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Antineoplastic agents xyz

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  • Xanthohumol - A prenylated flavonoid derived from the female flowers of the hops plant (Humulus lupulus L), with potential chemopreventive and antineoplastic activities. Upon administration, xanthohumol scavenges reactive oxygen species (ROS), thereby preventing DNA damage due to oxidative stress. In addition, xanthohumol is able to increase the expression of phase II cytoprotective enzymes, thereby inactivating carcinogens. This agent exerts anti-inflammatory activity, through the inhibition of inflammation-inducing enzymes, inhibits DNA synthesis, and induces apoptosis of susceptible cancer cells. Xanthohumol also decreases the expression of C-X-C chemokine receptor 4 (CXCR4), thereby preventing cancer cell invasion.
  • Xbp1-us/xbp1-sp/cd138/cs1 multipeptide vaccine pvx-410 - A cancer vaccine containing immunogenic, HLA-A2-specific epitopes derived from X-box-binding protein 1-unspliced (XBP1-US), XBP1-spliced (SP), syndecan-1 (CD138), and CS1 (CD2 subset 1, CRACC, SLAMF7, CD319) with potential immunomodulating and antineoplastic activities. Upon subcutaneous administration, XBP1-US/XBP1-SP/CD138/CS1 multipeptide vaccine PVX-410 may stimulate the immune system to induce a cytotoxic T-lymphocyte response against the four myeloma-specific antigens. The tumor associated antigens (TAAs) XBP1-US, XBP1-SP, CD138 and CS1, are overexpressed on the surface of multiple myeloma (MM) cells.
  • Xenogeneic tyrosinase dna vaccine - A plasmid DNA vaccine, encoding an epitope of mouse tyrosinase, with potential antineoplastic activity. Administered via intramuscular electroporation, vaccination with xenogeneic tyrosinase DNA vaccine may induce both humoral and cytotoxic lymphocyte (CTL) immune responses against melanoma cells that express tyrosinase, resulting in decreased tumor growth.
  • Xentuzumab - A humanized IgG1 insulin-like growth factor (IGF) monoclonal antibody targeting the IGF ligands 1 (IGF-1) and 2 (IGF-2), with potential antineoplastic activity. Upon administration, xentuzumab binds to both IGF-1 and IGF-2 and inhibits the binding of these ligands to their receptor, IGF-1R. This blocks the insulin growth factor (IGF) signaling pathway, which is upregulated in a number of cancer cell types and plays a key role in cancer cell proliferation and chemoresistance. In addition, BI 836845 prevents the binding of IGF-2 to insulin receptor variant A (IR-A), preventing its activation.
  • Xevinapant - An orally available mimetic of the natural second mitochondrial-derived activator of caspases (Smac) and inhibitor of Inhibitor of Apoptosis Proteins (IAPs), with potential immunomodulating, apoptotic-inducing, chemo-radio-sensitizing and antineoplastic activities. Upon oral administration,xevinapant targets and binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP), and the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2). This inhibits the activities of these IAPs and promotes the induction of apoptosis. Additionally, as xevinapant inhibits the activity of IAPs, it may work synergistically with cytotoxic drugs and/or radiation to overcome tumor cell resistance to apoptosis. As IAPs regulate nuclear factor-kappa B (NFkB) signaling pathways, which drives the expression of genes involved in immune and inflammatory responses, xevinapant may enhance anti-tumor immune responses when administered with certain immunomodulating agents, such as immune checkpoint inhibitors. IAPs are overexpressed by many cancer cell types and suppress both intrinsic and extrinsic apoptosis by binding to and inhibiting active caspases via their baculoviral lAP repeat (BIR) domains. They contribute to chemo-radio-resistance of cancer cells to certain cytotoxic agents and radiation, promote tumor cell survival and are associated with poor prognosis in certain types of cancer. SMAC, a pro-apoptotic mitochondrial protein, is an endogenous inhibitor of the IAPs family of cellular proteins.
