NCI Drug Dictionary

161 results found for: Z

Z-360: A selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells.
zabadinostat: A novel histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Although the exact therapeutic mechanism of action for CXD101 is not known, oral administration of this agent should inhibit the catalytic activity of HDAC, which results in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. HDAC, a family of enzymes upregulated in many tumor types, deacetylates chromatin-associated histone proteins.
Zactima: (Other name for: vandetanib)
Zadaxin: (Other name for: thymalfasin)
Zaditen: (Other name for: ketotifen fumarate)
Zaditor: (Other name for: ketotifen fumarate)
zafirlukast: A tolyl compound and leukotriene receptor antagonist (LTRA), with anti-asthmatic and potential capsular contracture-preventing activities. Upon administration, zafirlukast selectively and competitively binds to and blocks the cysteinyl leukotriene 1 receptor (CYSLTR1), thereby preventing the potent pro-inflammatory mediators leukotriene C4, D4 and E4 from binding. This prevents leukotriene-mediated actions, including enhanced migration of eosinophils and neutrophils, increased adhesion of leukocytes, increased monocyte and neutrophil aggregation, increased airway edema, inflammation, capillary permeability and bronchoconstriction. In addition, zafirlukast may decrease collagen deposition, fibrosis, and capsular thickness after implantation, thereby preventing scar tissue.
zalcitabine: A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zalcitabine preferentially inhibits the gamma form of DNA polymerase present in tumor cell mitochondria, resulting in the inhibition of tumor cell mitochondrial DNA replication and tumor cell death.
zalifrelimab: A recombinant human monoclonal antibody directed against the human T-cell receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4), with immune checkpoint inhibitory and antineoplastic activities. Upon administration, zalifrelimab 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. CTLA-4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system.
Zaltrap: (Other name for: ziv-aflibercept)
zalutumumab: A fully human IgG1 monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Zalutumumab selectively binds to the EGFR receptor and blocks receptor binding of EGF and transforming growth factor-alpha (TGF-a), which results in the disruption of EGFR-mediated cell signaling, cell growth inhibition and apoptosis in EGFR-expressing tumor cells. In addition, this agent triggers antibody dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. EGFR is a cell surface receptor tyrosine kinase, overexpressed on many cancer cells.
Zalypsis: (Other name for: PM00104)
zamtocabtagene autoleucel: A preparation of autologous CD4/CD8 enriched T lymphocytes engineered to express pLTG1497, a tandem chimeric antigen receptor (CAR) specific for the two tumor-associated antigens (TAAs) cluster of differentiation 19 (CD19) and CD20, with potential immunostimulating and antineoplastic activities. Upon administration, zamtocabtagene autoleucel target and bind to CD19- and CD20-expressing tumor B cells. This induces selective toxicity in tumor B-cells expressing these TAAs. Both CD19 and CD20 are B-cell-specific cell surface antigens overexpressed in B-cell lineage malignancies. Targeting both CD19 and CD20 may prevent tumor cell antigen escape and relapse.
Zanaflex: (Other name for: tizanidine hydrochloride)
zanamivir: A sialic acid-analogue neuraminidase inhibitor with antiviral activity. Administered into the respiratory tract by aerosol inhalation, zanamivir selectively binds to and inhibits influenza A and B virus neuraminidase-mediated cleavage of sialic acid residues in host cell membrane-bound glycoprotein receptors for influenza viruses, preventing the release of progeny viruses from host cell surfaces and, so, further viral replication.
zandelisib: An orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity. Upon oral administration, zandelisib selectively inhibits the delta isoform of PI3K and prevents the activation of the PI3K/AKT signaling pathway. This both decreases proliferation and induces cell death in PI3K-delta-overexpressing tumor cells. PI3K-delta plays a key role in the proliferation and survival of hematologic cancer cells. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells. PI3K, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival.
zanidatamab-hrii: A humanized, immunoglobulin G1 (IgG1) bispecific monoclonal antibody that targets two different non-overlapping epitopes of the human tumor-associated antigen (TAA) epidermal growth factor receptor 2 (HER2), ECD2 and ECD4, with potential immunomodulating and antineoplastic activities. Upon administration, zanidatamab-hrii targets and binds to the two distinct HER2 domains on the tumor cell surface. This results in dual HER2 signal blockade, HER2 clustering, receptor internalization and downregulation. This inhibits HER2 activation, HER2-mediated signaling and HER2-mediated tumor cell growth. The specific binding of zanidatamab to tumor cells and HER2 aggregation also activates various immune-mediated responses, and induces complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), and antibody-dependent cellular phagocytosis (ADCP) against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
zanolimumab: A human IgG1k monoclonal antibody against the CD4 receptor on T lymphocytes, with potential antineoplastic and immunosuppressing activities. Zanolimumab targets and binds to the CD4 receptor on certain T cells thereby preventing the interaction between the CD4 receptor and the major histocompatibility complex class II molecule. This prevents activation of CD4-positive T cells. In addition, zanolimumab is able to induce an antibody-dependent cellular cytotoxicity (ADCC) response against CD4-expressing tumor cells. CD4, a receptor located on a subset of T-lymphocytes, is upregulated in T-cell lymphomas.
Zanosar: (Other name for: streptozocin)
Zantac: (Other name for: ranitidine hydrochloride)
Zanthoxylum fructus/Zingiberis siccatum Rhizoma/Ginseng radix-based supplement TU-100: A traditional Japanese medicine composed of extracts from dried Japanese pepper (Zanthoxylum fructus), processed ginger (Zingiberis siccatum rhizoma), ginseng radix and maltose powder, with potential gastrointestinal (GI) prokinetic activity. Upon administration, Zanthoxylum fructus/Zingiberis siccatum rhizoma/ginseng radix-based supplement TU-100 may increase GI motility via cholinergic and serotonergic mechanisms.
zanubrutinib: An inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, zanubrutinib inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival.
zanzalintinib: An orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) hepatocyte growth factor receptor (c-Met; HGFR), vascular endothelial growth factor receptor type 2 (VEGFR2), AXL and MER, with potential anti-angiogenesis and antineoplastic activities. Upon oral administration, zanzalintinib targets and binds to c-Met, VEGFR2, AXL and MER, and prevents their RTK activity. This blocks c-Met/VEGFR2/AXL/MER-mediated signal transduction pathways, and inhibits the proliferation and migration of c-Met-, VEGFR2-, AXL- and MER-overexpressing tumor cells. c-Met, overexpressed in many tumor cell types, plays a critical role in tumor formation, proliferation, invasion and metastasis, and contributes to tumor resistance. VEGFR2, overexpressed in certain tumor types, plays an essential role in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells. AXL and MER, both members of the TAM (Tyro3, Axl and Mer) family of RTKs, are overexpressed by many tumor cell types. They play key roles in tumor cell proliferation, survival, invasion, angiogenesis and metastasis, and their expression is associated with enhanced immunosuppression, drug resistance and poor prognosis.
