US2006111273A1PendingUtilityA1

Water soluble paclitaxel derivatives

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Assignee: PG TXL CO LPPriority: Mar 30, 1998Filed: Oct 20, 2005Published: May 25, 2006
Est. expiryMar 30, 2018(expired)· nominal 20-yr term from priority
Inventors:Chun LiSidney WallaceDong-Fang YuDavid J. Yang
A61K 47/60A61L 31/16A61P 35/00A61L 2300/606A61K 51/065A61K 47/645A61K 47/59C08G 73/1092A61K 2123/00A61K 51/0497A61P 35/04A61K 2121/00A61K 38/13A61L 31/10A61K 31/337A61K 47/547A61L 2300/416A61K 41/0038A61K 31/4375A61P 35/02
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Claims

Abstract

Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as polyglutamic 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.

Claims

exact text as granted — not AI-modified
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 30,000 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 . The pharmaceutical composition of  claim 15 , which is useful in enhancing the response of a tumor to irradiation in irradiation therapy, wherein the conjugated camptothecin has increased water solubility, efficacy and accumulation within a tumor compared with the corresponding unconjugated drugs.  
   
   
       19 . The pharmaceutical composition of  claim 18 , wherein the pharmaceutical composition is administered prior to irradiation.  
   
   
       20 . The pharmaceutical composition of  claim 18 , wherein the pharmaceutical composition is administered following irradiation.  
   
   
       21 . The pharmaceutical composition of  claim 18 , wherein the irradiation dose is 10 Gray per week, and the pharmaceutical composition administered within 1-2 days of irradiation.  
   
   
       22 . The pharmaceutical composition of  claim 15 , wherein the tumor is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
   
   
       23 . The pharmaceutical composition of  claim 15 , wherein the ratio of camptothecin molecules to polyglutamic acid molecules is 1-75:1.

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