{"meta":{"totalResults":4,"from":0},"results":[{"aliases":[{"type":"CodeName","name":"ORM-5029"},{"type":"CodeName","name":"ORM5029"},{"type":"CodeName","name":"ORM 5029"},{"type":"Synonym","name":"antibody neodegrader conjugate ORM-5029"},{"type":"Synonym","name":"pertuzumab-SMol006 ORM-5029"},{"type":"Synonym","name":"AnDC ORM-5029"},{"type":"Synonym","name":"anti-HER-2 GSPT1 degrader ORM-5029"}],"definition":{"html":"A targeted protein degrader (TPD) composed of pertuzumab, an antibody directed against the tumor-associated antigen (TAA) human tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), conjugated, via a Val-Cit PABc cleavable linker, to SMol006, a membrane-permeable selective molecular glue degrader (MGD) of the translational termination factor GSPT1, with potential antineoplastic activity. Upon intravenous administration, anti-HER2 GSPT1 degrader ORM-5029 specifically targets and binds, with its pertuzumab moiety, to HER-2-expressing tumor cells. Upon internalization and cleavage, SMol006 specifically targets and binds to GSPT1, leading to GSPT1 degradation via the E3 ubiquitin ligase pathway. This disrupts oncogenic signaling, inhibits proliferation, and induces apoptosis in HER-2-driven tumors. The translation termination factor GSPT1, a G-loop degron-containing protein, plays a key role in protein translation and is dysregulated in various tumor cell types.","text":"A targeted protein degrader (TPD) composed of pertuzumab, an antibody directed against the tumor-associated antigen (TAA) human tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), conjugated, via a Val-Cit PABc cleavable linker, to SMol006, a membrane-permeable selective molecular glue degrader (MGD) of the translational termination factor GSPT1, with potential antineoplastic activity. Upon intravenous administration, anti-HER2 GSPT1 degrader ORM-5029 specifically targets and binds, with its pertuzumab moiety, to HER-2-expressing tumor cells. Upon internalization and cleavage, SMol006 specifically targets and binds to GSPT1, leading to GSPT1 degradation via the E3 ubiquitin ligase pathway. This disrupts oncogenic signaling, inhibits proliferation, and induces apoptosis in HER-2-driven tumors. The translation termination factor GSPT1, a G-loop degron-containing protein, plays a key role in protein translation and is dysregulated in various tumor cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C191715","nciConceptName":"Anti-HER2 GSPT1 Degrader ORM-5029","termId":811095,"name":"anti-HER2 GSPT1 degrader ORM-5029","firstLetter":"a","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"anti-her2-gspt1-degrader-orm-5029"},{"aliases":[{"type":"USBrandName","name":"Perjeta"},{"type":"Synonym","name":"rhuMAb-2C4"},{"type":"LexicalVariant","name":"rhuMAb 2C4"},{"type":"Synonym","name":"2C4 antibody"},{"type":"Synonym","name":"monoclonal antibody 2C4"},{"type":"Abbreviation","name":"MOAB 2C4"},{"type":"Synonym","name":"rhuMAb2C4"},{"type":"Synonym","name":"2C4"},{"type":"CodeName","name":"RO4368451"},{"type":"Synonym","name":"pertuzumab biosimilar HS627"},{"type":"Synonym","name":"pertuzumab biosimilar HLX11"},{"type":"Synonym","name":"pertuzumab biosimilar EG1206A"},{"type":"Synonym","name":"pertuzumab biosimilar TQB2440"},{"type":"CodeName","name":"TQB2440"},{"type":"CodeName","name":"TQB 2440"},{"type":"CodeName","name":"TQB-2440"},{"type":"CodeName","name":"TQB2440"},{"type":"CASRegistryName","name":"380610-27-5"},{"type":"CodeName","name":"EG1206A"},{"type":"CodeName","name":"HLX11"},{"type":"CodeName","name":"HS627"},{"type":"ChemicalStructureName","name":"immunoglobulin G1, anti-(human V (receptor)) (human-mouse monoclonal 2C4 heavy chain), disulfide with human-mouse monoclonal 2C4 kappa-chain, dimer"},{"type":"Synonym","name":"omnitarg"},{"type":"Synonym","name":"pertuzumab biosimilar BCD-178"},{"type":"CodeName","name":"BCD-178"}],"definition":{"html":"A humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the HER-2 tyrosine kinase receptor. Binding of the antibody to the dimerization domain of the HER-2 tyrosine kinase receptor