第一三共株式会社;DAIICHI SANKYO EUROPE GMBH;第一三共欧洲有限公司;第一三共株式會社;第一三共歐洲有限公司;DAIICHI SANKYO COMPANY, LIMITED
发明人:
T．黑特曼,R．亚伯拉罕,R．亞伯拉罕,S．布卢姆,S．布盧姆,上野杰
申请号：
MOJ004150
公开号：
MOJ004150B
申请日:
2020.05.05
申请国别(地区):
MO
年份:
2020
代理人:
摘要：
The invention provides an anti-tumor drug with excellent therapeutic effect in terms of anti-tumor effect and safety. The present invention provides an antibody drug conjugate, wherein the anti-tumor compound represented by the following formula is coupled with the anti-her3 antibody via a connector with the structure represented by the formula: l1-l2-lp-nh-ch2-n1-la-ch2-n2-c (= O) or l1-l2-lp-lp (the anti-her3 antibody is connected to the end of L1, and the anti-tumor compound is connected to ￣ (CH2) N2 ￣ C (= O) with the nitrogen atom of 1-amino as the connecting site The carbonyl group of the part or the C-terminal of the LP).本發明提供在抗腫瘤效果和安全性方面優異的具有優異治療效果的抗腫瘤藥。本發明提供了抗體－藥物偶聯物，其中下式表示的抗腫瘤化合物與抗HER3抗體經由具有式：‑L1‑L2‑LP‑NH‑(CH2)n1‑La‑(CH2)n2‑C(=O)‑或‑L1‑L2‑LP‑表示的結構的接頭偶聯(抗HER3抗體連接於L1的末端，抗腫瘤化合物以1位氨基的氮原子為連接部位連接於‑(CH2)n2‑C(=O)‑部分的羰基或LP的C末端)。