Zarnestra: (Other name for: tipifarnib)
Zarontin: (Other name for: ethosuximide)
Zarxio: (Other name for: filgrastim)
ZD6126: A water-soluble phosphate prodrug of N-acetylcolchinol with potential antiangiogenesis and antineoplastic activities. ZD6126 is converted in vivo into N-acetylcolchinol. N-acetylcolchinol binds to and destabilizes the tubulin cytoskeleton of endothelial cells in tumor blood vessels, which may result in tumor endothelial cel apoptosis, the selective occlusion of tumor blood vessels, cessation of tumor blood flow, and tumor necrosis.
zebutinib: An orally bioavailable inhibitor of Bruton's tyrosine kinase (BTK), with potential antineoplastic activity. Upon oral administration, zebutinib targets, binds to and inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival.
zedoresertib: An orally bioavailable inhibitor of the human tyrosine kinase Wee1 (Wee1-like protein kinase; Wee1A kinase; WEE1hu), with potential antineoplastic sensitizing activity. Upon oral administration, zedoresertib targets, binds to and inhibits Wee1. Inhibition of Wee1 inhibits Cdk1 (Cdc2) phosphorylation, promotes both premature mitosis and a prolonged mitotic arrest, which results in the accumulation of unrepaired DNA damage. This leads to apoptosis in susceptible tumor cells, such as p53-deficient or mutated human cancers that lack the G1 checkpoint, especially in combination with DNA-damaging chemotherapeutic agents. Unlike normal cells, most p53-deficient or mutated human cancers lack the G1 checkpoint as p53 is the key regulator of the G1 checkpoint and these cells rely on the G2 checkpoint for DNA repair to damaged cells. Annulment of the G2 checkpoint may therefore make p53-deficient tumor cells more vulnerable to antineoplastic agents and enhance their cytotoxic effect. Overexpression of Wee1 occurs in several cancer types and high expression of Wee1 is associated with poor outcomes. Wee1 phosphorylates Cdc2 in the Cdc2/cyclin B (CDK1/cyclin B) complex which blocks progression from G2 into mitosis. The Wee1 tyrosine kinase is activated upon DNA damage and regulates the G2-M and S cell cycle checkpoints.
Zejula: (Other name for: niraparib tosylate monohydrate)
zelavespib: A purine-based heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Zelavespib specifically inhibits active Hsp90, thereby inhibiting its chaperone function and promoting the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. This may result in the inhibition of cellular proliferation in susceptible tumor cell populations. Hsp90, a molecular chaperone protein, is upregulated in a variety of tumor cell types.
Zelboraf: (Other name for: vemurafenib)
zelenectide pevedotin: A Bicycle toxin conjugate (BTC) composed of a zelenectide, a synthetic, bicyclic peptide targeting the cell adhesion molecule nectin-4 (PVRL4) and conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), via an inert sarcosine spacer chain and a valine-citrulline cleavable linker, with potential antineoplastic activity. Upon administration, the bicyclic peptide moiety of zelenectide pevedotin selectively binds to nectin-4. After internalization and proteolytic cleavage by peptidases that are upregulated in the tumor microenvironment (TME), MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in nectin-4 overexpressing tumor cells. 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. It is associated with poor disease prognosis.
zelenoleucel: A preparation of allogeneic multi-tumor-associated antigen (MultiTAA)-specific T lymphocytes, with potential immunomodulating and antineoplastic activities. Upon administration, zelenoleucel may target and kill tumor cells expressing the TAAs.
Zemplar: (Other name for: paricalcitol)
Zemuron: (Other name for: rocuronium bromide)
Zenapax: (Other name for: daclizumab)
zenocutuzumab-zbco: A full-length IgG1 bispecific antibody with enhanced antibody-dependent cellular cytotoxicity (ADCC) directed against human epidermal growth factor receptor 2 (HER2; EGFR2, ERBB2) and human epidermal growth factor receptor 3 (HER3; ErbB3), with potential antineoplastic activity. Upon intravenous administration of zenocutuzumab, the bispecific antibody docks on HER2, and subsequently blocks heregulin-stimulated proliferation of tumor cells by binding HER3. In addition to inhibiting HER3-dependent signaling, simultaneous targeting of HER2 and HER3 by zenocutuzumab-zbco may overcome a common resistance mechanism driven by heregulin-mediated dimerization of HER2 and HER3. Zenocutuzumab-zbco is expected to eliminate tumor cells by recruiting natural killer (NK) cells to tumor cells coated with the bispecific antibody.
Zenpep: (Other name for: pancrelipase)
Zentel: (Other name for: albendazole)
Zepatier: (Other name for: elbasvir/grazoprevir)
Zeposia: (Other name for: ozanimod hydrochloride)
Zepzelca: (Other name for: lurbinectedin)
Zerbaxa: (Other name for: ceftolozane-tazobactam)
Zerit: (Other name for: stavudine)
Zestril: (Other name for: lisinopril)
zeteletinib: An orally bioavailable selective inhibitor of wild-type, fusion products and mutated forms, including gatekeeper mutations, of the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, zeteletinib selectively binds to and inhibits the activity of RET. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.
Zetia: (Other name for: ezetimibe)
Zevalin: (Other name for: ibritumomab tiuxetan)
Zeven: (Other name for: Hsp90 inhibitor debio 0932)
Zeven: (Other name for: dalbavancin)
zhongyao fufang: A combination formula consisting of two or more unknown Traditional Chinese Medicine (TCM) ingredients, with potential anti-osteoporotic activity. Upon oral administration, this particular formula of zhongyao fufang may promote increased bone strength and density.
Ziagen: (Other name for: abacavir sulfate)
zibotentan: An orally available selective antagonist of the endothelin-A (ET-A) receptor with potential antineoplastic activity. Zibotentan binds selectively to the ET-A receptor, thereby inhibiting endothelin-mediated mechanisms that promote tumor cell proliferation.
ziconotide: A synthetic, nonopiod, twenty-five amino acid polybasic peptide analogue of an omega-conotoxin derived from the marine snail Conus magus with analgesic activity. Ziconotide appears to block neuronal N-type voltage-sensitive calcium channels (NCCB), inhibiting transmission from pain-sensing primary nociceptors. This agent may exhibit significant analgesic activity in refractory pain.
zidesamtinib: An orally available selective inhibitor of the receptor tyrosine kinase c-ros oncogene 1 (ROS1), with potential antineoplastic activity. Upon oral administration, zidesamtinib targets, binds to and inhibits wild-type, point mutants and fusion proteins of ROS1. This inhibits proliferation of ROS-1-driven tumor cells, including in tumor cells harboring certain ROS1 resistance mutations, such as the solvent front mutation G2032R and the S1986Y/F, L2026M, and D2033N resistance mutations. Inhibition of ROS1 leads to the disruption of downstream signaling pathways and the inhibition of cell growth of tumors in which ROS1 overexpressed, rearranged or mutated. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells. NVL-520 is able to penetrate the blood-brain barrier (BBB).
zidovudine: A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zidovudine inhibits DNA polymerase, resulting in the inhibition of DNA replication and cell death. This agent also decreases levels of available pyrimidines.
Ziextenzo: (Other name for: pegfilgrastim)
ziftomenib: An orally bioavailable inhibitor of the menin-mixed lineage leukemia (MLL; myeloid/lymphoid leukemia; KMT2A) fusion protein, with potential antineoplastic activity. Upon oral administration, ziftomenib prevents the interaction between the two proteins menin and MLL, and thus the formation of the menin-MLL complex. This reduces the expression of downstream target genes and results in an inhibition of the proliferation of MLL-rearranged leukemic cells. The menin-MLL complex plays a key role in the survival, growth and proliferation of certain kinds of leukemia cells.