  • Xiaoai jiedu decoction - A traditional Chinese medicine (TCM) decoction composed of Oldenlandia, Kuh-seng, Codonopsis pilosula, bighead atractylodes rhizome, smoked plum, the rhizome of Chinese goldthread, rhizome zingiberis preparata and semen Coicis, with potential chemopreventive and antineoplastic activities. Upon administration of Xiaoai Jiedu decoction, the active ingredients in this decoction may inhibit a variety of signal transduction pathways involved in carcinogenesis. This may induce cell cycle arrest and tumor cell apoptosis and inhibit tumor cell formation and proliferation.
  • Xiap antisense oligonucleotide aeg35156 - A second-generation synthetic antisense oligonucleotide with potential antineoplastic activity. AEG35156 selectively blocks the cellular expression of X-linked inhibitor of apoptosis protein (XIAP), a pivotal inhibitor of apoptosis that is overexpressed in many tumors. This agent reduces total levels of XIAP in tumor cells, working synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. XIAP interferes with both the intrinsic and extrinsic program-death signaling pathways, which may render tumor cells resistant to apoptosis.
  • Xiap/ciap1 antagonist astx660 - An orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptotic activities. Upon administration, XIAP/cIAP1 antagonist ASTX660 selectively binds to and inhibits the activity of XIAP and cIAP1. This restores and promotes the induction of apoptotic signaling pathways in cancer cells, and inactivates the nuclear factor-kappa B (NF-kB)-mediated survival pathway. XIAP and cIAP1 are overexpressed by many cancer cell types and suppress apoptosis by inhibiting the activity of certain caspases; they promote both cancer cell survival and chemotherapy resistance.
  • Xiliertinib - An orally available, ATP-competitive inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, xiliertinib binds to and inhibits the activity of EGFR. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • Xisomab 3g3 - A humanized anti-factor XI (FXI) antibody, with potential anti-thrombotic activity. Upon administration, xisomab 3G3 targets and binds to the apple 2 domain of FXI, thereby preventing the binding of FXI to factor XIIa (FXIIa). This blocks factor XIIa-mediated FXI activation without inhibiting FXI activation by thrombin or the procoagulant function of FXIa. The abrogation of FXI activation prolongs the activated partial thromboplastin time (aPTT), and reduces platelet and fibrin accumulation. This results in the inhibition of contact activation-initiated blood coagulation and prevents thrombus formation. FXI contributes to thrombotic disease while playing a limited role in normal hemostasis. Activation of FXI is essential for thrombus growth and stabilization.
  • Xpo1 inhibitor sl-801 - An orally bioavailable inhibitor of the nuclear export protein exportin-1 (XPO1; chromosome region maintenance 1 protein homolog; CRM1), with potential antineoplastic and pro-apoptotic activities. Upon administration, XPO1 inhibitor SL-801 reversibly binds to the cargo binding site of XPO1, and prevents the XPO1-mediated nuclear export of cargo proteins, including tumor suppressor proteins (TSPs), such as p53, FOXO, p21, and p27, and leads to their selective accumulation in the nuclei of tumor cells. As a selective inhibitor of nuclear export (SINE), SL-801 restores the nuclear localization and function of TSPs, which leads to the induction of apoptosis in tumor cells. XPO1, the major export factor that transports proteins and RNA from the nucleus to the cytoplasm, is overexpressed in a variety of cancer cell types while minimally expressed in normal, healthy cells. The dysregulated export of TSPs into the cytoplasm prevents TSP-initiated apoptosis. XPO1 overexpression leads to uncontrolled tumor cell proliferation and is associated with poor prognosis.
  • Y 90 monoclonal antibody cc49 - A radioimmunoconjugate of the humanized monoclonal antibody (MoAb) CC49 labeled with Yttrium 90 (Y-90). MoAb CC49 recognizes the pancarcinoma tumor-associated glycoprotein (TAG)-72 with high affinity. Y-90 MoAb CC49 delivers beta particles emitting Y-90 radionuclide directly to tumor cells that express TAG-72, thereby this agent may be used in radioimmunotherapeutic treatment of cancers.
