{"meta":{"totalResults":14,"from":0},"results":[{"aliases":[{"type":"Synonym","name":"trastuzumab-MCC-DM1"},{"type":"USBrandName","name":"Kadcyla"},{"type":"Synonym","name":"trastuzumab-DM1"},{"type":"Abbreviation","name":"T-DM1"},{"type":"Synonym","name":"trastuzumab-MCC-DM1 antibody-drug conjugate"},{"type":"CodeName","name":"PRO132365"},{"type":"Synonym","name":"trastuzumab emtansine"},{"type":"Synonym","name":"trastuzumab-MCC-DM1 immunoconjugate"},{"type":"CodeName","name":"RO5304020"},{"type":"CASRegistryName","name":"1018448-65-1"},{"type":"Synonym","name":"ado trastuzumab emtansine"},{"type":"ChemicalStructureName","name":"immunoglobulin G1, anti-(human p185neu receptor) (human-mouse monoclonal RhuMab HER2 gamma1-chain), disulfide with human-mouse monoclonal RhuMab HER2 light chain, dimer, tetraamide with N2'-(3-((1-((4-carboxycyclohexyl)methyl)-2,5-dioxo-3-pyrrolidinyl)thio)-1-oxopropyl)-N2'-deacetylMaytansine"}],"definition":{"html":"An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers.","text":"An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/ado-trastuzumab-emtansine","text":"Ado-Trastuzumab Emtansine"},"nciConceptId":"C82492","nciConceptName":"Trastuzumab Emtansine","termId":564399,"name":"ado-trastuzumab emtansine","firstLetter":"a","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-emtansine"},{"aliases":[{"type":"Synonym","name":"ADC FDA022-BB05"},{"type":"CodeName","name":"FDA022-BB05"},{"type":"Synonym","name":"anti-HER2 ADC FDA022-BB05"},{"type":"CodeName","name":"FDA022 BB05"},{"type":"CodeName","name":"FDA022BB05"},{"type":"Synonym","name":"trastuzumab/DXd ADC FDA022-BB05"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a valine-alanine (Val-Ala)-based cathepsin B-cleavable linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration, anti-HER2 ADC FDA022-BB05 targets and binds to HER2 expressed on tumor cells. Upon binding, internalization, and linker cleavage, DXd is released. DXd inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of HER2-expressing tumor cells. FDA022-BB05 is also able to induce a bystander effect on neighboring cells in the tumor environment. This further inhibits the proliferation of tumor cells. HER2, a receptor tyrosine kinase that is mutated or overexpressed in many tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization.","text":"An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a valine-alanine (Val-Ala)-based cathepsin B-cleavable linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration, anti-HER2 ADC FDA022-BB05 targets and binds to HER2 expressed on tumor cells. Upon binding, internalization, and linker cleavage, DXd is released. DXd inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of HER2-expressing tumor cells. FDA022-BB05 is also able to induce a bystander effect on neighboring cells in the tumor environment. This further inhibits the proliferation of tumor cells. HER2, a receptor tyrosine kinase that is mutated or overexpressed in many tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization."},"drugInfoSummaryLink":null,"nciConceptId":"C216085","nciConceptName":"Anti-HER2 Antibody-drug Conjugate FDA022-BB05","termId":817934,"name":"anti-HER2 antibody-drug conjugate FDA022-BB05","firstLetter":"a","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"anti-her2-antibody-drug-conjugate-fda022-bb05"},{"aliases":[{"type":"CodeName","name":"FS 1502"},{"type":"CodeName","name":"FS1502"},{"type":"CodeName","name":"FS-1502"},{"type":"Synonym","name":"ADC FS-1502"},{"type":"Synonym","name":"anti-HER2 ADC FS-1502"},{"type":"Synonym","name":"antibody-drug conjugate FS-1502"},{"type":"Synonym","name":"trastuzumab MMAF"},{"type":"CodeName","name":"IKS014"},{"type":"CodeName","name":"IKS 014"},{"type":"CodeName","name":"IKS-014"},{"type":"CodeName","name":"LCB14"},{"type":"CodeName","name":"LCB-14"},{"type":"CodeName","name":"LCB 14"},{"type":"Synonym","name":"trastuzumab monomethyl auristatin F"},{"type":"Synonym","name":"trastuzumab/MMAF ADC IKS014"},{"type":"CodeName","name":"LCB14-0110"},{"type":"CASRegistryName","name":"2930814-97-2"},{"type":"Synonym","name":"trastuzumab/MMAF