Proposed INN: List 105 <strong>WHO</strong> <strong>Drug</strong> <strong>Information</strong> <strong>Vol</strong>. <strong>25</strong>, <strong>No</strong>. 2, <strong>2011</strong>calaspargasum pegolum #calaspargase pegolcalaspargase pégolcalaspargasa pegolpegylated Escherichia coli asparaginase;[27-alanine,64-aspartic acid,<strong>25</strong>2-threonine,263-asparagine]-L-asparaginase 2 (EC 3.5.1.1, L-asparagine amidohydrolase II)Escherichia coli (strain K12) tetramer α 4 , carbamates withα-carboxy-ω-methoxypoly(oxyethylene)antineoplasticasparaginase d'Escherichia coli pégylée;carbamates entre le tétramère α 4 de [27-alanine,64-acideaspartique,<strong>25</strong>2-thréonine,263-asparagine]-L-asparaginase 2(EC 3.5.1.1, L-asparagine amidohydrolase II) d’Escherichia coli(souche K12) et le α-carboxy-ω-méthoxypoly(oxyéthylène)antinéoplasiqueasparaginasa de Escherichia coli pegilada;carbamatos entre el tetrámero α 4 de [27-alanina,64-ácidoaspártico,<strong>25</strong>2-treonina,263-asparagina]-L-asparaginasa 2(EC 3.5.1.1, L-asparagina amidohidrolasa II) de Escherichia coli(cepa K12) y el α-carboxi-ω-metoxipoli(oxietileno)antineoplásicoC 1516 H 2423 N 415 O 492 S 8 (peptide monomer) 941577-06-6Monomer / Monomère / MonómeroLPNITILATG GTIAGGGDSA TKSNYTAGKV GVENLVNAVP QLKDIANVKG 50EQVVNIGSQD MNDDVWLTLA KKINTDCDKT DGFVITHGTD TMEETAYFLD 100LTVKCDKPVV MVGAMRPSTS MSADGPFNLY NAVVTAADKA SANRGVLVVM 150NDTVLDGRDV TKTNTTDVAT FKSVNYGPLG YIHNGKIDYQ RTPARKHTSD 200TPFDVSKLNE LPKVGIVYNY ANASDLPAKA LVDAGYDGIV SAGVGNGNLY <strong>25</strong>0KTVFDTLATA AKNGTAVVRS SRVPTGATTQ DAEVDDAKYG FVASGTLNPQ 300KARVLLQLAL TQTKDPQQIQ QIFNQY 326approximately 9 residues are pegylated out of 23 (1 L and 22 K)environ 9 résidus sur 23 (1 L et 22 K) sont pegylésaproximadamente están pegilados 9 restos de 23 ( 1L y 22K)L1K22-29-43-49-71-72-79-104-107-139-162-172-186-196-207-213-229-<strong>25</strong>1-262-288-301-314H 3 COOH 3 CO Hnn # 112NHCH 3CO 2 HH 3 COOOnNHn # 112H 2 NHCO 2 HDisulfide bridges location / Position des ponts disulfure / Posiciones de los puentes disulfuro77-105 77'-105' 77'''-105''' 77''''-105''''158
<strong>WHO</strong> <strong>Drug</strong> <strong>Information</strong> <strong>Vol</strong>. <strong>25</strong>, <strong>No</strong>. 2, <strong>2011</strong> Proposed INN: List 105cantuzumabum ravtansinum #cantuzumab ravtansinecantuzumab ravtansinecantuzumab ravtansinaimmunoglobulin G1-kappa, anti-[Homo sapiens MUC1 sialylatedcarbohydrate, tumour-associated (CA242, cancer antigen 242)],humanized monoclonal antibody conjugated to maytansinoid DM4;gamma1 heavy chain (1-449) [humanized VH (Homo sapiensIGHV7-4-1*02 (76.50%) -(IGHD)-IGHJ2*01 R120>Q (111), L123>T(114)) [8.8.12] (1-119) -Homo sapiens IGHG1*01 (120-449)], (222-219')-disulfide with kappa light chain (1’-219’) [humanized V-KAPPA(Homo sapiens IGKV2-28*01 (82.00%) -IGKJ3*01 V124>L (109),D1<strong>25</strong>>E (110), I126>L (111)) [11.3.9] (1'-112') -Homo sapiensIGKC*01 (113'-219')]; (228-228":231-231")-bisdisulfide dimer;conjugated, on an average of 3 to 4 lysyl, to maytansinoid DM4 [N 2’ -deacetyl-N 2’ -(4-mercapto-4-methyl-1-oxopentyl)-maytansine] via thereducible SPDB linker [N-succinimidyl 4-(2-pyridyldithio)butanoate]For the ravtansine part, please refer to the document "INN forpharmaceutical substances: Names for radicals, groups and others"*antineoplasticimmunoglobuline G1-kappa, anti-[Homo sapiens glycane sialylé deMUC1, associé à des tumeurs (CA242, antigène du cancer 242)],anticorps monoclonal humanisé conjugué au maytansinoïde DM4;chaîne lourde gamma1 (1-449) [VH humanisé (Homo sapiensIGHV7-4-1*02 (76.50%) -(IGHD)-IGHJ2*01 R120>Q (111), L123>T(114)) [8.8.12] (1-119) -Homo sapiens IGHG1*01 (120-449)], (222-219')-disulfure avec la chaîne légère kappa (1'-219') [V-KAPPAhumanisé (Homo sapiens IGKV2-28*01 (82.00%) -IGKJ3*01 V124>L(109), D1<strong>25</strong>>E (110), I126>L (111)) [11.3.9] (1'-112') -Homo sapiensIGKC*01 (113'-219')]; dimère (228-228":231-231")-bisdisulfure;conjugué, sur 3 à 4 lysyl en moyenne, au maytansinoïde DM4 [N 2' -déacétyl-N 2' -(4-mercapto-4-méthyl-1-oxopentyl)-maytansine] via lelinker SPDB réductible [4-(2-pyridyldithio)butanoate deN-succinimidyle]Pour la partie ravtansine, veuillez vous référer au document "INN forpharmaceutical substances: Names for radicals, groups andothers"*.antinéoplasiqueinmunoglobulina G1-kappa, anti-[Homo sapiens glicano sialilo deMUC1, asociado al tumor (CA242, antígeno del cancer 242)]anticuerpo monoclonal humanizado conjugado con el maitansinoideDM4;cadena pesada gamma1 (1-449) [VH humanizada (Homo sapiensIGHV7-4-1*02 (76.50%) -(IGHD)-IGHJ2*01 R120>Q (111), L123>T(114)) [8.8.12] (1-119) -Homo sapiens IGHG1*01 (120-449)], (222-219')-disulfuro con la cadena ligera kappa (1'-219') [V-KAPPAhumanizada (Homo sapiens IGKV2-28*01 (82.00%) -IGKJ3*01V124>L (109), D1<strong>25</strong>>E (110), I126>L (111)) [11.3.9] (1'-112') -Homosapiens IGKC*01 (113'-219')]; dímero (228-228":231-231")-bisdisulfuro; conjugado, en 3-4 grupos lisil por término medio, con elmaitansinoide DM4 [N 2' -desacetil-N 2' -(4-mercapto-4-metil-1-oxopentil)-maitansina] mediante el conector SPDB reducible[4-(2-piridilditio)butanoato de N-succinimidilo]Para la fracción ravtansina, se ruega referirse al documento "INN forpharmaceutical substances: Names for radicals, groups andothers"*.antineoplásico159
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