POLY(GLUTAMIC ACID)-DRUG CONJUGATE WITH AN AMINO ACID AS A LINKER
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United States of America Patent
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Issued Date -
Feb 16, 2012
app pub date -
Nov 7, 2007
filing date -
Dec 30, 2006
priority date (Note) -
Abandoned
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Abstract
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 α-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 α-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.
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