MODIFIED DOCETAXEL LIPOSOME FORMULATIONS AND USES THEREOF
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United States of America Patent
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Sep 1, 2016
app pub date -
Feb 17, 2016
filing date -
Feb 17, 2015
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Abstract
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.
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