Ziihera: (Other name for: zanidatamab-hrii)
zileuton: A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.
zilovertamab vedotin: An antibody-drug conjugate (ADC) composed of a monoclonal antibody against the tumor-associated antigen (TAA) receptor tyrosine kinase-like orphan receptor 1 (ROR1) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of zilovertamab vedotin targets and binds to ROR1 expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the ROR1-expressing cancer cells, through an as of yet unknown mechanism of action. ROR1, also known as neurotrophic tyrosine kinase, receptor-related 1 (NTRKR1), is expressed during embryogenesis and by certain leukemias. It plays key roles in tumor cell proliferation and survival.
zilucoplan: A synthetic macrocyclic peptide inhibitor of the terminal complement protein C5, with potential anti-inflammatory and cell protective activities. Upon subcutaneous administration, complement zilucoplan binds to a unique site in terminal complement protein C5, which blocks C5 cleavage into C5a and C5b and prevents the C5b-dependent assembly of the membrane-attack complex (MAC). Zilucoplan also inhibits the interaction between C5b and C6, thereby further blocking MAC assembly. This prevents MAC-mediated lysis and destruction of red blood cells (RBCs) that occurs in complement-mediated diseases, such as paroxysmal nocturnal hemoglobinuria (PNH), generalized myasthenia gravis (gMG) and lupus nephritis (LN). C5, a complement pathway protein, is expressed at high levels by the liver.
zimberelimab: A human immunoglobulin G4 (IgG4) monoclonal antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, zimberelimab targets, binds to and inhibits PD-1 and its downstream signaling pathways. This may restore immune function through the activation of T cells and T-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; B7-H1; CD274) and 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
zinc finger nuclease ZFN-603: A zinc finger nuclease (ZFN) targeting the human papillomavirus (HPV) type 16 (HPV16) oncoprotein E7, with potential antineoplastic activity. Upon transfection of ZFN-603 into HPV16-positive cells, ZFN-603 targets, binds to and cleaves the HPV16 E7 oncogene in HPV16-infected cells. By cleaving the HPV16 E7 DNA, the E7 oncoprotein is not expressed. This results in an inhibition of E7-mediated signaling, an induction of apoptosis, and inhibition of tumor cell proliferation in HPV16-expressing cells. In addition, preventing E7 expression induces the expression of tumor suppressor genes, thereby further preventing HPV-induced cancer cell formation and proliferation. E7 plays a key role in promoting both viral infection and carcinogenesis. ZFN, an engineered endonuclease in which a DNA-binding zinc finger protein is fused to a DNA-cleavable domain, cleaves specific DNA sites.
zinc finger nuclease ZFN-758: A zinc finger nuclease (ZFN) targeting the human papillomavirus (HPV) type 18 (HPV18) oncoprotein E7, with potential antineoplastic activity. Upon transfection of ZFN-758 into HPV18-positive cells, ZFN-758 targets, binds to and cleaves the HPV18 E7 oncogene in HPV18-infected cells. By cleaving the HPV18 E7 DNA, the E7 oncoprotein is not expressed. This results in an inhibition of E7-mediated signaling, an induction of apoptosis, and an inhibition of tumor cell proliferation in HPV18-expressing cells. In addition, preventing E7 expression induces the expression of tumor suppressor genes, thereby further preventing HPV-induced cancer cell formation and proliferation. E7 plays a key role in promoting both viral infection and carcinogenesis. ZFN, an engineered endonuclease in which a DNA-binding zinc finger protein is fused to a DNA-cleavable domain, cleaves specific DNA sites.
zinc gluconate: A nutritional supplement containing the zinc salt form of gluconic acid for the purpose of providing zinc. As an essential trace element, zinc is of key importance in many biological processes, acts as an antioxidant and strengthens the immune system. Although the mechanism of action is not completely known, zinc supplementation may be used to increase immunity against viruses or may interfere with the replication of certain viruses, such as the human papillomavirus (HPV).
zinc oxide/aluminum starch octenylsuccinate/glycyrrhetinic phytosome/vitamin E/botanical extracts-based skin protectant paste: A paste containing multiple skin protectants with anti-oxidant, skin protecting, moisturizing, anti-erythema and anti-inflammatory activities. The paste includes zinc oxide, aluminum starch octenylsuccinate, lanolin, allantoin, chamomile and sweet almond oil, rice bran oil, shea butter, dimethicone (polymerized siloxane), petrolatum, vitamin E, phytosome of glycyrrhetinic acid and botanical extracts derived from Calendula officinalis, Malva sylvestris and Tilia tomentosa. Upon application, this paste provides a physical barrier on the skin and may help protect, soothe and moisturize the skin as well as restore skin softness, integrity and elasticity. When this paste is applied to the perineum area, it may help prevent radiation-induced dermatitis.
zinc sulfate: A salt of the essential trace metal zinc. Zinc is involved in tissue repair and is an important constituent of some proteins, including those involved in taste and smell. Zinc sulfate supplementation may prevent radiation-induced aguesia.
Zinecard: (Other name for: dexrazoxane hydrochloride)
zinostatin: An enediyne antineoplastic antibiotic hybrid containing an aminoglycoside chromophore. Zinostatin is isolated from the bacterium Streptomyces carzinostaticus. The aminoglycoside component of zinostatin intercalates into DNA and the benzene diradical intermediate of the enediyne core binds to the minor groove of DNA, resulting in single- and double-strand breaks in DNA and apoptosis.
zinpentraxin alfa: A fully recombinant form of the human pentraxin 2 (PTX2) protein with potential antifibrotic activity. Upon intravenous administration, zinpentraxin alfa may inhibit myofibroblast generation by preventing the differentiation of circulating monocytes into fibrocytes and profibrotic macrophages. PTX2 is a circulating plasma protein that belongs to the class of pattern recognition receptors (PRR) of the innate immune system.
Zinplava: (Other name for: bezlotoxumab)
zipalertinib: An orally available selective inhibitor of a broad spectrum of epidermal growth factor receptor (EGFR) mutations, including EGFR exon 20 insertion mutations (EGFR Ex20ins; Ex20ins mutations), with potential antineoplastic activity. CLN-081 is also active against other EGFR mutations including exon 19 deletions (exon19del), L858R, and T790M, as well as the less common G719X, L861Q and S768I mutations. Upon administration, zipalertinib specifically and covalently binds to and inhibits a variety of EGFR mutations, with particularly high selectivity against EGFR Ex20ins, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, CLN-081 may have therapeutic benefits in tumors with EGFR Ex20ins, as most EGFR mutant-selective inhibitors are not active against EGFR Ex20ins. This agent shows minimal activity against wild-type EGFR (wt EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit wt EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
Zipan: (Other name for: promethazine hydrochloride)
Zirabev: (Other name for: bevacizumab)
zirconium Zr 89 anti-CD8 antibody ZED88082A: A radioimmunoconjugate consisting of an antibody targeting the human CD8 antigen on CD8-positive (CD8+) T cells and labeled with the radioisotope zirconium Zr 89, with potential imaging activity using positron emission tomography (PET). Upon administration, the antibody moiety of ZED88082A specifically targets and binds to the CD8 antigen expressed on T cells. This allows for visualization of CD8+ T cells upon imaging using PET. CD8+ T cells are effector cells involved in the immune response against tumor cells and play a key role in the eradication of tumor cells.
