WILLIAM McGHEE,JAMES BLACKLEDGE,MARGARET GRAPPERHAUS,LOUISE ROCHON,KRISHNA DEVARAKONDA
申请号:
US15046243
公开号:
US20160250177A1
申请日:
2016.02.17
申请国别(地区):
US
年份:
2016
代理人:
摘要:
The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and a taxane. The PEG-lipid constitutes from about 2 to about 8 mol % of the lipids in the liposome. The taxane is docetaxel esterified at the 2′-O position with a heterocyclyl-(C2-5 alkanoic acid). The present invention also provides liposomal compositions for the treatment of cancer comprising administering to a patient in need thereof a liposome, wherein the liposome comprises: a phosphatidylcholine lipid a sterol a PEG-lipid and a taxane or a pharmaceutically acceptable salt thereof wherein the taxane is docetaxel esterified at the 2′-O-position with a heterocyclyl-(C2-5alkanoic acid) and wherein upon administration of the liposomal composition to the patient, the plasma concentration of docetaxel remain above an efficacy threshold of 0.2 μM for at least 5 hours.