Fatty acid-anticancer conjugates and uses thereof

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.

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 10% 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. 
     
     
         2 - 11 . (canceled) 
     
     
         12 . The fatty acid-anticancer compound conjugate composition of  claim 1 , wherein the anticancer compound is a taxane. 
     
     
         13 . The fatty acid-anticancer compound conjugate composition of  claim 12 , wherein the taxane is paclitaxel or docetaxel. 
     
     
         14 . The fatty acid-anticancer compound conjugate composition of  claim 1 , wherein the conjugate is not encapsulated in a liposome. 
     
     
         15 . The fatty acid-anticancer compound conjugate composition of  claim 1 , wherein the fatty acid is a C8-C26 unbranched, naturally occurring fatty acid. 
     
     
         16 . The fatty acid-anticancer compound conjugate composition of  claim 1 , wherein the fatty acid is docosahexaenoic acid. 
     
     
         17 . 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 10% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the unconjugated at least one anticancer compound. 
     
     
         18 - 27 . (canceled) 
     
     
         28 . The method of  claim 17 , wherein the anticancer compound is a taxane. 
     
     
         29 . The method of  claim 28 , wherein the taxane is paclitaxel or docetaxel. 
     
     
         30 . (canceled) 
     
     
         31 . The method of  claim 17 , wherein the fatty acid is a C8-C26 unbranched, naturally occurring fatty acid. 
     
     
         32 . The method of  claim 17 , wherein the fatty acid is docosahexaenoic acid. 
     
     
         33 . 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 10% on a molar basis greater than the maximum tolerated dose (MTD) in the subject for the unconjugated at least one anticancer compound.   
     
     
         34 - 42 . (canceled) 
     
     
         43 . The kit of  claim 33 , wherein the anticancer compound is paclitaxel or docetaxel. 
     
     
         44 - 46 . (canceled) 
     
     
         47 . The kit of  claim 33 , wherein the fatty acid is docosahexaenoic acid. 
     
     
         48 - 118 . (canceled) 
     
     
         119 . The fatty acid-anticancer compound conjugate composition of  claim 1 , wherein the anticancer compound is doxorubicin. 
     
     
         120 . The fatty acid-anticancer compound conjugate composition of  claim 1 , wherein the fatty acid is linoleic acid. 
     
     
         121 . The method of  claim 17 , wherein the anticancer compound is doxorubicin. 
     
     
         122 . The method of  claim 17 , wherein the fatty acid is linoleic acid. 
     
     
         123 . The kit of  claim 33 , wherein the anticancer compound is doxorubicin. 
     
     
         124 . The kit of  claim 33 , wherein the fatty acid is linoleic acid.