ГЕРБЕР Ханс-Питер (US),ДИДЖОЗЕФ Джон Фрэнсис (US),ХАНДКЕ Киран Манохар (US),МАРКЕТТ Киберли Энн (US),САПРА Пуджа (US),ЧИСТЯКОВА Людмила Геннадьевна (US)
申请号：
RU2013142004/10
公开号：
RU2013142004A
申请日:
2012.03.19
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. The antibody-drug conjugate of the formula: Ab- (LU-D) or a pharmaceutically acceptable salt thereof, wherein: a) Ab is an anti-5T4 antibody or antigen binding fragment thereof comprising a heavy chain variable region (VH) having: 1) VH CDR1 region (complementarity determining region 1), as shown in SEQ ID NO: 5.2) VH CDR2 region, as shown in SEQ ID NO: 6, and 3) VH CDR3 region, as shown in SEQ ID NO: 7 ； b) LU is a linker unit selected from the group consisting of maleimidocaproyl and maleimidocaproyl-Val-Cit； c) p is a whole The number of from about 1 to about 8, u) D is a structural unit of a medicament, selected from the group consisting of MMAE (monometilauristatin E), MMAD (monometilauristatin D) and MMAF (monometilauristatin F) .2. The antibody-drug conjugate according to claim 1, wherein said anti-5T4 antibody or antigen binding fragment thereof comprises a light chain variable region (VL) having: a) a VL region of CDR1, as shown in SEQ ID NO: 8, b) a region VL CDR2, as shown in SEQ ID NO: 9, iv) the VL region of CDR3, as shown in SEQ ID NO: 10.3. The antibody-drug conjugate of claim 1, wherein said anti-5T4 antibody or antigen binding fragment thereof further comprises: 1) a heavy chain variable region having: a) a VH region of CDR1, as shown in SEQ ID NO: 5, b) VH region of CDR2, as shown in SEQ ID NO: 6, iv) region of VH CDR3, as shown in SEQ ID NO: 7； 2) a variable region of the light chain having: a) region of VL CDR1, as shown in SEQ ID NO: 8b) the VL region of CDR2, as shown in SEQ ID NO: 9, iv) the VL region of CDR3, as shown in SEQ ID NO: 10.4. The antibody-drug conjugate according to claim 1, wherein said anti-5T4 antibody or antigen binding thereof1. Конъюгат «антитело-лекарственное средство» формулы:Ab-(LU-D)pили его фармацевтически приемлемая соль, где:a) Ab представляет собой антитело против 5T4 или его антигенсвязывающий фрагмент, содержащие вариабельную область тяжелой цепи (VH), имеющую:1) область VH CDR1 (определяющая комплементарность о
