Pavel STROP,Katherine Anne DELARIA,Magdalena DORYWALSKA,Davide Luciano FOLETTI,Russell George DUSHIN,David Louis SHELTON,Arvind RAJPAL
申请号：
US15306481
公开号：
US20170043033A1
申请日:
2015.04.21
申请国别(地区):
US
年份:
2017
代理人:
摘要：
The present invention provides transglutaminase-mediated antibody-drug conjugates with high anti-body-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity)； and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates.
