E. V. Nurieva, O. Yu. Kravtsova, A. V. Sydoriuk, E. V. Britikova, V. V. Britikov, N. A. Zefirov, E. R. Milaeva, O. N. Zefirova, “The homodimer approach to the design of a new long-acting depot prodrug of abiraterone”, Mendeleev Commun., 2024, Volume 34, Issue 4,Pages <nobr>502

This article is cited in 1 paper

Communications

The homodimer approach to the design of a new long-acting depot prodrug of abiraterone

E. V. Nurieva^a, O. Yu. Kravtsova^b, A. V. Sydoriuk^a, E. V. Britikova^c, V. V. Britikov^c, N. A. Zefirov^a, E. R. Milaeva^a, O. N. Zefirova^ab

^a Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
^b Federal Research Center for Innovator and Emerging Biomedical and Pharmaceutical Technologies, Moscow, Russian Federation
^c Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Minsk, Belarus

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.

Keywords: steroid derivatives, succinic acid, pimelic acid, citric acid, abiraterone prodrugs, depot formulations, twin drugs, cytochrome P450 17A1 inhibitors, plasma hydrolysis, prostate cancer.

Language: English

DOI: 10.1016/j.mencom.2024.06.010

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