Water soluble paclitaxel derivatives

Abstract

Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.

1 - 14 . (canceled) 
     
     
         15 . A pharmaceutical composition for the treatment of a tumor, comprising (A) camptothecin conjugated to a polyglutamic acid and (B) a pharmaceutically acceptable carrier; wherein said polyglutamic acid has a molecular weight range between 25,000 to 50,000 daltons. 
     
     
         16 . The pharmaceutical composition of  claim 15 , wherein the polymer is poly(L-glutamic) acid. 
     
     
         17 . The pharmaceutical composition of  claim 15 , wherein the conjugate comprises from 2% to 35% by weight of camptothecin. 
     
     
         18 . A method for enhancing the response of a tumor to irradiation, comprising administering the pharmaceutical composition of  claim 15  to a patient with a tumor before or after the patient is exposed to irradiation. 
     
     
         19 . The method of  claim 18 , wherein the irradiation dose is 10 Gray per week, and the pharmaceutical composition administered within 1-2 days of irradiation. 
     
     
         20 . The method of  claim 18 , wherein the patient has a tumor associated with breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.