Strop, Pavel,Delaria, Katherine Anne,Dorywalska, Magdalena,Foletti, Davide Luciano,Dushin, Russell George,Shelton, David Louis,Rajpal, Arvind
申请号：
AU2015249452
公开号：
AU2015249452A1
申请日:
2015.04.21
申请国别(地区):
AU
年份:
2016
代理人:
摘要：
The present invention provides transglutaminase-mediated antibody-drug conjugates with high antibody-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.
