INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A.
发明人:
ZHONG, BOHUA,ZHANG, JIANXIN,CHEN, LANFU
申请号:
EP07816772
公开号:
EP2108368A4
申请日:
2007.11.07
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
A poly(glutamic acid)-drug conjugate with an amino acid as a linker, and nontoxic pharmaceutically acceptable salt thereof, are provided in the present invention. The drug is gemcitabine, paclitaxel or docetaxel. The ±-carboxyl group in the amino acid is linked to 5-hydroxy in gemcitabine molecule or linked to 2-hydroxy in paclitaxel (docetaxel) molecule via an ester linkage. The ±-amino group in the amino acid is linked to the carboxyl group in the poly-(L-glutamic acid) molecule via an amide linkage. The content of gemcitabine in the conjugate is 5-30% in weight, and the content of paclitaxel or docetaxel is 10-40% in weight.