antibody-drug conjugate IKS014"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized monoclonal antibody targeting the tumor-associated antigen (TAA) epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), site-specifically conjugated, via a tumor-selective beta-glucuronide linker, to the auristatin analog and potent microtubule inhibitor monomethyl auristatin F (MMAF), with potential antineoplastic activity. Upon administration of caxmotabart entudotin, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells. Upon binding, internalization and linker cleavage, MMAF is released. MMAF binds to and inhibits tubulin polymerization, which results in G2/M phase arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.","text":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized monoclonal antibody targeting the tumor-associated antigen (TAA) epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), site-specifically conjugated, via a tumor-selective beta-glucuronide linker, to the auristatin analog and potent microtubule inhibitor monomethyl auristatin F (MMAF), with potential antineoplastic activity. Upon administration of caxmotabart entudotin, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells. Upon binding, internalization and linker cleavage, MMAF is released. MMAF binds to and inhibits tubulin polymerization, which results in G2/M phase arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C172821","nciConceptName":"Caxmotabart Entudotin","termId":801696,"name":"caxmotabart entudotin","firstLetter":"c","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"caxmotabart-entudotin"},{"aliases":[{"type":"Synonym","name":"trastuzumab deruxtecan"},{"type":"CodeName","name":"DS-8201"},{"type":"USBrandName","name":"Enhertu"},{"type":"CodeName","name":"DS-8201a"},{"type":"CodeName","name":"WHO 10516"},{"type":"CASRegistryName","name":"1826843-81-5"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2; EGFR2; HER2) conjugated to deruxtecan, a derivative of the camptothecin analog exatecan (DXd; DX-8951 derivative), a DNA topoisomerase 1 (topoisomerase I; Top1) inhibitor, with antineoplastic activity. Upon administration of fam-trastuzumab deruxtecan-nxki, trastuzumab targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, deruxtecan binds to and inhibits Top1-DNA complexes, which results in an inhibition of DNA replication, cell cycle arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. In addition, trastuzumab deruxtecan induces antibody-dependent cell-mediated cytotoxicity (ADCC) and causes a bystander killing effect.","text":"An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2; EGFR2; HER2) conjugated to deruxtecan, a derivative of the camptothecin analog exatecan (DXd; DX-8951 derivative), a DNA topoisomerase 1 (topoisomerase I; Top1) inhibitor, with antineoplastic activity. Upon administration of fam-trastuzumab deruxtecan-nxki, trastuzumab targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, deruxtecan binds to and inhibits Top1-DNA complexes, which results in an inhibition of DNA replication, cell cycle arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. In addition, trastuzumab deruxtecan induces antibody-dependent cell-mediated cytotoxicity (ADCC) and causes a bystander killing effect."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/famtrastuzumabderuxtecan-nxki","text":"Fam-Trastuzumab Deruxtecan-nxki"},"nciConceptId":"C128799","nciConceptName":"Trastuzumab Deruxtecan","termId":783025,"name":"fam-trastuzumab deruxtecan-nxki","firstLetter":"f","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-deruxtecan"},{"aliases":[{"type":"Synonym","name":"trastuzumab analogue inetetamab"},{"type":"ForeignBrandName","name":"Cipterbin"}],"definition":{"html":"An Fc-engineered monoclonal antibody targeting the tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2), with potential immunomodulating and antineoplastic activities. Upon administration, inetetamab targets and specifically binds to HER2 on tumor cells, thereby blocking HER2-mediated signaling. This may inhibit proliferation of HER2-expressing tumor cells. In addition, the Fab