccine NWRD06 and following electroporation, the plasmids enter the cells, and the cells express GPC3 and elicit a GPC3-specific cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing GPC3. GPC3, a heparan sulfate proteoglycan and a member of the glypican family, is overexpressed on certain tumor cell types while minimally expressed on normal, healthy cells; GPC3 plays an important role in cellular proliferation and differentiation.
GPI-0100
A semi-synthetic triterpene glycoside, derived from the naturally occurring saponins. GPI-0100 functions as an adjuvant when given as part of a vaccine preparation to improve the immunogenicity of antigens such as proteins, carbohydrates. GPI-0100 containing vaccines have been used with both viral and tumor antigens to elicit a Type 1 helper T cell response for those diseases in which a cytotoxic T lymphocyte (CTL) response is desired.
GPR35 inhibitor CT3001
An orally bioavailable inhibitor of G-protein coupled receptor 35 (GPR35) and formulated with polyethylene glycol 400 (PEG400), with potential antineoplastic activity. Upon oral administration, GPR35 inhibitor CT3001 targets, binds to and inhibits the activity of GPR35. As GPR35 promotes the activity of the transcription coactivators yes-associated protein 1 (YAP) and transcriptional coactivator with PDZ-binding motif (TAZ), the inhibition of GPR35 decreases YAP/TAZ activity and prevents the interaction between YAP/TAZ and the transcription factor TEAD (TEA domain). This may inhibit YAP/TAZ-TEAD promoted gene transcription involved in tumor cell proliferation, angiogenesis and survival, and may inhibit tumor cell proliferation. In addition, CT3001 may abrogate YAP/TAZ-mediated immunosuppression in the tumor microenvironment (TME) and may suppress regulatory T cells (Tregs) and increase cytotoxic T-lymphocyte (CTL) tumor infiltration. This may promote an anti-tumor immune response. GPR35, an oncogenic protein and member of the G protein-coupled receptor family, is overexpressed in a variety of tumors. It promotes tumor immune escape and mediates YAP/TAZ oncogenic activation. Pegylation increases the half-life of this agent.
GPRC5D/BCMA/CD3-targeting T-cell engager IBI3003
A T-cell engager (TCE) targeting the tumor-associated antigens (TAAs) B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17) and G-protein coupled receptor family C group 5 member D (GPRC5D), and the T-cell surface antigen CD3, with potential antineoplastic activity. Upon administration, GPRC5D/BCMA/CD3-targeting TCE IBI3003 binds to CD3 expressed on T cells, and BCMA and GPRC5D expressed on tumor cells. This results in the cross-linking of T-cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against BCMA- and GPRC5D-expressing tumor cells. BCMA, a receptor for both a proliferation-inducing ligand (APRIL) and B-cell activating factor (BAFF), is a member of the tumor necrosis factor receptor superfamily (TNFRSF). BCMA, found on the surfaces of plasma cells and overexpressed on malignant plasma cells, plays a key role in plasma cell proliferation and survival. GPRC5D is overexpressed in certain malignancies, such as multiple myeloma, while minimally expressed in normal, healthy cells. It plays a key role in tumor cell proliferation.
Grafapex
(Other name for: treosulfan)
Gralise
(Other name for: gabapentin)
granisetron
An indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
granisetron hydrochloride
The hydrochloride salt of an indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
granisetron hydrochloride nasal spray
An intranasal formulation containing the hydrochloride salt form of the indazole derivative granisetron, a selective serotonin (5-hydroxytryptamine; 5-HT) receptor antagonist, with antinauseant and antiemetic activities. Upon administration to the nostril, granisetron selectively binds to and inhibits 5-HT subtype 3 receptors (5-HT3R) located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting (CINV).
granisetron transdermal system
A transdermal system containing the selective serotonin (5-HT) receptor antagonist granisetron with antinauseant and antiemetic activities. Upon application of the transdermal system (patch) to the skin and the subsequent sustained release of granisetron into the bloodstream, granisetron selectively binds to and inhibits 5-HT subtype 3 (5-HT3) receptors located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting.
