Fatty acid-anticancer conjugates and uses thereof
First Claim
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1. A fatty acid-anticancer compound conjugate composition for administration to a subject, comprising at least one fatty acid-anticancer compound conjugate in a container for administration to a subject, wherein the amount of the fatty acid-anticancer compound in the container is at least about 30% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the unconjugated at least one anticancer compound, wherein the container is a container for intravenous administration.
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Abstract
The invention provides conjugates of fatty acids and anticancer agents useful in treating cancer, and compositions and formulations thereof. Methods for using the conjugates also are provided.
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97 Claims
- 1. A fatty acid-anticancer compound conjugate composition for administration to a subject, comprising at least one fatty acid-anticancer compound conjugate in a container for administration to a subject, wherein the amount of the fatty acid-anticancer compound in the container is at least about 30% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the unconjugated at least one anticancer compound, wherein the container is a container for intravenous administration.
- 5. A method for treating a subject having an abnormal mammalian cell proliferative disorder, comprising administering to the subject a fatty acid-anticancer compound conjugate composition in an amount which is at least about 30% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the unconjugated at least one anticancer compound.
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9. A kit for administration of a fatty acid-anticancer compound conjugate composition to a subject, comprising
a container containing at least one fatty acid-anticancer compound conjugate, and instructions for administering the at least one fatty acid-anticancer compound conjugate to subject in need of such treatment in an amount which is at least about 30% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the unconjugated at least one anticancer compound.
- 10. An injectable preparation of at least one fatty acid-taxane conjugate composition, comprising greater than about 6 mg/ml of the at least one fatty acid-taxane conjugate composition.
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13. An injectable composition of at least one fatty acid-taxane conjugate in a polyoxyethylated castor oil, comprising less than about 0.3 mg/ml of the at least one fatty acid-taxane conjugate.
- 14. A fatty acid-taxane conjugate composition, comprising greater than about 6 mg/ml of at least one fatty acid-taxane conjugate, and a surfactant.
- 18. A fatty acid-taxane conjugate composition, comprising at least one fatty acid-taxane conjugate and a surfactant, wherein the ratio of the weight of the at least one fatty acid-taxane conjugate and volume of the surfactant is at least about 50 mg/ml.
- 22. A fatty acid-taxane conjugate composition, comprising at least one fatty acid-taxane conjugate and a solvent, wherein the ratio of the weight of the at least one fatty acid-taxane conjugate and volume of the solvent is at least about 42 mg/ml.
- 27. A fatty acid-taxane conjugate composition, comprising at least about 37 mg/ml of at least one fatty acid-taxane conjugate.
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46. A method for increasing the therapeutic index of anticancer compounds in a subject, comprising:
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conjugating a fatty acid to an anticancer compound to form a fatty acid-anticancer compound conjugate; and
administering the fatty acid-anticancer compound conjugate to the subject, whereby the therapeutic index of the anticancer compound is improved relative to non-conjugated formulations of the anticancer compound, and wherein the fatty acid-anticancer compound conjugate is in an amount which is at least about 30% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the non-conjugated anticancer compound. - View Dependent Claims (47, 48, 49, 50, 51, 52)
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- 53. A method for administering a fatty acid-taxane conjugate to a subject in need of such treatment, comprising infusing the conjugate in fewer than 3 hours.
Specification