Claims
- 1. A pharmaceutical composition comprising a taxane and at least one nonaqueous, pharmaceutically acceptable solvent, wherein the taxane has a solubility in ethanol at room temperature of at least 200 mg/ml and an ID50 value determined relative to the HCT116 cell line that is at least 4 times less than that of paclitaxel.
- 2. The composition of claim 1 wherein the ID50 value of the taxane is at least 5 times less than that of paclitaxel.
- 3. The composition of claim 2 wherein the ID50 value of the taxane is at least 6 times less than that of paclitaxel.
- 4. The composition of claim 3 wherein the ID50 value of the taxane is at least 7 times less than that of paclitaxel.
- 5. The composition of claim 4 wherein the ID50 value of the taxane is at least 8 times less than that of paclitaxel.
- 6. The composition of claim 5 wherein the ID50 value of the taxane is at least 9 times less than that of paclitaxel.
- 7. The composition of claim 6 wherein the ID50 value of the taxane is at least 10 times less than that of paclitaxel.
- 8. The composition of claim 1 wherein the taxane concentration is between 0.01 mg and 10 mg per ml of the composition.
- 9. The composition of claim 1 wherein the taxane dosage is at least 20 mg/m2.
- 10. The composition of claim 9 wherein the taxane dosage is between 20 mg/m2 and about 600 mg/m2.
- 11. The composition of claim 10 wherein the taxane dosage is between about 25 mg/m2 and about 400 mg/m2.
- 12. The composition of claim 11 wherein the taxane dosage is between about 40 mg/m2 and about 300 mg/m2.
- 13. The composition of claim 12 wherein the taxane dosage is between about 50 mg/m2 and about 200 mg/m2.
- 14. The composition of claim 1 wherein the taxane has the formula: whereinone of R7 and R10 is hydroxy and the other is acyloxy; X3 is substituted or unsubstituted alkyl, alkenyl, alkynyl, phenyl or heterocyclo; X5 is —COX10, —COOX10, or —CONHX10; X10 is hydrocarbyl, substituted hydrocarbyl, or heterocyclo; R2 is acyloxy; R9 is keto, hydroxy, or acyloxy; R14 is hydrido or hydroxy; and Ac is acetyl.
- 15. The composition of claim 14 wherein the composition is for parenteral administration.
- 16. The composition of claim 14 wherein the composition is for oral administration.
- 17. The composition of claim 14 wherein X3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C2-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl.
- 18. The composition of claim 14 wherein X5 is —COX10 and X10 is substituted or unsubstituted phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl or X5 is —COOX10 and X10 is substituted or unsubstituted C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl.
- 19. The composition of claim 14 wherein R14 is hydrido and R2 is benzoyloxy.
- 20. The composition of claim 14 wherein R7 is hydroxy and R10 is R10aC(O)O—, R10aR10bNC(O)O—, R10aOC(O)O— or R10aSC(O)O— wherein R10a is hydrocarbyl, substituted hydrocarbyl or heterocyclo and R10b is hydrogen, hydrocarbyl, substituted hydrocarbyl or heterocyclo.
- 21. The composition of claim 20 wherein X3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C2-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl.
- 22. The composition of claim 20 wherein X5 is —COX10 and X10 is substituted or unsubstituted phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl or X5 is —COOX10 and X10 is substituted or unsubstituted C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl.
- 23. The composition of claim 20 wherein R14 is hydrido and R2 is benzoyloxy.
- 24. The composition of claim 20 wherein R14 is hydroxy; X3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C2-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl; X5 is —COX10 and X10 is phenyl, or X5 is —COOX10 and X10 is t-butyl.
- 25. The composition of claim 24 wherein X3 is furyl or thienyl.
- 26. The composition of claim 25 wherein X5 is —COOX10 and X10 is t-butyl.
- 27. The composition of claim 14 wherein R10 is hydroxy and R7 is R7aC(O)O—, R7aR7bNC(O)O—, R7aOC(O)O— or R7aSC(O)O— wherein R7a is hydrocarbyl, substituted hydrocarbyl or heterocyclo and R7b is hydrogen, hydrocarbyl, substituted hydrocarbyl or heterocyclo.
- 28. The composition of claim 27 wherein X3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C2-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl.
- 29. The composition of claim 27 wherein X5 is —COX10 and X10 is substituted or unsubstituted phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl or X5 is —COOX10 and X10 is substituted or unsubstituted C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl.
- 30. The composition of claim 27 wherein R14 is hydrido and R2 is benzoyloxy.
- 31. The composition of claim 27 wherein R14 is hydroxy; X3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, C2-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl; X5 is —COX10 and X10 is phenyl, or X5 is —COOX10 and X10 is t-butyl.
- 32. The composition of claim 31 wherein X3 is furyl or thienyl.
- 33. The composition of claim 32 wherein X5 is —COOX10 and X10 is t-butyl.
REFERENCE TO RELATED APPLICATIONS
This application claims priority based on the following U.S. provisional applications: Ser. No. 60/179,684, filed on Feb. 2, 2000; Ser. No. 60/179,793, filed on Feb. 2, 2000; Ser. No. 60/179,782, filed on Feb. 2, 2000; Ser. No. 60/179,669, filed on Feb. 2, 2000; Ser. No. 60/179,671, filed on Feb. 2, 2000; Ser. No. 60/179,670, filed on Feb. 2, 2000; and Ser. No. 60/179,794, filed on Feb. 2, 2000, all incorporated herein by reference.
US Referenced Citations (10)
Provisional Applications (8)
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Number |
Date |
Country |
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60/179684 |
Feb 2000 |
US |
|
60/179793 |
Feb 2000 |
US |
|
60/179782 |
Feb 2000 |
US |
|
60/179669 |
Feb 2000 |
US |
|
60/179671 |
Feb 2000 |
US |
|
60/179670 |
Feb 2000 |
US |
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60/179794 |
Feb 2000 |
US |
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60/179672 |
Feb 2000 |
US |