  • Y 90 monoclonal antibody hmfg1 - A radioimmunoconjugate consisting of HMFG1, a humanized monoclonal antibody directed against the tumor associated antigen mucin-1 (MUC-1), labeled with the beta-emitting radioisotope yttrium 90 (Y-90), with potential antineoplastic activities. Upon administration, the monoclonal antibody moiety targets and binds to MUC-1 on the surface of certain tumor cells. Upon binding and internalization, pemtumomab and delivers a cytotoxic dose of beta radiation to MUC1-expressing tumor cells. MUC1, a glycoprotein overexpressed on the surface of a variety of cancer cells, plays a key role in tumor cell survival and proliferation.
  • Y 90 monoclonal antibody lym-1 - A radioimmunoconjugate of a murine monoclonal antibody, MoAb Lym-1, labeled with yttrium 90 (Y-90). MoAb Lym-1 recognizes an epitope of the histocompatibility antigen HLA-DR, which is over-expressed on most B-cell lymphomas. Y-90 MoAb Lym-1 delivers Y-90 radionuclide directly to tumor cells that express HLA-DR antigen, thereby this agent may be used in radioimmunotherapy of cancers.
  • Y 90 monoclonal antibody m170 - A radioimmunoconjugate of m170 monoclonal antibody (MoAb) conjugated with isotope yttrium 90. MoAb m170 is a murine MoAb that recognizes MUC-1 antigen present on the surface of many adenocarcinomas. This radioimmunoconjugate emits beta particles that cause cytotoxicity in tumor cells and has both imaging and therapeutic uses.
  • Y 90 monoclonal antibody m195 - A radioimmunoconjugate of humanized M195 monoclonal antibody (MoAb) conjugated with isotope yttrium 90. MoAb M195 is reactive with the cell surface antigen CD33, a glycoprotein found on myeloid leukemia blasts and early hematopoietic progenitor cells but not on normal stem cells. This radioimmunoconjugate emits beta particles that causes cytotoxicity in tumor cells and has both imaging and therapeutic uses.
  • Yang yin fu zheng - A traditional Chinese medicine (TCM)-based formulation, with potential immuno-enhancing, detoxifying and antineoplastic activities. Upon administration, Yang Yin Fu Zheng may activate the immune system and may help inhibit tumor cell proliferation. This TCM may also help remove toxic substances.
  • Yangzheng xiaoji extract - A traditional Chinese medicine (TCM)-based formulation containing the Yangzheng Xiaoji (YZXJ) extract, consisting of various components, with potential antineoplastic and anti-angiogenic activities. Some of the main components in Yangzheng Xiaoji are Radix Astragali, Fructus Ligustri Lucidi, Radix Ginseng, Ganoderma, Rhizoma Curcumac, Fried Rhizoma Atractylodis, Macrocephalae and Herba Hedyotidis. Although the exact mechanism(s) through which Yangzheng Xiaoji exerts its effects have yet to be fully elucidated, this agent, upon administration, inhibits the activation of various signaling protein kinases, such as focal adhesion kinase (FAK) and paxillin. This prevents signal transduction pathways that are upregulated in cancer, prevents the adhesion and migration of tumor cells and inhibits tumor cell growth.
  • Yiqi-yangyin-jiedu herbal decoction - A traditional Chinese medicine (TCM) based formulation consisting of milkvetch root, glehnia root, asparagus root, lilyturf root, grossy privet fruit, spikemoss herb, Chinese sage herb, and manyleaf paris rhizome, with potential immuno-enhancing, detoxifying and antineoplastic activities. Upon administration, yiqi-yangyin-jiedu decoction (YYJD) may activate the immune system by enhancing T-lymphocyte activity, and inhibiting tumor cell proliferation. YYJD may also ameliorate the qi-yin deficiency syndrome by strengthening qi and nourishing yin. YYJD may help remove toxic substance.
