Keywords
abiraterone prodrugs
citric acid
cytochrome P450 17A1 inhibitors
depot formulations
pimelic acid
plasma hydrolysis
prostate cancer.
steroid derivatives
succinic acid
twin drugs
Abstract
The synthesis of homodimeric bis-esters of abiraterone (an inhibitor of androgens synthesis used for treatment of prostate cancer) as a novel depot form of the drug intended for parenteral administration has been undertaken. The conjugate with succinic linker has been synthesized, while only mono-esters of malic and citric acid were obtained. The target ‘twin’ demonstrated excellent characteristics in preliminary biotests, proving the concept of long-lasting depot-prodrug.
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