zirconium Zr 89 anti-TAA monoclonal antibody BAY3630942: A radioimmunoconjugate comprised of a monoclonal antibody directed against an as of yet undisclosed tumor-associated antigen (TAA) conjugated to the radioisotope zirconium Zr 89 (Zr89), with potential use as an imaging agent upon positron emission tomography/computed tomography (PET/CT). Upon administration of Zr89 anti-TAA monoclonal antibody BAY3630942, the antibody moiety specifically targets and binds to the TAA expressed on tumor cells. Upon binding, the radioisotope moiety is detected using PET, thereby allowing the imaging of TAA-expressing tumors.
zirconium Zr 89 crefmirlimab berdoxam: A radioimmunoconjugate comprised of a minibody (Mb), an inert antibody fragment against the human CD8-antigen on CD8-positive T cells, conjugated to the chelator desferrioxamine (Df) and labeled with the radioisotope zirconium Zr 89, with potential positron emission tomography (PET) imaging activity. Upon administration, zirconium Zr 89 crefmirlimab berdoxam specifically targets and binds to the CD8 antigen expressed on T cells. This enables PET detection of the radioisotope moiety, and may allow the imaging, tracking and quantification of CD8-expressing T-cells. This may detect CD8-positive T-cell distribution and activity, and may help determine the patient's response to cancer immunotherapeutic agents. CD8-positive T cells play a key role in the eradication of cancer cells. Although the Mb has the same antigen specificity and binding affinity as the full-length antibody, the Mb does not activate or induce the proliferation of CD8-positive T cells.
zirconium Zr 89 girentuximab: A radioimmunoconjugate comprised of the recombinant chimeric monoclonal antibody girentuximab, that binds an extracellular epitope of carbonic anhydrase IX (CAIX), and labeled with the radioisotope zirconium 89 (Zr 89) with potential use as an imaging agent upon positron emission tomography (PET). The antibody moiety of zirconium Zr 89 girentuximab binds to CAIX expressed on tumor cells. Upon binding, the radioisotope moiety may be detected using PET, which enables the imaging and quantification of CAIX-expressing tumor cells. CAIX, a hypoxia-inducible transmembrane glycoprotein, is overexpressed on renal cell carcinoma (RCC) and various other tumors; it plays a key role in intra- and extracellular pH regulation, cancer cell progression, survival, migration and invasion.
zirconium Zr 89 panitumumab: A radioimmunoconjugate composed of panitumumab, a human immunoglobulin G2 (IgG2) monoclonal antibody directed against the epidermal growth factor receptor (EGFR; HER1; ErbB1), labeled with the radioisotope zirconium Zr 89, with potential use as an imaging agent upon positron emission tomography (PET). Upon administration of zirconium Zr 89 panitumumab, the antibody moiety targets and binds to the extracellular domain of EGFR on tumor cells. Upon PET imaging, EGFR-expressing tumor cells can be visualized and assessed. This allows quantification of EGFR-expressing tumor cells and may allow selection of patients that would respond to panitumumab therapy. EGFR, a receptor tyrosine kinase overexpressed on the cell surfaces of many tumor cell types, plays a key role in tumor cell proliferation.
zirconium Zr 89-anti-EGFR monoclonal antibody ABT-806: A radioimmunoconjugate composed of ABT-806, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the epidermal growth factor receptor (EGFR), labeled with the radioisotope zirconium Zr 89, with potential use as an imaging agent upon positron emission tomography (PET). Upon administration of zirconium Zr 89 anti-EGFR monoclonal antibody ABT-806, the antibody moiety binds to a specific EGFR epitope of either the wild-type or the variant III mutant (EGFRvIII; de2-7 EGFR; DEGFR) on tumor cells. Upon PET imaging, EGFR-expressing tumor cells can be visualized and assessed. This may result in the quantification of EGFR-expressing tumor cells, an assessment of the expected response to treatment with ABT-806 and the selection of patients that would respond to ABT-806. ABT-806 is the humanized version of chimeric monoclonal antibody 806. EGFR, a receptor tyrosine kinase overexpressed on the cell surfaces of many tumor cell types, plays a key role in tumor cell proliferation.
zirconium Zr 89-bevacizumab: A radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody bevacizumab labeled with the radioisotope zirconium Zr 89 (Zr 89) with radioisotopic activity and potential imaging use. The antibody moiety of zirconium Zr 89-bevacizumab targets and binds to the extracellular domain of the vascular endothelial growth factor receptor (VEGFR). Upon binding, the radioisotope moiety may be detected using positron emission tomography (PET), allowing the imaging and quantification of VEGFR-expressing tumor cells. VEGFR, a tyrosine kinase, is overexpressed on the cell surfaces of various tumor cell types.
zirconium Zr 89-cetuximab: A radioimmunoconjugate comprised of the recombinant chimeric monoclonal antibody cetuximab labeled with the radioisotope zirconium Z 89 (Zr 89) with radioisotopic activity and potential imaging use. The antibody moiety of zirconium Zr 89-cetuximab binds to the extracellular domain of the epidermal growth factor receptor (EGFR). Upon binding, the radioisotope moiety may be detected using positron emission tomography (PET), allowing the imaging and quantification of EGFR-expressing tumor cells. EGFR is a tyrosine kinase that may be overexpressed on the cell surfaces of various tumor cell types.
zirconium Zr 89-desferrioxamine B monoclonal antibody huJ591: A radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody J591 against prostate-specific membrane antigen (PSMA) conjugated to chelator desferrioxamine B (DFO-B) and labeled with the radioisotope zirconium Zr 89 with potential imaging property used in positron emission tomography (PET) imaging. Upon administration of zirconium Zr 89-desferrioxamine B monoclonal antibody huJ591, the antibody moiety binds to the extracellular domain of PSMA, and the radioisotope moiety may be detected using PET, thereby allowing the imaging and quantification of PSMA-expressing tumor cells. PSMA, or folate hydrolase is a cell surface peptidase highly expressed by malignant prostate epithelial cells and vascular endothelial cells of numerous solid tumor malignancies. In addition, upon PET imaging this agent provides high tumor:background tissue ratios.
zirconium Zr 89-Df-IAB2M: A radioimmunoconjugate comprised of an antibody fragment (IAB2M) against prostate-specific membrane antigen (PSMA), conjugated to the chelator desferrioxamine (Df) and labeled with the radioisotope zirconium Zr 89, with potential positron emission tomography (PET) imaging activity. Upon administration of zirconium Zr 89-Df-IAB2M, the antibody moiety binds to the extracellular domain of PSMA expressed on cancer cells. This may enable PET detection of the radioisotope moiety, and allows the imaging and quantification of PSMA-expressing tumor cells. PSMA is a cell surface peptidase highly expressed by malignant prostate epithelial cells and vascular endothelial cells in various solid tumor malignancies.