region of inetetamab may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed in a variety of cancer cell types and is associated with increased tumor cell proliferation.","text":"An Fc-engineered monoclonal antibody targeting the tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2), with potential immunomodulating and antineoplastic activities. Upon administration, inetetamab targets and specifically binds to HER2 on tumor cells, thereby blocking HER2-mediated signaling. This may inhibit proliferation of HER2-expressing tumor cells. In addition, the Fab region of inetetamab may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed in a variety of cancer cell types and is associated with increased tumor cell proliferation."},"drugInfoSummaryLink":null,"nciConceptId":"C179282","nciConceptName":"Inetetamab","termId":804693,"name":"inetetamab","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"inetetamab"},{"aliases":[{"type":"Synonym","name":"trastuzumab-strf"},{"type":"USBrandName","name":"Hercessi"},{"type":"Synonym","name":"trastuzumab biosimilar QL1701"},{"type":"USBrandName","name":"Kanjinti"},{"type":"Synonym","name":"trastuzumab-anns"},{"type":"USBrandName","name":"Ontruzant"},{"type":"Synonym","name":"trastuzumab-dttb"},{"type":"USBrandName","name":"Trazimera"},{"type":"Synonym","name":"trastuzumab-qyyp"},{"type":"CodeName","name":"ABP 980"},{"type":"Synonym","name":"anti-c-erB-2"},{"type":"Synonym","name":"anti-c-erbB2 monoclonal antibody"},{"type":"Synonym","name":"anti-ERB-2"},{"type":"Synonym","name":"anti-erbB-2"},{"type":"Synonym","name":"anti-erbB2 monoclonal antibody"},{"type":"Synonym","name":"anti-HER2/c-erbB2 monoclonal antibody"},{"type":"Synonym","name":"anti-p185-HER2"},{"type":"LexicalVariant","name":"HER2 monoclonal antibody"},{"type":"USBrandName","name":"Herceptin"},{"type":"Synonym","name":"Herceptin biosimilar PF-05280014"},{"type":"Synonym","name":"trastuzumab biosimilar PF-05280014"},{"type":"Abbreviation","name":"MoAB HER2"},{"type":"Synonym","name":"MoAB HER2"},{"type":"Synonym","name":"monoclonal antibody HER2"},{"type":"Synonym","name":"monoclonal antibody c-erb-2"},{"type":"USBrandName","name":"Ogivri"},{"type":"CodeName","name":"PF-05280014"},{"type":"Abbreviation","name":"rhuMAb HER2"},{"type":"CodeName","name":"RO0452317"},{"type":"Synonym","name":"trastuzumab biosimilar PF-05280014"},{"type":"Synonym","name":"trastuzumab biosimilar SIBP-01"},{"type":"Synonym","name":"trastuzumab biosimilar ABP 980"},{"type":"Synonym","name":"trastuzumab biosimilar SB3"},{"type":"Synonym","name":"trastuzumab biosimilar HLX02"},{"type":"Synonym","name":"trastuzumab biosimilar ALT02"},{"type":"Synonym","name":"trastuzumab biosimilar EG12014"},{"type":"USBrandName","name":"Herzuma"},{"type":"NSCNumber","name":"688097"},{"type":"CASRegistryName","name":"180288-69-1"},{"type":"CodeName","name":"ALT02"},{"type":"Synonym","name":"c-erb-2 monoclonal antibody"},{"type":"Synonym","name":"Herceptin trastuzumab biosimilar PF-05280014"},{"type":"ChemicalStructureName","name":"immunoglobulin G 1 (human-mouse monoclonal RhuMab HER2gamma1-chain antihuman p185(Sup c-erbB2) receptor), disulfide with human-mouse monoclonal RhuMab HER2 light chain, dimer"},{"type":"CodeName","name":"QL 1701"},{"type":"CodeName","name":"QL-1701"},{"type":"CodeName","name":"QL1701"},{"type":"CodeName","name":"SB3"},{"type":"Synonym","name":"trastuzumab-dkst"},{"type":"Synonym","name":"trastuzumab-pkrb"},{"type":"CodeName","name":"CT-P06"},{"type":"CodeName","name":"CT-P6"},{"type":"Synonym","name":"trastuzumab biosimilar CT-P6"},{"type":"ForeignBrandName","name":"Biceltis"},{"type":"ForeignBrandName","name":"CANMab"},{"type":"ForeignBrandName","name":"Herclon"},{"type":"ForeignBrandName","name":"Hertraz"}],"definition":{"html":"A recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2). After binding to HER2 on the tumor cell surface, trastuzumab induces an antibody-dependent cell-mediated cytotoxicity against tumor cells that overexpress HER2. HER2 is overexpressed by many adenocarcinomas, particularly breast adenocarcinomas.","text":"A recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2). After binding to HER2 on the tumor cell surface, trastuzumab induces an antibody-dependent cell-mediated cytotoxicity against tumor cells that overexpress HER2. HER2 is overexpressed by many adenocarcinomas, particularly breast adenocarcinomas."