  • Young autologous tumor-infiltrating lymphocytes - A preparation of autologous young tumor infiltrating lymphocytes (TILs), that are isolated from the patient's tumor tissue and minimally cultured ex vivo, with potential antineoplastic and immunomodulating activities. Upon re-administration of the young TILs, the TILs re-infiltrate the tumor, recognize the tumor cells and initiate tumor cell lysis. This inhibits tumor cell growth.
  • Yttrium y 90 anti-cd19 monoclonal antibody bu12 - A radioimmunoconjugate consisting of the murine IgG1 anti-CD19 monoclonal antibody (MoAb) BU12 labeled with the beta-emitting radioisotope yttrium Y 90 with radioisotopic and antibody activities. Yttrium Y 90 anti-CD19 monoclonal antibody BU12 binds to the CD19 molecule, specifically delivering cytotoxic beta radiation to CD19-expressing B cells. CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.
  • Yttrium y 90 anti-cd45 monoclonal antibody ahn-12 - A radioimmunoconjugate comprised of the monoclonal antibody AHN-12 conjugated to the radioisotope yttrium 90 with potential radioimmunotherapeutic activity. Yttrium Y 90 monoclonal antibody AHN-12 binds to the tyrosine phosphatase CD45, expressed on the surface of normal and malignant hematopoietic cells. After binding and internalization by CD45-expressing tumor cells, this agent may deliver a cytotoxic dose of beta radiation.
  • Yttrium y 90 anti-cd45 monoclonal antibody bc8 - A radioimmunoconjugate containing the murine IgG1 anti-CD45 monoclonal antibody (MoAb) BC8 labeled with yttrium 90 (Y90), with potential immunotherapeutic activity. Yttrium Y 90 anti-CD45 monoclonal antibody BC8 binds to CD45 antigen, a receptor protein-tyrosine phosphatase expressed on the surface of both normal and malignant hematopoietic cells. After binding and internalization by CD45-expressing tumor cells, this agent may deliver a cytotoxic dose of beta radiation.
  • Yttrium y 90 anti-cdh3 monoclonal antibody ff-21101 - A radioimmunoconjugate consisting of a chimeric monoclonal antibody targeting human cadherin-3 (CDH3) and labeled, via the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), with the beta-emitting radioisotope yttrium Y 90, with potential antineoplastic activities. Upon administration, the antibody moiety of yttrium Y 90 anti-CDH3 monoclonal antibody FF-21101 binds to CDH3 expressed on tumor cells, thereby specifically delivering cytotoxic beta radiation to CDH3-expressing tumor cells. CDH3, also known as P-cadherin, is a tumor-associated antigen (TAA) and member of the cadherin family; it is overexpressed in a variety of tumors and plays a role in cell adhesion, motility, invasion, and proliferation.
  • Yttrium y 90 anti-cea monoclonal antibody ct84.66 - A radioimmunoconjugate comprised of a chimeric monoclonal antibody against human carcinoembryonic antigen (CEA) conjugated with the radioisotope yttrium 90 (Y-90) via the chelator tetra-azacyclododecanetetra-acetic acid (DOTA) with potential antineoplastic activity. The antibody moiety of yttrium Y90 DOTA anti-CEA monoclonal antibody cT84.66 binds to cells expressing the CEA antigen. Upon cellular internalization, this agent selectively delivers a cytotoxic dose of beta radiation. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers.
  • Yttrium y 90 basiliximab - A radioimmunoconjugate composed of basiliximab, a chimeric, mouse-human monoclonal antibody directed against the alpha subunit of interleukin-2 receptor (IL-2R alpha, CD25 or Tac antigen), and labeled with yttrium y 90, with potential antineoplastic activity. The basiliximab moiety of yttrium Y 90 basiliximab selectively binds to IL-2R alpha expressed on the surface of activated T-lymphocytes, thereby preventing IL-2 binding and blocking the IL-2-mediated activation of lymphocytes. The yttrium y 90 moiety selectively delivers a cytotoxic dose of beta radiation to lymphocytes that express the IL-2 receptor. This may prevent T cell-mediated activation of the immune system against a certain transplant and may prevent transplant rejection.