zirconium Zr 89-DFO-cRGDY PEG-Cy5-C' dots: A radioconjugate composed of a tumor-selective fluorescent imaging agent containing silica-based nanoparticles labeled with a near-infrared (NIR) fluorophore, cyanine 5 (Cy5), and surrounded by polyethylene glycol (PEG) chains attached to cyclic arginine-glycine-aspartic acid-tyrosine) (cyclo-(Arg-Gly-Asp-Tyr; cRGDY) peptides (C' dots; Cornell prime dots; cRGDY-PEG-C' dots), and linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential diagnostic properties upon positron emission tomography (PET) imaging. Upon intradermal administration of the zirconium Zr 89 cRGDY PEG-Cy5-C' dots, the cRGDY moiety selectively binds to alphaVbeta3 integrin expressed on tumor cells. Upon binding, the radioisotope moiety may be detected using PET, thereby allowing the imaging and quantification of integrin-expressing tumor cells as well as the visualization of the distribution, uptake and removal within tumor tissues. The fluorescence imaging agent is used to visualize alphaVbeta3-expressing tumor cells and assess the degree of both tumor metastasis and sentinel lymph node (SLN) trafficking. Integrins are transmembrane glycoproteins upregulated on proliferating tumor vessel endothelial cells and various cancer cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells, metastasis and an overall poor prognosis.
zirconium Zr 89-DFO-daratumumab: A radioimmunoconjugate containing daratumumab, a human immunoglobulin G1 kappa (IgG1k) monoclonal antibody directed against the cell surface glycoprotein CD38, and linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential diagnostic properties upon positron emission tomography (PET) imaging. Upon administration, the monoclonal antibody moiety of zirconium Zr 89-DFO-daratumumab specifically targets and binds to cell surface antigen CD38. Upon binding, the radioisotope moiety may be detected using PET, thereby allowing the imaging and quantification of CD38-expressing tumor cells. CD38, a cell surface glycoprotein, is expressed on various hematopoietic cells and is overexpressed on multiple myeloma (MM) cells.
zirconium Zr 89-DFO-emapalumab: A radioimmunoconjugate comprised of emapalumab, a human monoclonal antibody directed against the cytokine interferon-gamma (IFN-gamma; IFNg), linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential use as an imaging agent upon positron emission tomography (PET). Upon administration of Zr89-DFO-emapalumab, the emapalumab moiety specifically targets and binds to IFNg. Upon binding, the radioisotope moiety is detected using PET, thereby allowing the imaging of IFNg. This may help detect lesions and assess response to immunotherapeutic agents. IFNg, a cell-signaling protein, plays a key role in the regulation and activation of the immune system.
zirconium Zr 89-DFO-fianlimab: A radioimmunoconjugate consisting of fianlimab, a human monoclonal antibody directed against the inhibitory receptor lymphocyte activation gene-3 protein (LAG-3; LAG3; CD223), linked, via the chelator desferrioxamine (DFO), to the positron-emitting radionuclide zirconium Zr 89 (Zr89), with potential use as an imaging agent upon positron emission tomography (PET) imaging. Upon administration of zirconium Zr 89-DFO- fianlimab, the fianlimab moiety specifically targets and binds to LAG-3. Upon binding, the radioisotope moiety may be detected using PET, thereby allowing the imaging and quantification of LAG-3-expressing tumor infiltrating lymphocytes (TILs). LAG-3, a member of the immunoglobulin superfamily (IgSF), is expressed on various immune cells; its expression on TILs is associated with tumor-mediated immune suppression and the negative regulation of both cellular proliferation and T-cell activation.
zirconium Zr 89-DFO-REGN3504: A radioimmunoconjugate consisting of an antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential diagnostic properties upon positron emission tomography (PET) imaging. Upon administration, the antibody moiety of zirconium Zr 89-DFO-REGN3504 specifically targets and binds to PD-L1. Upon binding, the radioisotope moiety may be detected using PET, thereby allowing the imaging and quantification of PD-L1-expressing tumor cells. PD-L1, a transmembrane protein expressed on activated T cells, is overexpressed in some cancer types and plays a significant role in immune evasion by tumor cells.
zirconium Zr 89-DFO-SC16.56: A radioimmunoconjugate composed of SC16.56, a monoclonal antibody directed against the tumor-associated antigen (TAA) delta-like protein 3 (DLL3; delta like canonical notch ligand 3; drosophila delta homolog 3; delta3; delta-like 3; SCDO1), and linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential diagnostic properties upon positron emission tomography (PET) imaging. Upon administration of zirconium Zr 89-DFO-SC16.56, the monoclonal antibody moiety specifically targets and binds to DLL3. Upon binding, the radioisotope moiety is detected using PET, thereby allowing the imaging and quantification of DLL3-expressing tumor cells. DLL3, a Notch pathway protein, is overexpressed on a variety of cancer cell types. It plays a key role in embryonic development and in tumor initiation and proliferation.
zirconium Zr 89-DFO-starPEG: A radioconjugate containing starPEG, a 4-armed polyethylene glycol (PEG)-based nanodrug carrier moiety, linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential use as an imaging agent upon positron emission tomography (PET) imaging. Upon administration, starPEG is taken up by tumors due to enhanced permeability and retention (EPR) effect. Upon PET imaging, EPR-mediated tumor uptake and distribution of the nanodrug carrier may be visualized.
zirconium Zr 89-DFO-vandortuzumab vedotin: A radioimmunoconjugate composed of the radioisotope zirconium Zr 89 conjugated to an antibody that targets six transmembrane epithelial antigen of the prostate 1 (STEAP1) that can potentially be used as a prostate cancer tracer during positron emission tomography (PET). Upon administration of zirconium Zr 89-DFO-vandortuzumab vedotin, the antibody moiety DFO-vandortuzumab vedotin binds to STEAP1 on prostate cancer cells. In turn, Zr 89 allows for the visualization of those cells using PET. STEAP1, a six-transmembrane domain protein, is overexpressed on the surface of prostate cancer cells.
zirconium Zr 89-DFO-YS5: A radioimmunoconjugate containing YS5, a human immunoglobulin G1 (IgG1) monoclonal antibody directed against the cell surface antigen cluster of differentiation 46 (CD46; membrane cofactor protein; MCP), and linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential diagnostic properties upon positron emission tomography (PET) imaging. Upon administration, the monoclonal antibody moiety of zirconium Zr 89-DFO-YS5 specifically targets and binds to a conformational epitope formed within Sushi domains (complement control protein repeats; CCPs) 1 and 2 on the immune modulatory receptor CD46 expressed on certain tumor cells. Upon binding, internalization and PET, CD46-expressing tumor cells can be imaged and assessed. The conformational epitope on CD46 is highly expressed in multiple tumor cell types while minimally expressed or absent in normal, healthy tissues. CD46 plays a key role in the negative regulation of innate immunity.
zirconium Zr 89-labeled anti-CA19-9 monoclonal antibody 5B1: A radioimmunoconjugate comprised of the recombinant human monoclonal antibody against the carbohydrate antigen sialyl-Lewis a (carbohydrate antigen 19-9; CA19-9) conjugated to the chelator desferrioxamine (DFO) and labeled with the radioisotope zirconium Zr 89 (Zr 89), with radioisotopic activity and potential use as an imaging agent in positron emission tomography (PET). The antibody moiety of zirconium Zr 89 anti-CA19-9 monoclonal antibody 5B1 targets and binds to CA19-9 expressing-tumor cells. Upon binding, internalization and proteolysis, the radioisotope moiety may be detected using PET, thus allowing imaging and quantification of CA19-9-expressing tumor cells. CA19-9, overexpressed on a number of different tumor cell types, plays a key role in tumor cell survival and metastasis.