protein directly inhibits the ability of the HER-2 tyrosine kinase receptor protein (the most common pairing partner) to dimerize with other HER tyrosine kinase receptor proteins; inhibiting receptor protein dimerization prevents the activation of HER signaling pathways, resulting in tumor cell apoptosis.","text":"A humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the HER-2 tyrosine kinase receptor. Binding of the antibody to the dimerization domain of the HER-2 tyrosine kinase receptor protein directly inhibits the ability of the HER-2 tyrosine kinase receptor protein (the most common pairing partner) to dimerize with other HER tyrosine kinase receptor proteins; inhibiting receptor protein dimerization prevents the activation of HER signaling pathways, resulting in tumor cell apoptosis."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/pertuzumab","text":"Pertuzumab"},"nciConceptId":"C38692","nciConceptName":"Pertuzumab","termId":322808,"name":"pertuzumab","firstLetter":"p","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"pertuzumab"},{"aliases":[{"type":"LexicalVariant","name":"HER2-directed TLR8 agonist SBT6050"},{"type":"Synonym","name":"HER2-directed TLR8 ImmunoTAC SBT6050"},{"type":"Synonym","name":"ImmunoTAC SBT6050"},{"type":"CodeName","name":"SBT 6050"},{"type":"CodeName","name":"SBT6050"},{"type":"Synonym","name":"TLR8 agonist-HER2-directed monoclonal antibody conjugate SBT6050"},{"type":"CASRegistryName","name":"2500674-05-3"},{"type":"CodeName","name":"SBT-6050"}],"definition":{"html":"An immunotherapeutic composed of a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated to a Toll-like receptor 8 (TLR8; CD288) agonist, with potential immunostimulating and antineoplastic activities. Upon intravenous administration pertuzumab zuvotolimod, the anti-HER2 monoclonal antibody targets and binds to HER2 expressed on tumor cells, thereby localizing the TLR8 agonist directly to the tumor site. In turn, the TLR8 agonist moiety binds to TLR8 expressed on myeloid cells within the tumor microenvironment (TME). This activates myeloid cells, including tumor-associated macrophages (TAMs), myeloid cell-derived suppressive cells (MDSCs), and conventional dendritic cells (cDCs). This may lead to the activation of nuclear factor NF-kappa-B, the production of pro-inflammatory cytokines and chemokines, macrophage-induced tumor cell killing, inflammasome activation, activation of cytolytic natural killer (NK) cells and neutrophils, and the induction of a Th1-weighted anti-tumor immune response. It also reverses the suppression of senescent naive and tumor-specific T cells, and enhances the anti-tumor cytotoxic T-lymphocyte (CTL) immune response. TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in innate and adaptive immunity. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.","text":"An immunotherapeutic composed of a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated to a Toll-like receptor 8 (TLR8; CD288) agonist, with potential immunostimulating and antineoplastic activities. Upon intravenous administration pertuzumab zuvotolimod, the anti-HER2 monoclonal antibody targets and binds to HER2 expressed on tumor cells, thereby localizing the TLR8 agonist directly to the tumor site. In turn, the TLR8 agonist moiety binds to TLR8 expressed on myeloid cells within the tumor microenvironment (TME). This activates myeloid cells, including tumor-associated macrophages (TAMs), myeloid cell-derived suppressive cells (MDSCs), and conventional dendritic cells (cDCs). This may lead to the activation of nuclear factor NF-kappa-B, the production of pro-inflammatory cytokines and chemokines, macrophage-induced tumor cell killing, inflammasome activation, activation of cytolytic natural killer (NK) cells and neutrophils, and the induction of a Th1-weighted anti-tumor immune response. It also reverses the suppression of senescent naive and tumor-specific T cells, and enhances the anti-tumor cytotoxic T-lymphocyte (CTL) immune response. TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in innate and adaptive immunity. