Анбенитамаб реподатекан

Prop. INN (наименование, предложенное ВОЗ)

2923420-38-4

immunoglobulin G1-kappa, anti-[Homo sapiens ERBB2 (epidermal growth factor receptor 2, receptor tyrosine protein kinase erbB-2, EGFR2, HER2, HER-2, p185c-erbB2, NEU, CD340)], humanized monoclonal antibody, bispecific biparatopic, tetravalent, conjugated at O-4 of the four terminal GlcNAc groups of the two branched glycans to a repodatecan group, consisting of a cleavable linker and a camptothecin derivative;
H-gamma1 heavy chain anti-ERBB2 domain II humanized (1-449) [VH (Homo sapiens IGHV3-66*01 (78.8%) -(IGHD) -IGHJ4*01 (100%), CDR-IMGT [8.8.12] (26-33.51-58.97-108)) (1-119) -Homo sapiens IGHG1*01, G1m17,1 CH1 K120, CH3 D12, L14, 14-G1v32 CH3 W22 (knob), 18-G1v82-4 CH3 A88 (CH1 K120 (216) (120-217), hinge 1-15 (218-232), CH2 (233-342), CH3 D12 (358), L14 (360), T22>W (368), K88>A (411) (343-447), CHS (448-449)) (120-449)], (222-214')-disulfide with L-kappa light chain anti-ERBB2 humanized (1'-214') [V-KAPPA (Homo sapiens IGKV1-39*01 (86.3%) -IGKJ1*01 (100%), CDR-IMGT [6.3.9] (27'-32'.50'-52'.89'-97')) (1'-107') - Homo sapiens IGKC*01 (100%) Km3 A45.1, V101 (C-KAPPA A45.1 (153'), V101 (191')) (108'-214')];
H-gamma1 heavy chain anti-ERBB2 domain IV humanized (1''-450'') [VH (Homo sapiens IGHV3-66*01 (81.6%) -(IGHD) -IGHJ4*01 (100%), CDR-IMGT [8.8.13] (26''-33''.51''-58''.97''-109'')) (1''-120'') -Homo sapiens IGHG1*01, G1m17,1 CH1 K120, CH3 D12, L14, 14-G1v33 CH3 S22, A24, V86 (hole), 18-G1v82-3 CH3 K85.1 (CH1 K120 (217'') (121''-218''), hinge 1-15 (219''-233''), CH2 (234''-343''), CH3 D12 (359), L14 (361) T22>S (369''), L24>A (371''), F85.1>K (408''), Y86>V (410'') (344''-448''), CHS (449''-450'')) (121''-450'')], (223''-214''')-disulfide with L-kappa light chain anti-ERBB2 humanized (1'''-214''') [V-KAPPA (Homo sapiens IGKV1-39*01 (86.3%) -IGKJ1*01 (100%), CDR-IMGT [6.3.9] (27'''-32'''.50'''-52'''.89'''-97''')) (1'''-107''') - Homo sapiens IGKC*01 (100%) Km3 A45.1, V101 (C-KAPPA A45.1 (153'''), V101 (191''')) (108'''-214''')]; dimer (228-229'':231-232'')-bisdisulfide, produced in Chinese hamster ovary (CHO) cells, glycoform alfa, substituted at O-4 of the four distal 2-acetamido-2-deoxy-β-d-glucopyranosyl groups of the two glycans at N-4 of the asparaginyl residues 299 and 300'' with 2-(2-{8-[(10S)-10-benzyl-1-{[(1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl]amino}-1,6,9,12,15,18,34-heptaoxo-3,21,24,27,30-pentaoxa-5,8,11,14,17,33-hexaazaheptatriacontan-37-oyl]-8,9-dihydro-1(or 3)H-dibenzo[b,f][1,2,3]triazolo[4,5-d]azocin-1(or 3)-yl}acetamido)-2-deoxy-β-d-galactopyranosyl (repodatecan) groups (introduced by enzymatic glycosylation with 2-(2-azidoacetamido)-2-deoxy-d-galactopyranose and subsequent reaction of the azido groups with the specific click reagent), resulting in a drug/antibody ratio of ~3.8 on average

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