zirconium Zr 89-labeled anti-PIGF monoclonal antibody RO5323441: A radioimmunoconjugate comprised of the humanized IgG1 monoclonal antibody directed against placental growth factor (PlGF) and labeled with zirconium Zr 89 (Zr 89), with potential radiotracer activity upon positron emission tomography (PET) imaging. The monoclonal antibody moiety of RO5323441 binds to both PlGF-1 and -2, thereby preventing the binding of PlGF-1 and -2 to the vascular endothelial growth factor receptor-1 (VEGFR-1) and the subsequent activation of VEGFR-1. The radioisotope moiety of RO5323441 may be detected using PET, thereby allowing for visualization of the antibody’s distribution and PlGF expression. PlGF, a member of the VEGF sub-family and a key molecule in angiogenesis and vasculogenesis, is upregulated in many cancers.
zirconium Zr 89-labeled atezolizumab: A radioimmunoconjugate composed of atezolizumab, a humanized, Fc-optimized, monoclonal antibody directed against programmed cell death-1 ligand 1 (PD-L1) and labeled with the radioisotope zirconium Zr 89, with potential use for assessing PD-L1-expressing tumor cells using positron emission tomography (PET). Upon administration of zirconium Zr 89-labeled atezolizumab, the antibody moiety targets and binds to PD-L1. Following tumor cell uptake, the radioisotope moiety can be visualized using PET. This may result in the quantification of PD-L1-expressing tumor cells, an assessment of the expected response to treatment with atezolizumab as well as selection of patients that would respond to atezolizumab. PD-L1 is overexpressed on many human cancer cell types; PD-L1 binding to programmed cell death 1 (PD-1) on T-cells suppresses the immune system and results in increased immune evasion.
zirconium Zr 89-labeled monoclonal antibody MMOT0530A: A radioimmunoconjugate composed of a monoclonal antibody that targets an antigen overexpressed in pancreatic and ovarian cancer and labeled with the radioisotope zirconium Zr 89, with potential use for assessing tumor antigen expression using positron emission tomography (PET). Upon administration of zirconium Zr 89-labeled monoclonal antibody MMOT0530A, this agent targets an antigen expressed on certain tumor cells and is internalized. Following tumor cell uptake, the radioisotope moiety can be visualized using PET imaging. This may result in both the quantification of tumor antigen expression and an assessment of the response to treatment with therapeutics targeting the antigen.
zirconium Zr 89-labeled RO5479599: A radioimmunoconjugate containing a glycoengineered, humanized monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3) and labeled with the radioisotope zirconium Zr 89, with radioisotopic activity and potential use as an imaging agent as well as potential antineoplastic activity. Upon administration, the RO5479599 moiety of zirconium Zr 89-labeled RO5479599 binds to the extracellular domain of HER3 and inhibits HER3 dimerization, thereby preventing EGFR-dependent signaling. In addition, RO5479599 elicits enhanced antibody-dependent cellular cytotoxicity (ADCC). Upon binding, the radioisotope moiety may be detected using positron emission tomography (PET), thereby allowing the imaging and quantification of HER3-expressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors; it has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.
zirconium Zr 89-nanocolloidal albumin: A radioimmunoconjugate composed of a nanoformulation of colloidal human serum albumin (HSA) labeled with zirconium Zr 89 (Zr89), via the bifunctional chelate p-isothiocyanatobenzyl-desferrioxamine B, with potential imaging activity using positron emission tomography (PET). Upon administration, the zirconium Zr 89-nanocolloidal albumin travels through the bloodstream and into the lymphatic system. Using PET, the draining pattern of the lymph nodes can be visualized and lymph node status, including that of the sentinel lymph node (SLN), can be detected and analyzed. Compared to some other formulations, the smaller particle size of nanocolloidal albumin allows for enhanced imaging of the lymphatic system.
zirconium Zr 89-pembrolizumab: A radioimmunoconjugate composed of pembrolizumab, a humanized monoclonal antibody immunoglobulin (Ig) G4 antibody directed against the human cell surface receptor programmed cell death 1 (PD-1; PDCD1; CD279; programmed cell death-1), labeled with the radioisotope zirconium Zr 89, with potential use as an imaging agent upon positron emission tomography (PET). Upon administration of zirconium Zr 89 pembrolizumab, the antibody moiety binds to PD-1, an inhibitory signaling receptor expressed on the surface of activated T cells, and blocks the binding to and activation of PD-1 by its ligands. Upon PET imaging, PD-1-expressing T cells, as well as pembrolizumab biodistribution, can be visualized and the expected response to treatment with pembrolizumab, as well as selection of patients that would respond to pembrolizumab, can be assessed. The ligands for PD-1 include programmed cell death-1 ligand 1 (PD-L1), which is overexpressed on certain cancer cells, and programmed cell death-1 ligand 2 (PD-L2), which is primarily expressed on antigen-presenting cells (APCs). Activated PD-1 negatively regulates T-cell activation and plays a key role in tumor evasion from host immunity.
zirconium Zr 89-pertuzumab: A radioimmunoconjugate composed of pertuzumab, a humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the tyrosine kinase receptor human epidermal growth factor-2 (HER2; HER-2), and linked, via the chelator desferrioxamine (DFO), to the radioisotope zirconium Zr 89 (Zr89), with potential use in imaging of HER-2-expressing tumor cells upon positron emission tomography (PET). Upon administration of zirconium Zr 89-DFO-pertuzumab, the pertuzumab moiety targets and binds to HER-2. After binding and internalization into HER-2-expressing tumor cells, Zr89 facilitates the visualization and detection of HER-2-expressing tumor cells using PET. This assesses HER2-expression and may predict or evaluate the tumor's response to certain HER-2-targeting chemotherapeutics.
zirconium Zr 89-ss-pertuzumab: A radioimmunoconjugate composed of pertuzumab, a humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the tyrosine kinase receptor human epidermal growth factor-2 (HER2; HER-2), and linked, using a site-specific bioconjugation method, to the radioisotope zirconium Zr 89 (Zr89), with potential use in the imaging of HER-2-expressing tumor cells upon positron emission tomography (PET). Upon administration of zirconium Zr 89-ss-pertuzumab, the pertuzumab moiety targets and binds to HER-2. After binding and internalization into HER-2-expressing tumor cells, Zr89 facilitates the visualization and detection of HER-2-expressing tumor cells using PET. This assesses HER2-expression and may predict or evaluate the tumor's response to certain HER-2-targeting chemotherapeutics. Site-specific bioconjugation may produce better defined and more homogeneous radioimmunoconjugates.