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/trastuzumab","text":"Trastuzumab"},"nciConceptId":"C1647","nciConceptName":"Trastuzumab","termId":42265,"name":"trastuzumab","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab"},{"aliases":[{"type":"Synonym","name":"trastuzumab and hyaluronidase"},{"type":"USBrandName","name":"Herceptin Hylecta"},{"type":"Synonym","name":"trastuzumab and recombinant human hyaluronidase PH20"},{"type":"Synonym","name":"trastuzumab and rHuPH20"},{"type":"Synonym","name":"trastuzumab-hyaluronidase-oysk"},{"type":"Synonym","name":"trastuzumab/hyaluronidase-oysk"}],"definition":{"html":"A ready-to-use combination of trastuzumab, a recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; receptor tyrosine-protein kinase erbB-2), and hyaluronidase-oysk, a recombinant human hyaluronidase PH20 (rHuPH20), that may be used for the treatment of HER2-overexpressing breast cancers. Upon subcutaneous administration, hyaluronidase-oysk temporarily breaks down the hyaluronan barrier, which decreases viscosity of, and allows trastuzumab to spread rapidly through the interstitial space. This improves access to lymphatic and capillary vessels and facilitates the absorption of trastuzumab into the bloodstream. Trastuzumab binds to the extracellular ligand-binding domain of HER2 and mediates the activation of an antibody-dependent cell-mediated cytotoxicity (ADCC) against HER2-expressing tumor cells. HER2 is overexpressed in many adenocarcinomas, particularly breast adenocarcinomas.","text":"A ready-to-use combination of trastuzumab, a recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; receptor tyrosine-protein kinase erbB-2), and hyaluronidase-oysk, a recombinant human hyaluronidase PH20 (rHuPH20), that may be used for the treatment of HER2-overexpressing breast cancers. Upon subcutaneous administration, hyaluronidase-oysk temporarily breaks down the hyaluronan barrier, which decreases viscosity of, and allows trastuzumab to spread rapidly through the interstitial space. This improves access to lymphatic and capillary vessels and facilitates the absorption of trastuzumab into the bloodstream. Trastuzumab binds to the extracellular ligand-binding domain of HER2 and mediates the activation of an antibody-dependent cell-mediated cytotoxicity (ADCC) against HER2-expressing tumor cells. HER2 is overexpressed in many adenocarcinomas, particularly breast adenocarcinomas."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/trastuzumabandhyaluronidase-oysk","text":"Trastuzumab and Hyaluronidase-oysk"},"nciConceptId":"C158060","nciConceptName":"Trastuzumab/Hyaluronidase-oysk","termId":797111,"name":"trastuzumab and hyaluronidase-oysk","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-hyaluronidase-oysk"},{"aliases":[{"type":"CodeName","name":"A166"},{"type":"CodeName","name":"A 166"},{"type":"CodeName","name":"A-166"},{"type":"Synonym","name":"anti-HER2 ADC A166"},{"type":"Synonym","name":"ADC A166"},{"type":"CASRegistryName","name":"2699055-12-2"},{"type":"Synonym","name":"anti-HER2 antibody-drug conjugate A166"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a cleavable linker, to the microtubule inhibitor and auristatin derivative duostatin-5 (Duo-5), with potential antineoplastic activity. Upon administration of trastuzumab botidotin, the trastuzumab moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, duo-5 binds to tubulin and inhibits its polymerization, which results in cell cycle arrest and induces tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.","text":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a cleavable linker, to the microtubule inhibitor and auristatin derivative duostatin-5 (Duo-5), with potential antineoplastic activity. Upon administration of trastuzumab botidotin, the trastuzumab moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, duo-5 binds