抗ＨＥＲ２抗體－藥物結合物

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专利权人:

DAIICHI SANKYO COMPANY; LIMITED

发明人:

NAITO, HIROYUKI,内藤博之,內藤博之,OGITANI, YUSUKE,扇谷佑辅,扇谷祐輔,MASUDA, TAKESHI,益田刚,益田剛,NAKADA, TAKASHI,中田隆,YOSHIDA, MASAO,吉田昌生,ASHIDA, SHINJI,芦田真二,蘆田真二,MORITA, KOJI,森田浩司,MIYAZAKI, HIDEKI,宫崎秀树,宮崎秀樹

申请号：

TW104103127

公开号：

TW201613649A

申请日:

2015.01.30

申请国别(地区):

TW

年份:

2016

代理人:

摘要：

As an anti-tumor drug having an excellent anti-tumor effect and safety and also having an excellent therapeutic effect, an antibody-drug conjugate is provided, which is characterized in that an anti-tumor compound represented by formula (1) is linked to an anti-HER2 antibody through a linker having a structure represented by the formula: -L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)- (wherein the anti-HER2 antibody is linked at the terminal of L1, and the anti-tumor compound is linked to a carbonyl group in a -(CH2)n2-C(=O)- moiety wherein a nitrogen atom in an amino group located at position-1 in the anti-tumor compound serves as a linking part).本發明提供一種抗體-藥物結合物作為抗腫瘤效果及安全性面優異之具有優異治療效果的抗腫瘤藥，其特徵為使下式所示的抗腫瘤性化合物與抗HER2抗體，經由下式：-L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)-所示的構造之連接物(linker)而結合(抗HER2抗體係於L1之末端結合，抗腫瘤性化合物係將1位之胺基之氮原子作為結合部位，而與-(CH2)n2-C(=O)-部分之羰基結合)。

来源网站：

中国工程科技知识中心

来源网址：

http://www.ckcest.cn/home/