Granix
(Other name for: filgrastim)
Granocyte
(Other name for: lenograstim)
grape juice
Juice made from grapes that contain polyphenols, with potential antioxidant activity. Grape juice contains high amounts of flavonoids that may increase antioxidant activity and reduce oxidative stress. This may help to slow or prevent cell damage caused by oxidation.
grape seed extract supplement
An orally bioavailable dietary supplement composed of an extract from grape seeds containing high amounts of polyphenols, particularly lower proanthocyanidin oligomers (OPCs) and catechins, with antioxidant and chemopreventive activities. Upon administration, the active components in the grape seed extract (GSE) scavenge free radicals, protect against oxidation of low-density lipoprotein (LDL), and inhibit cell damage due to reactive oxygen species (ROS). This inhibits oxidative stress and protects against DNA damage. GSE also inhibits enzymes involved in inflammation, cell replication and DNA synthesis, and induces the expression of anti-oxidant enzymes. This may inhibit growth and induce apoptosis of cancer cells.
grapiprant
An orally bioavailable antagonist of the prostaglandin E receptor subtype 4 (EP4), with potential analgesic, immunomodulating and antineoplastic activities. Upon administration of grapiprant, this agent selectively binds to and inhibits the binding of prostaglandin E2 (PGE2) and prevents the activation of the EP4 receptor. This inhibits PGE2-EP4 receptor-mediated signaling and prevents proliferation in tumor cells in which the PGE2-EP4 signaling pathway is over-activated. In addition, EP4 receptor inhibition modulates the immune system by preventing both interleukin-23 (IL-23) production and the IL-23-mediated expansion of Th17 cells. As EP4 is expressed by peripheral sensory neurons, blockade of EP4-mediated signaling may induce an analgesic effect. EP4, a prostanoid receptor subtype, is a G protein-coupled receptor that is expressed in certain types of cancers; it promotes tumor cell proliferation and invasion.
green propolis supplement
An orally available, dietary supplement consisting of Taiwan green propolis dissolved in edible oil, with potential antibacterial, anti-inflammatory, antioxidant and anti-mucositis activities. Depending on location and seasons, a variety of phenolic acids, flavonoids, esters, diterpenes, sesquiterpenes, lignans, aromatic aldehydes, alcohols, amino acids, fatty acids, vitamins and minerals have been found in propolis, which is produced by bees using beeswax and saliva. The anti-mucositis effects of propolis may be attributable to the antibacterial, anti-inflammatory, and antioxidant activities of polyphenolic compounds including flavonoids and phenolic acids. Upon administration, green propolis supplement may kill bacteria thus potentially preventing inflammation of the mucosal membranes, thereby decreasing radiation-induced oral mucositis. In addition, propolis may act as antioxidant and scavenge free radicals. This may inhibit cellular oxidation and prevent free radical damage to cells.
green tea
Tea derived from the dried leaves of the plant Camellia sinensis with potential antioxidant, chemopreventive, and lipid-lowering activities. Green tea contains polyphenols that may be responsible for its chemopreventive effect. The polyphenol fraction contains mainly epigallocatechin-3-gallate (EGCG) and other catechins, such as epicatechin (EC), gallocatechin gallate (GCG), epigallocatechin (EGC), and epicatechin gallate (ECG). Green tea polyphenols act as antioxidants and free radical scavengers and may affect enzymes involved in cellular replication and tumor angiogenesis by modulating angiogenic factors, such as vascular endothelial growth factor (VEGF).
green tea extract
A defined, decaffeinated green tea polyphenol mixture isolated from Camellia sinensis, a plant native to Asia, with antiviral and antioxidant activities and potential chemopreventive activity. Green tea extract contains antioxidant compounds, including flavonoids, vitamins and polyphenols such as epigallocatechin-3-gallate (EGCG), which may have antineoplastic properties. Consumption of green tea extract may confer chemopreventive protection against various cancers including those of the prostate, stomach, and esophagus.
green tea extract-based antioxidant supplement
A dietary supplement containing a green tea extract including the catechin epigallocatechin gallate and other vitamins and antioxidants, with potential antineoplastic and chemopreventive activities. The polyphenols in green tea act as antioxidants and scavenge free radicals which may inhibit cellular oxidation and prevent free radical damage to cells. In addition, polyphenols may affect enzymes involved in cellular reproduction and tumor angiogenesis by modulating angiogenic factors. Other ingredients in green tea extract-based antioxidant supplement include dry cinnamon extract, germanium, zinc sulfate, manganese sulfate, arginine, cysteine, malic acid, ascorbic acid (vitamin c), glycyrrhizinic acid, glycine, glucosamine, pyridoxal (vitamin B6), calcium pantothenate (vitamin B5), folic acid, cyanocobalamin (vitamin B12).