to tubulin and inhibits its polymerization, which results in cell cycle arrest and induces tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C156480","nciConceptName":"Trastuzumab Botidotin","termId":795827,"name":"trastuzumab botidotin","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-botidotin"},{"aliases":[{"type":"CodeName","name":"BI-CON-02"}],"definition":{"html":"A conjugated form of trastuzumab, a humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; ERBB2), with potential immunomodulating and antineoplastic activities. Upon administration, the trastuzumab conjugate BI-CON-02 targets and binds to HER2 on the tumor cell surface, thereby inducing both cytotoxic T-lymphocyte (CTL) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.","text":"A conjugated form of trastuzumab, a humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; ERBB2), with potential immunomodulating and antineoplastic activities. Upon administration, the trastuzumab conjugate BI-CON-02 targets and binds to HER2 on the tumor cell surface, thereby inducing both cytotoxic T-lymphocyte (CTL) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C148165","nciConceptName":"Trastuzumab Conjugate BI-CON-02","termId":792543,"name":"trastuzumab conjugate BI-CON-02","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-conjugate-bi-con-02"},{"aliases":[{"type":"CodeName","name":"SYD985"},{"type":"Synonym","name":"antibody-drug conjugate SYD985"},{"type":"Synonym","name":"ADC SYD985"},{"type":"CodeName","name":"UNII-XCR2BZ80N7"},{"type":"Synonym","name":"trastuzumab-drug conjugate SYD985"},{"type":"Synonym","name":"trastuzumab vc-seco-DUBA"},{"type":"CASRegistryName","name":"1642152-40-6"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of the recombinant humanized anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab linked, via a cleavable linker, to the duocarmycin prodrug, seco-duocarmycin-hydroxybenzamide-azaindole (seco-DUBA), with potential antineoplastic activity. Upon administration of trastuzumab duocarmazine, the trastuzumab moiety binds to HER2 on the tumor cell surface, which triggers the endocytosis of this agent. The linker is then cleaved inside the tumor cell by proteases at the dipeptide valine-citrulline (vc), and releases the active moiety, duocarmycin. Duocarmycin binds to the minor groove of DNA, alkylates adenine at the N3 position, and induces cell death. In addition, trastuzumab induces antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed by many carcinomas and is associated with a poor prognosis.","text":"An antibody-drug conjugate (ADC) composed of the recombinant humanized anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab linked, via a cleavable linker, to the duocarmycin prodrug, seco-duocarmycin-hydroxybenzamide-azaindole (seco-DUBA), with potential antineoplastic activity. Upon administration of trastuzumab duocarmazine, the trastuzumab moiety binds to HER2 on the tumor cell surface, which triggers the endocytosis of this agent. The linker is then cleaved inside the tumor cell by proteases at the dipeptide valine-citrulline (vc), and releases the active moiety, duocarmycin. Duocarmycin binds to the minor groove of DNA, alkylates adenine at the N3 position, and induces cell death. In addition, trastuzumab induces antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed by many carcinomas and is associated with a poor prognosis."},"drugInfoSummaryLink":null,"nciConceptId":"C118674","nciConceptName":"Trastuzumab Duocarmazine","termId":766012,"name":"trastuzumab duocarmazine","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-duocarmazine"},{"aliases":[{"type":"CodeName","name":"BDC 1001"},{"type":"CodeName","name":"BDC-1001"},{"type":"Synonym","name":"immune stimulating antibody conjugate BDC-1001"},{"type":"Synonym","name":"ISAC BDC-1001"},{"type":"LexicalVariant","name":"trastuzumab-TLR 7/8 agonist BDC-1001"},{"type":"CASRegistryName","name":"2643926-85-4"},{"type":"CodeName","name":"BDC1001"}],"definition":{"html":"An immune stimulating antibody conjugate (ISAC) consisting of trastuzumab, an anti-human epidermal growth factor receptor 