zirconium Zr 89-TAK-164: A radioimmunoconjugate composed of TAK-164, an antibody-drug conjugate (ADC) comprised of a full-length, human immunoglobulin G1 (IgG1) monoclonal antibody (mAb) directed against the extracellular domain of guanylyl cyclase C (GCC; GUCY2C) conjugated to the DNA alkylator DGN549 (IGN-P1), and linked to the radioisotope zirconium Zr 89 (Zr89), with potential use in imaging of GCC-expressing tumor cells upon positron emission tomography (PET). Upon administration of zirconium Zr 89-TAK-164, the TAK-164 moiety targets and binds to GCC. After binding, Zr89 facilitates the visualization and detection of GCC-expressing tumor cells using PET. This assesses GCC-expression and may predict or evaluate the tumor's response to TAK-164.
zirconium Zr 89-trastuzumab: A radioimmunoconjugate containing the recombinant humanized monoclonal antibody trastuzumab labeled with the radioisotope zirconium Zr 89 with radioisotopic activity and potential use as an imaging agent. The trastuzumab moiety of zirconium Zr 89-trastuzumab binds with high affinity to the extracellular domain of human epidermal growth factor receptor 2 (HER2). Upon binding, the radioisotope moiety may be detected using positron emission tomography (PET), thereby allowing the imaging and quantification of HER2-expressing tumor cells. HER2, a tyrosine kinase client protein of heat shock protein 90 (Hsp90), may be overexpressed on the cell surfaces of various tumor cell types.
Zithromax: (Other name for: azithromycin)
ziv-aflibercept: A recombinant protein comprised of epitopes of the extracellular domains of human vascular endothelial growth factor receptors (VEGFR) fused to the constant region (Fc) of human IgG1 with potential antiangiogenic activity. Afilbercept, functioning as a soluble decoy receptor, binds to pro-angiogenic vascular endothelial growth factors (VEGFs), thereby preventing VEGFs from binding to their endogenous receptors. Disruption of the binding of VEGFs to their cellular receptors may result in the inhibition of tumor angiogenesis, metastasis, and ultimately tumor regression.
Ziverel: (Other name for: hyaluronic acid/chondroitin sulfate/poloxamer 407 oral solution)
Zocor: (Other name for: simvastatin)
ZoDex: (Other name for: dexamethasone)
Zofran: (Other name for: ondansetron hydrochloride)
Zofran: (Other name for: ondansetron)
Zofran ODT: (Other name for: ondansetron)
Zoladex: (Other name for: goserelin acetate)
zolbetuximab-clzb: A chimeric immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) Claudin18.2 (CLDN18.2; A2 isoform of claudin-18), with potential immunostimulating and antineoplastic activities. Upon administration, zolbetuximab-clzb specifically targets and binds to CLDN18.2 expressed on tumor cells. This may kill CLDN18.2-expressing tumor cells by antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), and inhibit cell proliferation. 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.
zoldonrasib: An orally bioavailable covalent tri-complex inhibitor of the oncogenic KRAS substitution mutation G12D, with potential antineoplastic activity. Upon oral administration, zoldonrasib specifically targets and non-covalently binds to cyclophilin A to form a non-covalent binary complex, which subsequently covalently and irreversibly binds to the active GTP-bound form of KRAS G12D (KRASG12D(ON)). This prevents KRAS G12D-mediated signaling and activation of downstream survival pathways. This causes apoptosis in KRAS G12D-expressing tumor cells. In addition, inhibition of KRAS G12D signaling by zoldonrasib abrogates the suppressive tumor microenvironment (TME) and enhances an anti-tumor immune response which further leads to an inhibition of proliferation of KRAS G12D-expressing tumor cells. 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 proliferation, invasion, and metastasis.
zoledronate disodium: The disodium salt form of zoledronate, a synthetic imidazole, third generation bisphosphonate analog of pyrophosphate with antiresorptive activity. Zoledronate binds to hydroxyapatite crystals in the bone matrix and inhibits farnesyl pyrophosphate (diphosphate) synthase, thereby preventing protein prenylation within the mevalonate pathway. This leads to the loss of downstream metabolites essential for osteoclast function, leading to the induction of apoptosis and eventually, osteoclast-cell death. By preventing osteoclast-mediated bone resorption, zoledronate decreases bone turnover and stabilizes the bone matrix.
zoledronic acid: A synthetic imidazole bisphosphonate analog of pyrophosphate with anti-bone-resorption activity. A third-generation bisphosphonate, zoledronic acid binds to hydroxyapatite crystals in the bone matrix, slowing their dissolution and inhibiting the formation and aggregation of these crystals. This agent also inhibits farnesyl pyrophosphate synthase, an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids, donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which are important in the process of osteoclast turnover. Decreased bone turnover and stabilization of the bone matrix contribute to the analgesic effect of zoledronic acid with respect to painful osteoblastic lesions. The agent also reduces serum calcium concentrations associated with hypercalcemia.
zoligratinib: An orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity. Zoligratinib binds to and inhibits FGFR-1, -2, and -3, which result in the inhibition of FGFR-mediated signal transduction pathways. This leads to the inhibition of both tumor cell proliferation and angiogenesis, and causes cell death in FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, is essential for tumor cellular proliferation, differentiation and survival.
Zolinza: (Other name for: Vorinostat)
zolmitriptan: A member of the triptan class agents with anti-migraine property. Zolmitriptan selectively binds to and activates serotonin (5-HT) 1B expressed in intracranial arteries and 5_HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei. Receptor binding results in constriction of cranial vessels, reduction of the vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relief migraine headaches by inhibition pro-inflammatory neuropeptide release.
Zoloft: (Other name for: sertraline hydrochloride)
zolpidem tartrate: The tartrate salt of an imidazopyridine with non-benzodiazepine benzodiazepine-receptor agonist and sedative-hypnotic activities. Zolpidem binds selectively to the alpha 1 subunit of the omega-1 (BZ1) receptor of the gamma-aminobutyric acid type A (GABA-A ) receptor-chloride ionophore complex, thereby opening neuronal chloride channels, hyperpolarizing neuronal cell membranes, and inhibiting neuronal firing. In contrast, benzodiazepines non-selectively bind to and activate all omega receptor subtypes, exhibiting anticonvulsant and myorelaxant activities in addition to a sedative-hypnotic activity.
Zometa: (Other name for: zoledronic acid)
Zomig: (Other name for: zolmitriptan)
zongertinib: An orally bioavailable inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential antineoplastic activity. Upon oral administration, zongertinib covalently binds to and inhibits the activity of both wild-type and HER2 mutants, including HER2 mutants with exon 20 insertion (ex20ins) mutations. This prevents HER2-mediated signaling and may lead to cell death in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase overexpressed on a variety of tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization.
zopiclone: The racemic form of a nonbenzodiazepine, cyclopyrrolone with hypnotic and sedative activity and without significant anxiolytic activity. Although the exact mechanism of action remains to be fully elucidated, zopiclone is able to bind to and activate the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization, inhibition of neuronal firing, and enhancement of the inhibitory effect of GABA. This eventually leads to a hypnotic effect and allows for an induction of sleep.
zoptarelin doxorubicin: A peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Zoptarelin doxorubicin binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates into DNA and inhibits the topoisomerase II activity, which may result in the inhibition of tumor cell DNA replication and tumor cell proliferation.
Zortress: (Other name for: everolimus)
zorubicin hydrochloride: A benzoyl-hydrazone derivative of the anthracycline antineoplastic antibiotic daunorubicin. Zorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.