green tea lozenge
A lozenge formulation of green tea, derived from the dried leaves of Camellia sinensis, with potential antioxidant and chemopreventive activities. Green tea lozenge contains polyphenols that may be responsible for its chemopreventive effect. The polyphenol fraction contains mainly epigallocatechin-3-gallate (EGCG) and other catechins, such as epicatechin (EC), gallocatechin gallate (GCG), epigallocatechin (EGC), and epicatechin gallate (ECG). Green tea polyphenols act as antioxidants and free radical scavengers, protecting cells from the damaging effects of reactive oxygen species (ROS).
green tea-based mouth rinse
A mouthwash containing green tea, derived from the dried leaves of Camelia sinensis, with potential antioxidant, protective and chemopreventive activities. Green tea contains polyphenols that are believed to be responsible for most of the green tea’s effects. The polyphenol fraction contains mainly epigallocatechin-3-gallate (EGCG) and other catechins, such as epicatechin (EC), gallocatechin gallate (GCG), epigallocatechin (EGC), and epicatechin gallate (ECG). Upon rinsing with the green tea mouthwash, the green tea polyphenols act as antioxidants and free radical scavengers, thereby protecting cells from reactive oxygen species (ROS) and prevent further cellular damage to the mucosa. This may decrease chemotherapy- and/or radiation-induced oral mucositis.
green tea/licorice extract-based antioxidant solution
A nutritional supplement containing a variety of antioxidants, vitamins, minerals and amino acids, including glycyrrhizic acid, epigallocatechin gallate (EGCG), zinc, vitamins B5, B6 and B12, vitamin C (ascorbic acid), folic acid, malic acid, glucosamine, arginine, and glycine, with potential immunomodulating, anti-inflammatory, protective, and antineoplastic activities. Upon oral administration, the antioxidants in the solution modulate certain enzymes involved in inflammation and oxidative stress and downregulate certain pro-inflammatory mediators. They also scavenge free radicals. This protects against inflammation- and reactive oxygen species (ROS)-induced cellular damage. In addition, this formulation may also inhibit various signal transduction pathways involved in inflammation and cancer, may suppress the growth of susceptible tumor cells, induce tumor cell cycle arrest, induce apoptosis and reduce angiogenesis and metastasis.
gridegalutamide
An orally bioavailable androgen receptor (AR) degrader, with potential antineoplastic activity. Upon administration, gridegalutamide 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).
GS/pan-Notch inhibitor AL102
An orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, GS/pan-Notch inhibitor AL102 binds to GS and blocks the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth of tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains and leads to their activation.
GSPT1 MGD MRT-2359
An orally bioavailable selective molecular glue degrader (MGD) of the translational termination factor GSPT1, with potential antineoplastic activity. Upon oral administration, MRT-2359 targets and binds to GSPT1, thereby promoting complex formation between the E3 ubiquitin ligase component cereblon (CRBN) and GSPT1, and inducing GSPT1 degradation in a CRBN- and degron-dependent manner. This downregulates L-MYC and N-MYC, thereby disrupting MYC-driven protein translation and reducing MYC-oncogenic signaling. This inhibits proliferation in MYC-driven tumors. The translation termination factor GSPT1, a G-loop degron-containing protein, plays a key role in protein translation in MYC-driven cancers.
GTN transdermal patch
(Other name for: nitroglycerin transdermal patch)
guadecitabine
A dinucleotide antimetabolite of a decitabine linked via phosphodiester bond to a guanosine, with potential antineoplastic activity. Following metabolic activation by phosphorylation and incorporation into DNA, guadecitabine inhibits DNA methyltransferase, thereby causing genome-wide and non-specific hypomethylation and inducing cell cycle arrest at S-phase. This agent is resistant to cytidine deaminase, hence may result in gradual release of decitabine both extra- and intracellularly, leading to more prolonged exposures to decitabine.
guanabenz acetate
The orally bioavailable, acetate salt form of guanabenz, a centrally-acting alpha-2 adrenergic receptor agonist, with anti-hypertensive and potential antineoplastic, cytoprotective and bone resorption inhibitory activities. Upon oral administration, guanabenz suppresses endoplasmic reticulum (ER) stress by inhibiting the stress-induced dephosphorylation of eukaryotic translation initiation factor 2 alpha (eIF2a), thereby enhancing the phosphorylation level of eIF2a. This causes elF2a-mediated downregulation of the Rac1 pathway, upregulates the expression of activating transcription factor 4 (ATF4), which plays a key role in osteoblastogenesis, and downregulates the expression of nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1), which is a transcription factor that plays a key role in osteoclastogenesis. This enhances osteoblastogenesis and suppresses osteoclastogenesis. Altogether, this promotes new bone formation and prevents bone degradation. In addition, guanabenz blocks the proliferation, survival, motility and invasiveness of tumor cells through the eIF2a-mediated downregulation of Rac1 signaling. Rac1, a Ras-related small GTPase belonging to the Rho family, plays a key role in tumor cell proliferation, survival and motility.