2 (HER2) monoclonal antibody, conjugated to a Toll-like receptor (TLR) 7/8 dual agonist, with potential immunostimulating and antineoplastic activities. Upon administration of trastuzumab imbotolimod, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells and, simultaneously, the TLR 7/8 dual agonist moiety targets, binds to and activates TLR7/8 expressed on antigen-presenting cells (APCs), specifically dendritic cells (DCs), in the tumor microenvironment (TME). The trastuzumab binding to the tumor cells causes the engulfment of the trastuzumab imbotolimod-bound tumor cells by tumor-associated myeloid (TAM) cells and the TAMs travel to the lymph nodes. The DCs activated by the TLR7/8 agonist causes the activation of TLR7/8-mediated pathways, and stimulates the maturation and activation of DCs, thereby re-activating the immune system against the tumor cells. Activation of DCs results in the production of pro-inflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL)- and B-lymphocyte-mediated immune responses against tumor-associated antigens (TAAs), which lead to tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the innate immune system, myeloid cell responses and tumor antigen presentation. HER2 is overexpressed by a variety of tumor cell types.","text":"An immune stimulating antibody conjugate (ISAC) consisting of trastuzumab, an anti-human epidermal growth factor receptor 2 (HER2) monoclonal antibody, conjugated to a Toll-like receptor (TLR) 7/8 dual agonist, with potential immunostimulating and antineoplastic activities. Upon administration of trastuzumab imbotolimod, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells and, simultaneously, the TLR 7/8 dual agonist moiety targets, binds to and activates TLR7/8 expressed on antigen-presenting cells (APCs), specifically dendritic cells (DCs), in the tumor microenvironment (TME). The trastuzumab binding to the tumor cells causes the engulfment of the trastuzumab imbotolimod-bound tumor cells by tumor-associated myeloid (TAM) cells and the TAMs travel to the lymph nodes. The DCs activated by the TLR7/8 agonist causes the activation of TLR7/8-mediated pathways, and stimulates the maturation and activation of DCs, thereby re-activating the immune system against the tumor cells. Activation of DCs results in the production of pro-inflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL)- and B-lymphocyte-mediated immune responses against tumor-associated antigens (TAAs), which lead to tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the innate immune system, myeloid cell responses and tumor antigen presentation. HER2 is overexpressed by a variety of tumor cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C172388","nciConceptName":"Trastuzumab Imbotolimod","termId":802017,"name":"trastuzumab imbotolimod","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-imbotolimod"},{"aliases":[{"type":"CodeName","name":"SHRA1811"},{"type":"CodeName","name":"SHR A1811"},{"type":"CodeName","name":"SHR-A1811"},{"type":"Synonym","name":"ADC SHR-A1811"},{"type":"Synonym","name":"anti-HER2 ADC SHR-A1811"},{"type":"Synonym","name":"anti-HER2 ADC BAT8001"},{"type":"CASRegistryName","name":"2647845-11-0"},{"type":"Synonym","name":"anti-HER2 antibody-drug conjugate SHR-A1811"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1-kappa (IgG1k) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated, via a cleavable linker, to rezetecan, an exatecan derivative and topoisomerase 1 inhibitor, with potential antineoplastic activity. Upon administration of trastuzumab rezetecan, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells. Upon cellular uptake and linker cleavage, rezetecan stabilizes covalent topoisomerase I-DNA complexes, and results in single-stranded and double-stranded DNA breaks, the inhibition of DNA replication, the induction of apoptosis and the inhibition of tumor cell proliferation in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.","text":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1-kappa (IgG1k) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated, via a cleavable linker, to rezetecan, an