  • Yttrium y 90 colloid - An injectable, colloidal formulation of the radioisotope yttrium Y 90, with potential antineoplastic activity. When injected into the tumor, the yttrium Y 90 colloid selectively delivers a cytotoxic dose of beta-emitting yttrium Y 90 to the tumor site, which may result in both tumor cell death and tumor regression.
  • Yttrium y 90 daclizumab - A synthetic radioimmunoconjugate comprised of a humanized anti-interleukin-2 (IL-2) antibody linked to the radioisotope Yttrium 90 with potential antineoplastic activity. Daclizumab binds with high affinity to the Tac (also called CD25) subunit of the IL-2 receptor complex and inhibits the binding of IL-2, thereby blocking the IL-2-mediated activation of lymphocytes. As Yttrium Y 90 daclizumab, daclizumab delivers radiation specifically to lymphocytes that express the IL-2 receptor.
  • Yttrium y 90 dota anti-cea monoclonal antibody m5a - A radioimmunoconjugate consisting of a monoclonal antibody directed against the human carcinoembryonic antigen (CEA) conjugated with the radioisotope yttrium 90 (Y-90) via the chelator tetra-azacyclododecanetetra-acetic acid (DOTA) with potential antineoplastic activity. The antibody moiety of yttrium Y 90 DOTA anti-CEA monoclonal antibody M5A binds to cells expressing the CEA antigen. Upon cellular internalization, this agent selectively delivers a cytotoxic dose of beta radiation. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers.
  • Yttrium y 90 glass microspheres - An injectable formulation of yttrium Y 90 consisting of glass microspheres containing the radioisotope yttrium Y 90. When injected into the tumor vascular bed, yttrium Y 90 glass microspheres occlude tumor blood vessels and deliver a cytotoxic dose of beta radiation to the tumor site, thereby reducing the tumor burden.
  • Yttrium y 90 monoclonal antibody b3 - A radioimmunoconjugate of monoclonal antibody (MoAb) B3 conjugated with isotope yttrium 90. MoAb B3 is a murine MoAb that recognizes a Lewis Y carbohydrate antigen present on the surface of many carcinomas. This radioimmunoconjugate emits beta particles that causes cytotoxicity in tumor cells and has both diagnostic and therapeutic uses.
  • Yttrium y 90 monoclonal antibody bre-3 - A radioimmunotherapeutic agent consisting of a monoclonal antibody (BrE-3) directed against the tumor-associated antigen epithelial glycoprotein mucin chelated to the radioisotope yttrium-90. Yttrium Y 90 monoclonal antibody BrE-3 binds to tumor cells expressing epithelial glycoprotein mucin, selectively delivering a cytotoxic dose of beta radiation.
  • Yttrium y 90 monoclonal antibody hu3s193 - A radioimmunotherapeutic agent consisting of a humanized murine monoclonal antibody (hu3S193) directed against the tumor-associated Lewis Y epithelial antigen chelated to the radioisotope yttrium-90. Yttrium Y 90 monoclonal antibody Hu3S193 binds to Lewis Y epithelial antigen-expressing tumor cells, selectively delivering a cytotoxic dose of beta radiation.
  • Yttrium y 90 monoclonal antibody mn-14 - A radioimmunotherapeutic monoclonal antibody (MN-14) directed against tumor-associated carcinoembryonic antigen (CEA) and chelated to the radioisotope yttrium-90 (Y 90). Yttrium 90 monoclonal antibody MN-14 binds to tumor cell expressing CEA, delivering a cytotoxic dose of beta radiation.
