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>AMENDMENTS TO PREVIOUS LISTSMODIFICATIONS APPORTÉES AUX LISTES ANTÉRIEURESMODIFICACIONES A LAS LISTAS ANTERIORESProposed International <strong>No</strong>n Proprietary Names (Prop. INN): List 89Denominations communes internationales proposées (DCI Prop.): Liste 89Denominaciones Comunes Internacionales Propuestas (DCI Prop.): Lista 89(<strong>WHO</strong> <strong>Drug</strong> <strong>Information</strong>, <strong>Vol</strong>. 17, <strong>No</strong>. 3, 2003)p. 188 cantuzumabummertansinum #cantuzumab mertansinecantuzumab mertansinecantuzumab mertansinareplace the description, the mechanism of action and the structure by thefollowingremplacer la description, le mécanisme d'action et la structure par lessuivantssustitúyase el nombre químico, el mecanismo de acción y la estructura porlos siguientesimmunoglobulin G1-kappa, anti-[Homo sapiens MUC1 sialylatedcarbohydrate, tumour-associated (CA242, cancer antigen 242)], humanizedmonoclonal antibody conjugated to maytansinoid DM1;gamma1 heavy chain (1-449) [humanized VH (Homo sapiens IGHV7-4-1*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 lightchain (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 sapiens IGKC*01 (113'-219')]; (228-228":231-231")-bisdisulfide dimer;conjugated, on an average of 4 lysyl, to maytansinoid DM1 [N 2’ -deacetyl-N 2’ -(3-mercapto-1-oxopropyl)-maytansine] via the reductible SPP linker[N-succinimidyl 4-(2-pyridyldithio)pentanoate]For the mertansine part, please refer to the document "INN for pharmaceuticalsubstances: Names for radicals, groups and others"*treatment of tumors that express CA242 antigenimmunoglobuline G1-kappa, anti-[Homo sapiens glycane sialylé de MUC1,associé à des tumeurs (CA242, antigène du cancer 242)], anticorpsmonoclonal humanisé conjugué au maytansinoïde DM1;chaîne lourde gamma1 (1-449) [VH humanisé (Homo sapiens IGHV7-4-1*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 chaînelégère kappa (1’-219’) [V-KAPPA humanisé (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 sapiens IGKC*01 (113'-219')]; dimère (228-228":231-231")-bisdisulfure; conjugué, sur 4 lysyl en moyenne, au maytansinoïde DM1[N 2’ -déacétyl-N 2’ -(3-mercapto-1-oxopropyl)-maytansine] via le linker SPPréductible [4-(2-pyridyldithio)pentanoate de N-succinimidyle]Pour la partie mertansine, veuillez vous référer au document "INN forpharmaceutical substances: Names for radicals, groups and others"*.antitumoral spécifique des cellules exprimant l'antigène CA242200
<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 105inmunoglobulina G1-kappa, anti-[glicano sialilado de MUC1 de Homosapiens, asociado a tumores (CA242, antígeno del cáncer 242)], anticuerpomonoclonal humanizado conjugado con el maitansinoide DM1; cadenapesada gamma1 (1-449) [VH humanizada (Homo sapiens IGHV7-4-1*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 cadenaligera kappa (1’-219’) [V-KAPPA humanizada (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 sapiens IGKC*01 (113'-219')]; dímero (228-228":231-231")-bisdisulfuro; conjugado, por término medio, en 4 grupos lisil, con elmaitansinoide DM1 [N 2 ’-desacetil-N 2 ’-(3-mercapto-1-oxopropil)-maitansina] mediante el espaciador SPP reducible[4-(2-piridilditio)pentanoato de N-succinimidilo]Para la mertansina, por favor, consulten el documento "INN forpharmaceutical substances: Names for radicals, groups and others"*.antitumoral específico de las células que expresan el antígeno CA242cantuzumab/ cantuzumab / cantuzumabHeavy chain / Chaîne lourde / Cadena pesadaQVQLVQSGAE VKKPGETVKI SCKASDYTFT YYGMNWVKQA PGQGLKWMGW 50IDTTTGEPTY AQKFQGRIAF SLETSASTAY LQIKSLKSED TATYFCARRG 100PYNWYFDVWG QGTTVTVSSA STKGPSVFPL APSSKSTSGG TAALGCLVKD 150YFPEPVTVSW NSGALTSGVH TFPAVLQSSG LYSLSSVVTV PSSSLGTQTY 200ICNVNHKPSN TKVDKKVEPK SCDKTHTCPP CPAPELLGGP SVFLFPPKPK <strong>25</strong>0DTLMISRTPE VTCVVVDVSH EDPEVKFNWY VDGVEVHNAK TKPREEQYNS 300TYRVVSVLTV LHQDWLNGKE YKCKVSNKAL PAPIEKTISK AKGQPREPQV 350YTLPPSRDEL TKNQVSLTCL VKGFYPSDIA VEWESNGQPE NNYKTTPPVL 400DSDGSFFLYS KLTVDKSRWQ QGNVFSCSVM HEALHNHYTQ KSLSLSPGK 449Light chain / Chaîne légère / Cadena ligeraDIVMTQSPLS VPVTPGEPVS ISCRSSKSLL HSNGNTYLYW FLQRPGQSPQ 50LLIYRMSNLV SGVPDRFSGS GSGTAFTLRI SRVEAEDVGV YYCLQHLEYP 100FTFGPGTKLE LKRTVAAPSV FIFPPSDEQL KSGTASVVCL LNNFYPREAK 150VQWKVDNALQ SGNSQESVTE QDSKDSTYSL SSTLTLSKAD YEKHKVYACE 200VTHQGLSSPV TKSFNRGEC 219Disulfide bridges location / Position des ponts disulfure / Posiciones de los puentes disulfuroIntra-H 22-96 146-202 263-323 369-42722''-96'' 146''-202'' 263''-323'' 369''-427''Intra-L 23'-93' 139'-199'23'''-93''' 139'''-199'''Inter-H-L 222-219' 222''-219'''Inter-H-H 228-228'' 231-231''N-glycosylation sites / Sites de N-glycosylation / Posiciones de N-glicosilación299, 299''mertansine / mertansine / mertansinaIgNHOSCH 3SO H CH 3ONH 3 C CH 3 OCH 3 ClOHH 3 CNHH HOOOHO NHH OCH 3 CH 3OCH 34cantuzumab = Ig(NH 2 ) 4201
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