exatecan derivative and topoisomerase 1 inhibitor, with potential antineoplastic activity. Upon administration of trastuzumab rezetecan, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells. Upon cellular uptake and linker cleavage, rezetecan stabilizes covalent topoisomerase I-DNA complexes, and results in single-stranded and double-stranded DNA breaks, the inhibition of DNA replication, the induction of apoptosis and the inhibition of tumor cell proliferation in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C178312","nciConceptName":"Trastuzumab Rezetecan","termId":804114,"name":"trastuzumab rezetecan","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-rezetecan"},{"aliases":[{"type":"Synonym","name":"ADC MRG002"},{"type":"Synonym","name":"anti-HER2/MMAE ADC MRG002"},{"type":"LexicalVariant","name":"anti-HER2/MMAE antibody-drug conjugate MRG002"},{"type":"CodeName","name":"MRG 002"},{"type":"CodeName","name":"MRG-002"},{"type":"CASRegistryName","name":"2740607-04-7"},{"type":"CodeName","name":"MRG002"}],"definition":{"html":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of trastuzumab vedotin, the trastuzumab moiety targets and binds to HER2 on the surface of tumor cells. Following internalization, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.","text":"An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of trastuzumab vedotin, the trastuzumab moiety targets and binds to HER2 on the surface of tumor cells. Following internalization, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C174205","nciConceptName":"Trastuzumab Vedotin","termId":804156,"name":"trastuzumab vedotin","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-vedotin"},{"aliases":[{"type":"Synonym","name":"ADC ADCT-502"},{"type":"CodeName","name":"ADCT 502"},{"type":"CodeName","name":"ADCT-502"},{"type":"CodeName","name":"ADCT50"},{"type":"Synonym","name":"anti-HER2/PBD ADC ADCT 502"}],"definition":{"html":"An antibody-drug conjugate (ADC) consisting of an engineered version of the humanized monoclonal anti-human epidermal growth factor receptor 2 (HER2) immunoglobulin G1 (IgG1) trastuzumab that is site-specifically conjugated, via a cleavable linker, to the cytotoxic, DNA cross-linking pyrrolobenzodiazepine (PBD) dimer-based drug tesirine, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the trastuzumab moiety of trastuzumab/tesirine ADC ADCT-502 targets the cell surface antigen HER2, which is expressed on various cancer cells. Upon antibody/antigen binding, internalization of the ADC and cleavage of the linker, the cytotoxic PBD moiety is released. The imine groups of tesirine bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death and inhibits the proliferation of HER2-overexpressing tumor cells. The tumor-associated antigen (TAA) HER2 is expressed by various solid tumors and is associated with a poor prognosis.","text":"An antibody-drug conjugate (ADC) consisting of an engineered version of the humanized monoclonal anti-human epidermal growth factor receptor 2 (HER2) immunoglobulin G1 (IgG1) trastuzumab that is site-specifically conjugated, via a cleavable linker, to the cytotoxic, DNA cross-linking pyrrolobenzodiazepine (PBD) dimer-based drug tesirine, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the trastuzumab moiety of trastuzumab/tesirine ADC ADCT-502 targets the cell surface antigen HER2, which is expressed on various cancer cells. Upon antibody/antigen binding, internalization of the ADC and cleavage of the linker, the cytotoxic PBD moiety is released. The imine groups of tesirine bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death and inhibits the proliferation of HER2-overexpressing tumor cells. The tumor-associated antigen (TAA) HER2 is expressed by various solid tumors and is associated with a poor prognosis."},"drugInfoSummaryLink":null,"nciConceptId":"C139800","nciConceptName":"Trastuzumab/Tesirine Antibody-drug Conjugate ADCT-502","termId":791110,"name":"trastuzumab/tesirine antibody-drug conjugate ADCT-502","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trastuzumab-tesirine-antibody-drug-conjugate-adct-502"}],"links":null}