Claims
- 1. A pharmaceutical composition comprising a conjugate comprising an anti-tumor drug conjugated to a water soluble polyglutamic acid polymer, wherein said polymer has a molecular weight of about 5,000 to about 100,000 daltons, wherein said drug is conjugated to said polymer so as to provide a drug conjugate having a higher water solubility than the unconjugated drug and the ability to accumulate in a tumor, and wherein said anti-tumor drug is paclitaxel, docetaxel, etoposide, teniposide, camptothecin or epothilone.
- 2. The pharmaceutical composition of claim 1, wherein said antitumor drug is directly conjugated to said water soluble polyglutamic acid polymer.
- 3. The pharmaceutical composition of claim 1, wherein said conjugate comprises paclitaxel.
- 4. The pharmaceutical composition of claim 1, wherein said conjugate comprises docetaxel.
- 5. The pharmaceutical composition of claim 2, wherein said conjugate comprises camptothecin.
- 6. The pharmaceutical composition of claim 1, wherein said conjugate comprises etoposide.
- 7. The pharmaceutical composition of claim 1, wherein said polyglutamic acid polymer is poly (L-glutamic) acid.
- 8. The pharmaceutical composition of claim 1, wherein said polyglutamic acid polymer is poly (D-glutamic) acid.
- 9. The pharmaceutical composition of claim 3, wherein said conjugate comprises up to 35% by weight of paclitaxel.
- 10. The pharmaceutical composition of claim 9, wherein said conjugate comprises from about 15% to about 25% by weight of paclitaxel.
- 11. The pharmaceutical composition of claim 10, wherein said drug conjugate has a molecular weight in the range of from 45 kd to 55 kd.
- 12. A pharmaceutical composition comprising a conjugate comprising an antitumor 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 daltons, said drug conjugate comprises up to 35% by weight of drug, 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 and the ability to accumulate in a tumor, and wherein said antitumor drug is paclitaxel.
- 13. The pharmaceutical composition of claim 12, wherein said antitumor drug is directly conjugated to said water soluble polyglutamic acid polymer.
- 14. A pharmaceutical composition comprising a conjugate of paclitaxel conjugated to a water soluble polymer comprising a polyglutamic acid polymer, wherein said polyglutamic acid polymer has a molecular weight of about 30,000 to about 60,000 daltons, and said conjugate comprises up to 35% by weight of paclitaxel, wherein said conjugate has a higher water solubility than unconjugated paclitaxel and the ability to accumulate in a tumor.
- 15. The pharmaceutical composition of claim 14, wherein said paclitaxel is directly conjugated at its 2′-hydroxyl group to said water soluble polyglutamic acid polymer.
- 16. The pharmaceutical composition of claim 1, wherein said conjugate comprises epothilone.
RELATED APPLICATIONS
This application is a continuation of application Ser. No. 08/815,104, filed Mar. 11, 1997, U.S. Pat. No. 5,977,163, which claims priority to U.S. Provisional Application No. 60/013,184, filed Mar. 12, 1996. The disclosures of the aforementioned applications are incorporated herein by reference in their entirety.
US Referenced Citations (22)
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Country |
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Sep 1993 |
EP |
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EP |
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EP |
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Non-Patent Literature Citations (2)
Entry |
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Provisional Applications (1)
|
Number |
Date |
Country |
|
60/013184 |
Mar 1996 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
08/815104 |
Mar 1997 |
US |
Child |
09/346263 |
|
US |