SINGH RAJEEVA,KOVTUN YELENA,WILHELM SHARON D,CHARI RAVI V J
申请号:
ZA201007806
公开号:
ZA201007806B
申请日:
2010.11.01
申请国别(地区):
ZA
年份:
2013
代理人:
摘要:
Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.