Zostavax: (Other name for: varicella zoster virus strain Oka/Merck live antigen)
zoster vaccine recombinant, adjuvanted: A recombinant, subunit herpes zoster (HZ) vaccine containing varicella-zoster virus (VZV) glycoprotein E (gE), that can potentially be used to prevent HZ infection, also called shingles. Upon administration, zoster vaccine recombinant, adjuvanted stimulates the host immune system to induce both specific CD4-positive T-cells and antibodies against VZV gE, thereby protecting against infection with HZ. VZV gE, the most common antigen in VZV viral particles, plays a key role in VZV infection. Compared to live-attenuated vaccines, the subunit vaccine prevents the risk of vaccine-induced HZ in immunocompromised patients.
zosuquidar trihydrochloride: A difluorocyclopropyl quinoline. Zosuquidar trihydrochloride binds with high affinity to P-glycoprotein and inhibits P-glycoprotein-mediated multidrug resistance (MDR). P-glycoprotein, encoded by the MDR-1 gene, is a member of the ATP-binding cassette superfamily of transmembrane transporters and prevents the intracellular accumulation of many natural product-derived cytotoxic agents.
zotatifin: A selective inhibitor of the eukaryotic translation initiation factor 4A (eIF4A), with potential antineoplastic activity. Upon administration of zotatifin, this agent targets and binds to elF4A, and promotes eIF4A binding to mRNA with specific polypurine motifs within their 5'-untranslated region (5'-UTR), leading to the formation of a stable sequence-specific ternary complex with eIF4A and mRNA (elF4A- zotatifin-mRNA). This results in the translational repression of key oncogenes and anti-apoptotic proteins involved in tumor cell proliferation, survival and metastasis, such as KRAS, Myc, myeloid cell leukemia-1 (Mcl-1), B-cell lymphoma 2 (Bcl-2), cyclin-dependent kinase (CDK) 4 and 6, cyclin D, fibroblast growth factor receptor (FGFR) 1 and 2, human epidermal growth factor receptor 2 (HER2; ERBB2), and beta-catenin. The inhibition of the expression of these oncogenes leads to the inhibition of various oncogenic signal transduction pathways. This inhibits proliferation and induces apoptosis in tumor cells. eIF4A, a RNA helicase and the rate-limiting component of the eukaryotic translation initiation complex, catalyzes the ATP-dependent unwinding of RNA duplexes and facilitates 43S ribosome scanning within the 5'-UTR. elF4A is activated by various oncogenic signaling pathways, including RAS/mitogen-activated protein kinase (MAPK) and phosphatidylinositide 3-kinase (PI3K)/AKT pathways, and regulates the translation of oncogenes and tumor survival factors with complex secondary structures within the 5'-UTRs that are required for tumor cell proliferation, survival and metastasis.
zotiraciclib citrate: An orally bioavailable citrate salt form of zotiraciclib a multi-kinase inhibitor for cyclin dependent kinase (CDK) subtypes 1, 2, 7 and 9, Janus-associated kinase 2 (JAK2), FMS-related tyrosine kinase 3 (FLT3, FLK2, STK1), with potential antineoplastic activity. Upon oral administration, CDK/JAK2/FLT3 Inhibitor TG02 binds to and inhibits the CDK subtypes, JAK2, and FLT3. TG02 also inhibits, to a lesser extent, TYK2, TYRO3, STAT5 and P38delta. This may result in both an induction of apoptosis and an inhibition of tumor cell proliferation in cancer cells that overexpress these kinases. JAK2, often upregulated or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key role in tumor cell proliferation and survival. CDKs are serine/threonine kinases that play key roles in the regulation of the cell cycle and cellular proliferation. FLT3, a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias.
zotizalkib: An orally available, compact macrocyclic structure-based inhibitor of the receptor tyrosine kinase (RTK) anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon oral administration, zotizalkib binds within the ATP binding boundary and inhibits ALK wild-type tyrosine kinase, ALK fusion proteins and numerous ALK point mutations, including acquired resistance mutations, such as the solvent front mutation (SFM) G1202R and compound mutations L1196M/G1202R, L1198F/G1202R, L1196M/L1198F, and C1156Y/G1202R. Inhibition of ALK leads to the disruption of ALK-mediated signaling and the inhibition of cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK is not expressed in healthy adult human tissue but ALK dysregulation and gene rearrangements are associated with a variety of tumor cell types. Compared to other ALK inhibitors, zotizalkib is able to inhibit ALK resistance mutations associated with acquired resistance to other ALK inhibitors.
Zovirax: (Other name for: acyclovir)
Zovirax for Injection: (Other name for: Acyclovir Sodium)
Ztalmy: (Other name for: ganaxolone)
zunsemetinib: An orally bioavailable, small molecule inhibitor of mitogen-activated protein (MAP) kinase-activated protein kinase 2 (MAPKAPK2; MK2), with potential anti-inflammatory activity. Upon oral administration, zunsemetinib targets and binds to the p38MAPK-MK2 complex, thereby inhibiting the p38MAPK phosphorylation and activation of MK2. This inhibits p38MAPK/MK2-mediated inflammatory signaling pathway. This may result in the inhibition of the production of proinflammatory cytokines, including tumor necrosis factor-alpha (TNF-alpha), interleukin (IL)-1-alpha, IL-1-beta and IL-6.
Zuplenz: (Other name for: ondansetron)
Zyban: (Other name for: bupropion hydrochloride)
Zyban: (Other name for: bupropion hydrochloride controlled-release)
Zybrestat: (Other name for: fosbretabulin tromethamine)
ZYBRESTAT: (Other name for: fosbretabulin disodium)
ZYC300: A plasmid DNA encoding an inactivated form of the carcinogen activator cytochrome P450 1B1 (CYP1B1) encapsulated in biodegradable poly-DL-lactide-coglycolide microparticles with potential antineoplastic activity. Vaccination with ZYC300 may stimulate the immune system to elicit a cytotoxic T lymphocyte (CTL) response against the tumor-associated antigen (TAA) CYP1B1, which may result in the lysis of tumor cells expressing CYP1B1. CYP1B1, an extrahepatic monooxygenase of the cytochrome P450 family, is overexpressed in many cancers with only restricted expression in normal tissues.
Zyclara: (Other name for: imiquimod)
Zydelig: (Other name for: idelalisib)
Zyflo: (Other name for: zileuton)
Zykadia: (Other name for: ceritinib)
Zyloprim: (Other name for: allopurinol sodium)
Zymase: (Other name for: pancrelipase)
zymosan: An insoluble beta-1,3-glucan polysaccharide derived from, and structural component of, yeast cell walls, with potential immunostimulating activity. Upon administration, zymosan targets, binds to and activates certain Toll-like receptors, primarily TLR type 2 (TLR-2), on leukocytes and dectin-1 on macrophages. Activation of TLR2 and dectin-1 stimulates the release of pro-inflammatory mediators, and enhances innate immune responses.
Zynlonta: (Other name for: loncastuximab tesirine-lpyl)
Zynteglo: (Other name for: betibeglogene autotemcel)
Zynyz: (Other name for: retifanlimab-dlwr)
Zyprexa: (Other name for: olanzapine)
Zyprexa Zydis: (Other name for: olanzapine)
Zytiga: (Other name for: abiraterone acetate)
Zyvox: (Other name for: linezolid)