Water soluble paclitaxel prodrugs
AssigneePG-TXL Company, L. P.
InventorsChun Li, Sidney Wallace, Dong-Fang Yu, David J. Yang
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Abstract
Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble chelator, polyethylene glycol or polymer such as poly (1-glutamic acid) or poly (1-aspartic acid). Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis and for prediction of paclitaxel uptake by tumors and radiolabeled DTPA-paclitaxel tumor imaging. Other embodiments include the coating of implantable stents for prevention of restenosis.
Claims22
A pharmaceutical composition comprising a conjugate comprising an anti-tumor or drug conjugated to a water soluble polyglutamic acid polymer, wherein said polymer has a molecular weight of greater than or equal to about 5,000, wherein said drug is conjugated to said polymer so as to provide a drug conjugate having a higher water solubility than the unconjugated drug, the ability to accumulate in a tumor, and wherein said anti-tumor drug is paclitaxel, docetaxel, etopside, teniposide, camptothecin or epothilone.
A pharmaceutical composition comprising a conjugate comprising paclitaxel conjugated at its 2'-or 7-hydroxyl group to a water soluble polyglutamic acid polymer, wherein said polymer has a molecular weight of greater than or equal to about 5,000, said conjugate having a higher water solubility than unconjugated paclitaxel, and having the ability to accumulate in a tumor.
A pharmaceutical composition comprising a conjugate comprising an anti-tumor drug conjugated to a water soluble polymer comprising a polyglutamic acid polymer, wherein said polyglutamic acid polymer has a molecular weight of about 20,000 to about 80,000, and wherein said drug is conjugated to said water soluble polymer so as to provide a drug conjugate having a higher water solubility than the unconjugated drug, the ability to accumulate in a tumor, and wherein said anti-tumor drug is paclitaxel, docetaxel, etopside, teniposide, camptothecin or epothilone.
A pharmaceutical composition comprising a conjugate of paclitaxel conjugated at its 2'-or 7-hydroxyl group to a water soluble polymer comprising a polyglutamic acid polymer, wherein said polyglutamic acid polymer has a molecular weight of about 20,000 to about 80,000, and wherein said conjugate has a higher water solubility than unconjugated paclitaxel, and has the ability to accumulate in a tumor.
Dependencies are inferred from the claim text.