guanazole
A cytostatic triazole derivative antimetabolite. Guanazole scavenges tyrosine free radicals, thereby inhibiting mammalian ribonucleotide reductase activity and DNA synthesis.
guarana supplement
An herbal supplement containing an extract from guarana (Paullinia cupana), a climbing plant of the Sapindaceae family which is native to the Amazon basin, with stimulant, antioxidant and potential chemoprotective activities. Guarana supplement contains various phytochemicals, including caffeine, theobromine, theophylline, tannins, saponins, catechins, epicatechins, proanthocyanidols and other compounds in minor concentrations. Caffeine is a central nervous system stimulant and may reduce chemotherapy-related fatigue. Tannins and other polyphenols may have chemopreventive activity. Intake of the guarana supplement may prevent cancer-related anorexia. In addition, animal studies have demonstrated that the ingestion of guarana resulted in decreased proliferation and increased apoptosis of tumor cells.
gum Arabic solution
A solution containing the polymer gum acacia (gum Arabic), exuded from various acacia trees, especially from Acacia senegal (Leguminosae), with potential protective and anti-mucositis activities. Upon administration of the gum Arabic solution in the oral cavity, the polymer forms a protective barrier over the oral mucosa, which may prevent inflammation of the mucosal membranes and may decrease chemotherapy- and/or radiation-induced oral mucositis.
gumarontinib
An orally bioavailable, small molecule inhibitor of the oncoprotein c-Met (hepatocyte growth factor receptor; HGFR), with potential antineoplastic activity. Upon oral administration, gumarontinib targets and binds to the c-Met protein, thereby disrupting c-Met-dependent signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.
gunagratinib
A small molecule pan inhibitor of human fibroblast growth factor receptors (FGFRs), with potential antiangiogenic and antineoplastic activities. Upon oral administration,gunagratinib inhibits the activities of FGFRs, which may result in the inhibition of both tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs, a family of receptor tyrosine kinases upregulated in various tumor cell types, may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival.
guselkumab
An orally available, human, immunoglobulin G1 (IgG1) kappa, monoclonal antibody directed against the p19 protein subunit of interleukin-23 (IL-23), with immunomodulating activity. Upon administration, guselkumab binds to the p19 subunit of IL-23, thereby blocking the binding of IL-23 to the IL-23 receptor. This inhibits IL-23-mediated signaling and the differentiation of CD4-positive T-cells into Th1 and Th17 cells. This prevents Th1- and Th17-mediated immune responses and inhibits the production of pro-inflammatory cytokines. This may prevent or reduce symptoms and severity of immune-mediated inflammatory disorders. IL-23 plays a key role in the regulation of inflammation and the immune system, and modulates the release of various pro-inflammatory cytokines and chemokines. It is upregulated in various immune-mediated inflammatory disorders.
gusperimus
A derivative of the antitumor antibiotic spergualin with immunosuppressant activity. Gusperimus inhibits the interleukin-2-stimulated maturation of T cells to the S and G2/M phases and the polarization of the T cells into IFN-gamma-secreting Th1 effector T cells, resulting in the inhibition of growth of activated naive CD4 T cells; this agent may suppress growth of certain T-cell leukemia cell lines.
Gwt1 inhibitor APX001
An orally available small molecule inhibitor of the Gwt1 fungal enzyme with potential antifungal activity. Upon administration APX001, a N-phosphonooxymethyl prodrug, is rapidly and completely metabolized by systemic alkaline phosphatases to its active moiety, APX001A (E1210). The active prodrug targets Gwt1, a highly conserved inositol acylase which catalyzes an essential step in the glycosylphosphatidylinositol (GPI)-anchor biosynthesis pathway. Inhibition of Gwt1 prevents localization of cell wall mannoproteins, which compromises cell wall integrity, biofilm formation, germ tube formation, and fungal growth.
Gyne-Lotrimin
(Other name for: clotrimazole)