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types."},"drugInfoSummaryLink":null,"nciConceptId":"C174010","nciConceptName":"Pertuzumab Zuvotolimod","termId":802452,"name":"pertuzumab zuvotolimod","firstLetter":"p","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"pertuzumab-zuvotolimod"},{"aliases":[{"type":"USBrandName","name":"Phesgo"},{"type":"Synonym","name":"hyaluronidase-zzxf/pertuzumab/trastuzumab"},{"type":"Synonym","name":"pertuzumab/trastuzumab/hyaluronidase-zzxf"}],"definition":{"html":"A ready-to-use fixed-dose combination of pertuzumab and trastuzumab, both recombinant humanized monoclonal antibodies directed against the tyrosine kinase receptor (TKR) human epidermal growth factor receptor 2 (HER2; HER-2; receptor tyrosine-protein kinase erbB-2), and hyaluronidase-zzxf, a biosimilar of the recombinant form of the naturally occurring endoglycosidase hyaluronidase, with antineoplastic activity that can be used for the treatment of HER2-overexpressing breast cancers. Upon subcutaneous administration, hyaluronidase-zzxf temporarily breaks down the hyaluronan barrier, which decreases viscosity of, and allows both pertuzumab and trastuzumab to spread rapidly through the interstitial space. This improves access to lymphatic and capillary vessels and facilitates the absorption of both antibodies into the bloodstream. Pertuzumab targets and binds to the extracellular dimerization domain (subdomain II) of HER2 and blocks ligand-dependent heterodimerization of HER2 with other HER family members, including EGFR, HER3 and HER4. This inhibits ligand-initiated intracellular signaling and prevents the activation of the mitogen-activated protein (MAP) kinase and the phosphoinositide 3-kinase (PI3K) signaling pathways, leading to growth arrest and apoptosis in HER2-overexpressing tumor cells, respectively. Trastuzumab targets and binds to subdomain IV of HER2 and inhibits ligand-independent, HER2 mediated cell proliferation and inhibits the PI3K signaling pathway in HER2-overexpressing tumor cells. Both antibodies induce 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 fixed-dose combination of pertuzumab and trastuzumab, both recombinant humanized monoclonal antibodies directed against the tyrosine kinase receptor (TKR) human epidermal growth factor receptor 2 (HER2; HER-2; receptor tyrosine-protein kinase erbB-2), and hyaluronidase-zzxf, a biosimilar of the recombinant form of the naturally occurring endoglycosidase hyaluronidase, with antineoplastic activity that can be used for the treatment of HER2-overexpressing breast cancers. Upon subcutaneous administration, hyaluronidase-zzxf temporarily breaks down the hyaluronan barrier, which decreases viscosity of, and allows both pertuzumab and trastuzumab to spread rapidly through the interstitial space. This improves access to lymphatic and capillary vessels and facilitates the absorption of both antibodies into the bloodstream. Pertuzumab targets and binds to the extracellular dimerization domain (subdomain II) of HER2 and blocks ligand-dependent heterodimerization of HER2 with other HER family members, including EGFR, HER3 and HER4. This inhibits ligand-initiated intracellular signaling and prevents the activation of the mitogen-activated protein (MAP) kinase and the phosphoinositide 3-kinase (PI3K) signaling pathways, leading to growth arrest and apoptosis in HER2-overexpressing tumor cells, respectively. Trastuzumab targets and binds to subdomain IV of HER2 and inhibits ligand-independent, HER2 mediated cell proliferation and inhibits the PI3K signaling pathway in HER2-overexpressing tumor cells. Both antibodies induce 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/pertuzumabtrastuzumabandhyaluronidase-zzxf","text":"Pertuzumab, Trastuzumab, and Hyaluronidase-zzxf"},"nciConceptId":"C173339","nciConceptName":"Hyaluronidase-zzxf/Pertuzumab/Trastuzumab","termId":801876,"name":"pertuzumab, trastuzumab, and hyaluronidase-zzxf","firstLetter":"p","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"hyaluronidase-zzxf-pertuzumab-trastuzumab"}],"links":null}