  • Yttrium y 90 tabituximab barzuxetan - A radioimmunoconjugate composed of a humanized monoclonal antibody (MoAb) OTSA101 against FZD10 and labeled with yttrium y 90, with potential antineoplastic activity. The MoAb moiety of yttrium Y 90-labeled anti-FZD10 monoclonal antibody OTSA101 binds to FZD10, thereby delivering a cytotoxic dose of beta radiation to FZD10 positive tumor cells. FZD10 (also called CD350), a member of the Frizzled family of G protein-coupled receptors that is involved in the Wnt/beta-catenin/TCF signaling pathway, is overexpressed in a variety of cancer cell types but undetectable in normal, healthy human tissues except for the placenta.
  • Yttrium y 90-dota-biotin - A radioconjugate of biotin and yttrium Y 90 (Y-90) linked through the bifunctional macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) with radioimmunotherapy property. Biotin is a water-soluble B-complex vitamin, present in minute amounts in every living cell, while its level in cancerous tissue is higher than that of normal tissue. Y 90-DOTA-Biotin could be used in 3-step pre-targeting radioimmunotherapy that employs a tumor targeting antibody conjugated with streptavidin, the natural ligand of biotin.
  • Yttrium y 90-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 beta-emitting radionuclide yttrium 90 (Y-90), with radioimmunotherapeutic activity. After pre-treating and targeting tumor cells with a bi-specific monoclonal antibody (BiMoAB) directed against both a tumor-associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of the administered yttrium Y 90-DOTA-di-HSG peptide IMP-288 binds to the anti-HSG sequence on the BiMoAB. In turn, Y-90 delivers a cytotoxic dose of beta radiation to tumor cells expressing the specific TAA.
  • Yttrium y 90-edotreotide - A radioconjugate consisting of the octreotide derivative edotreotide labeled with yttrium 90 (Y-90) with potential radiotherapeutic uses. Similar to octreotide, yttrium Y 90-edotreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells, delivering tissue-specific, beta-emitting nuclide Y-90-mediated cytotoxicity to SSTR-positive cells. Yttrium Y 90-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide and chelating the substituted octreotide to Y-90 via dodecanetetraacetic acid (DOTA).
  • Yttrium y-90 clivatuzumab tetraxetan - A radioimmunoconjugate comprised of the humanized monoclonal antibody clivatuzumab, directed against the pancreatic cancer antigen MUC1, that is conjugated to the chelating agent tetraxetan and radiolabeled with the beta-emitting radioisotope Yttrium Y 90. Yttrium Y 90 clivatuzumab tetraxetan binds to tumor cells expressing MUC1 antigen, thereby selectively delivering a cytotoxic dose of beta radiation.
  • Yttrium y-90 epratuzumab tetraxetan - A radioimmunotherapeutic humanized murine monoclonal antibody (LL2) directed against the CD22 pan-B-cell antigen and chelated to the radioisotope yttrium-90 (Y 90). Y 90 humanized monoclonal antibody LL2 binds to tumor cells expressing CD22, delivering a cytotoxic dose of beta radiation.
  • Yttrium y-90 ibritumomab tiuxetan - A radioimmunotherapeutic agent consisting of a murine monoclonal anti-CD20 antibody (ibritumomab) linked by the chelator tiuxetan to the radioisotope yttrium-90 (Y 90). Yttrium Y 90 ibritumomab tiuxetan binds to and specifically delivers beta radiation to CD20-expressing tumor cells, thereby minimizing the systemic effects of radiation.
  • Yttrium y-90 tacatuzumab tetraxetan - A radioimmunoconjugate comprised of the humanized monoclonal antibody tacatuzumab, directed against alpha fetoprotein, that is conjugated to the chelating agent tetraxetan and radiolabeled with the beta-emitting radioisotope Yttrium Y 90. Yttrium Y 90 tacatuzumab tetraxetan binds to tumor cells expressing alpha fetoprotein, thereby selectively delivering a cytotoxic dose of beta radiation.
