US2003130178A1PendingUtilityA1

Water soluble paclitaxel dervatives

48
Assignee: PG TXL CO LPPriority: Mar 12, 1996Filed: Nov 18, 2002Published: Jul 10, 2003
Est. expiryMar 12, 2016(expired)· nominal 20-yr term from priority
Inventors:Chun LiSidney WallaceDong-Fang YuDavid J. Yang
C08G 73/1092A61K 47/645A61L 31/16A61K 2121/00A61K 47/547A61K 51/0497A61K 47/59A61L 2300/606A61K 41/0038A61K 31/337A61L 2300/416A61L 31/10A61P 35/00A61K 31/4375A61P 35/04A61P 35/02A61K 51/065A61K 2123/00A61K 38/13A61K 47/60
48
PatentIndex Score
0
Cited by
0
References
0
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 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.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A method of treating a condition responsive to a therapeutic agent comprising administering to a subject an effective amount of a conjugate of a plurality of therapeutic agents and a water-soluble amino acid polymer wherein said plurality of therapeutic agents are covalently bonded to said polymer.  
     
     
         2 . The method of  claim 1 , wherein the condition is selected from the group consisting of prostate, breast, ovarian, colon, leukemia and lung cancers, malignant melanoma, head and neck cancers, gastric cancer and Kaposi's sarcoma.  
     
     
         3 . The method of  claim 1 , wherein the condition is selected from the group consisting of prostate, breast, ovarian, colon, leukemia and lung cancers.  
     
     
         4 . The method of  claim 1 , wherein the condition is ovarian cancer.  
     
     
         5 . The method of  claim 1 , wherein the condition is colon cancer.  
     
     
         6 . The method of  claim 1 , wherein the condition is leukemia.  
     
     
         7 . The method of  claim 1 , wherein the condition is lung cancer.  
     
     
         8 . The method of  claim 1 , wherein the condition is prostate cancer.  
     
     
         9 . The method of  claim 1  wherein the drug is a chemotherapeutic or antiangiogenic drug.  
     
     
         10 . The method of  claim 1  wherein at least one of said plurality of therapeutic agents is a taxoid, tamoxifen, etoposide, teniposide, fludarabine, doxorubicin, daunomycin, emodin, 5-fluorouracil, FUDR, estradiol, camptothecin, a retinoid, verapamil, an epothilone or a cyclosporin.  
     
     
         11 . The method of  claim 10 , wherein at least one of said plurality of therapeutic agents is paclitaxel or taxotere.  
     
     
         12 . The method of  claim 1 , wherein at least one of said plurality of therapeutic agents is paclitaxel.  
     
     
         13 . The method of  claim 1 , wherein said polymer has a molecular weight of from about 1 to about 100,000 daltons.  
     
     
         14 . The method of  claim 13 , wherein said polymer has a molecular weight of from about 20,000 to about 80,000 daltons.  
     
     
         15 . The method of  claim 14 , wherein said polymer has a molecular weight of from about 25,000 to about 50,000 daltons.  
     
     
         16 . The method of  claim 14 , wherein said polymer has a molecular weight of about 20,000, about 21,000, about 22,000, about 23,000, about 24,000, about 25,000, about 26,000, about 27,000, about 28,000, about 29,000, about 30,000, about 31,000, about 32,000, about 33,000, about 34,000, about 35,000, about 36,000, about 37,000, about 38,000, about 39,000, about 40,000, about 41,000, about 42,000, about 43,000, about 44,000, about 45,000, about 46,000, about 47,000, about 48,000, about 49,000 or about 50,000 daltons.  
     
     
         17 . The method of  claim 1  wherein amount of the drug is at least 10% (w/w) based on the mass of said conjugate.  
     
     
         18 . The method of  claim 1  wherein the amount of the drug is from about 10% to about 40% (w/w) based on the mass of said conjugate.  
     
     
         19 . The method of  claim 1  wherein amount of the drug is at least 20% (w/w) based on the mass of said conjugate.  
     
     
         20 . The method of  claim 1  wherein the amount of said drug is from about 20 to about 40% (w/w) based on mass of said conjugate.  
     
     
         21 . A method of treating a condition responsive to a therapeutic agent comprising administering to a subject an effective amount of a conjugate of a plurality of therapeutic agents and a water-soluble amino acid polymer wherein said plurality of therapeutic agents are covalently bonded to said polymer and said polymer comprises polyglutamate.  
     
     
         22 . The method of  claim 21 , wherein the condition is selected from the group consisting of prostate, breast, ovarian, colon, leukemia and lung cancers, malignant melanoma, head and neck cancers, gastric cancer and Kaposi's sarcoma.  
     
     
         23 . The method of  claim 21 , wherein the condition is selected from the group consisting of prostate, breast, ovarian, colon, leukemia and lung cancers.  
     
     
         24 . The method of  claim 21 , wherein the condition is ovarian cancer.  
     
     
         25 . The method of  claim 21 , wherein the condition is colon cancer.  
     
     
         26 . The method of  claim 21 , wherein the condition is leukemia.  
     
     
         27 . The method of  claim 21 , wherein the condition is lung cancer.  
     
     
         28 . The method of  claim 21 , wherein the condition is prostate cancer.  
     
     
         29 . The method of  claim 21  wherein the drug is a chemotherapeutic or antiangiogenic drug.  
     
     
         30 . The method of  claim 21  wherein at least one of said plurality of therapeutic agents is a taxoid, tamoxifen, etoposide, teniposide, fludarabine, doxorubicin, daunomycin, emodin, 5-fluorouracil, FUDR, estradiol, camptothecin, a retinoid, verapamil, an epothilone or a cyclosporin.  
     
     
         31 . The method of  claim 30 , wherein at least one of said plurality of therapeutic agents is paclitaxel or taxotere.  
     
     
         32 . The method of  claim 21 , wherein at least one of said plurality of therapeutic agents is paclitaxel.  
     
     
         33 . The method of  claim 21 , wherein said polymer has a molecular weight of from about 1 to about 100,000 daltons.  
     
     
         34 . The method of  claim 33 , wherein said polymer has a molecular weight of from about 20,000 to about 80,000 daltons.  
     
     
         35 . The method of  claim 34 , wherein said polymer has a molecular weight of from about 25,000 to about 50,000 daltons.  
     
     
         36 . The method of  claim 34 , wherein said polymer has a molecular weight of about 20,000, about 21,000, about 22,000, about 23,000, about 24,000, about 25,000, about 26,000, about 27,000, about 28,000, about 29,000, about 30,000, about 31,000, about 32,000, about 33,000, about 34,000, about 35,000, about 36,000, about 37,000, about 38,000, about 39,000, about 40,000, about 41,000, about 42,000, about 43,000, about 44,000, about 45,000, about 46,000, about 47,000, about 48,000, about 49,000 or about 50,000 daltons.  
     
     
         37 . The method of  claim 21  wherein amount of the drug is at least 10% (w/w) based on the mass of said conjugate.  
     
     
         38 . The method of  claim 21  wherein the amount of the drug is from about 10% to about 40% (w/w) based on the mass of said conjugate.  
     
     
         39 . The method of  claim 21  wherein amount of the drug is at least 20% (w/w) based on the mass of said conjugate.  
     
     
         40 . The method of  claim 21  wherein the amount of said drug is from about 20 to about 40% (w/w) based on mass of said conjugate.

Cited by (0)

No later patents cite this yet.

References (0)

No backward citations on record.