  • Yttrium-90 polycarbonate brachytherapy plaque - A polycarbonate-based semicylindrical plaque impregnated with yttrium Y 90 with radioisotopic and antineoplastic activities. An yttrium-90 polycarbonate brachytherapy plaque may be applied to a tumor site with a special brachytherapy applicator for a predetermined interval of time, selectively delivering a cytotoxic dose of beta-emitting yttrium Y 90.
  • 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.
  • Zalutumumab - A fully human IgG1 monoclonal antibody against epidermal growth factor receptor (EGFR) with potential antineoplastic activity. EGFR is a cell surface receptor tyrosine kinase, overexpressed on many cancer cells. Zalutumumab selectively binds to and blocks binding of EGF and transforming growth factor-alpha (TGF-a) to the EGFR receptor, thereby interfering with cellular signaling, leading to cell growth inhibition and apoptosis in tumor cells. In addition, zalutumumab also triggers cell lysis mediated through antibody dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells.
  • 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 - An engineered immunoglobulin G1 (IgG1) bi-specific 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 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 also induces a cytotoxic T-lymphocyte (CTL) response and antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. Antibody-dependent cellular phagocytosis (ADCP) is also induced and further stimulates the immune system to kill HER2-overexpressing tumor cells. The HER2 receptor internalization also further inhibits HER2 activation, HER2-mediated signaling and HER2-mediated tumor cell growth. 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.
  • 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.
  • Zebularine - A synthetic cytidine analogue and a cytidine deaminase inhibitor with anticancer activity. Following metabolic activation by phosphorylation and incorporation into DNA, zebularine inhibits DNA methyltransferase through covalent complex formation between the enzyme and zebularine-substituted DNA, hence resulting in non-specific, genome-wide induction of demethylation including the removal of aberrant methylation of promoter regions of genes critical for normal cellular functions.
  • 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.
  • 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.
  • Z-endoxifen hydrochloride - The hydrochloride salt and the z (cis-) stereoisomer of endoxifen with potential antineoplastic activity. Endoxifen, the active metabolite of tamoxifen, competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA and thus reducing DNA synthesis. Unlike tamoxifen, however, which relies on CYP2D6 activity for its conversion to the active metabolite endoxifen, the direct administration of endoxifen bypasses the CYP2D6 route. As CYP2D6 activity can vary widely among individuals due to genetic CYP2D6 polymorphisms, endoxifen is therefore theoretically more potent and more uniform in its bioavailability across patient populations.
  • 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.
  • 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.
  • 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.
  • Zinostatin stimalamer - A highly lipophilic conjugate protein comprised of the lipophilic antitumor protein, neocarzinostatin (NCS), conjugated with a water-soluble copolymer of styrene-maleic acid (SMA) with potential antineoplastic activity. Upon intra-hepatic arterial administration, zinostatin stimalamer is deposited within tumor tissues, where the NCS moiety induces sequence-specific single and double-stranded breaks via free-radical based mechanisms, resulting in tumor cell death.
  • 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.
  • Zolbetuximab - A chimeric monoclonal antibody directed against the antigen GC182 with potential immunostimulatory and antineoplastic activities. Upon administration, zolbetuximab specifically binds to GC128, which may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GC182-expressing tumor cells, resulting in decreased tumor cell proliferation. The CD20-like antigen GC182, a gastric differentiation protein, is often overexpressed on the cell surfaces of a variety of tumor cells, including gastric, pancreatic, esophageal cancer and non-small cell lung cancer (NSCLC) cells.
  • 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.
  • 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.
  • Zorifertinib - An orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, zorifertinib binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • Zorubicin - A benzoylhydrazone derivative of the anthracycline antineoplastic antibiotic daunorubicin. Zorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair as well as RNA and protein synthesis.
  • 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.
  • 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.
  • Zuclomiphene citrate - The cis isomer of clomiphene which exhibits weak estrogen agonist activity evaluated for antineoplastic activity against breast cancer.

Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ

 

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