Minoxidil as a Prodrug: Review of Chemical, Pharmacological, and Technological Aspects in Alopecia Therapeutics

March 2026 in “ Mini-Reviews in Medicinal Chemistry ”

Gustavo Terra de Oliveira, Ana Beatriz Kimie Baiocco Ikegaki, Isadora Luziana Izidoro de Souza, Sandra Barbosa Neder Agostini, Maria Betânia de Freitas Marques, Magali Benjamim De Araújo

minoxidil minoxidil sulphate alopecia SULT1A1 enzyme hepatic sulphation oral minoxidil molecular solubility therapeutic index molecular absorption pharmaceutical technologies molecular release systems Rogaine

TLDR Oral minoxidil can be improved for hair loss treatment with personalized strategies and new technologies.

Minoxidil, originally an oral antihypertensive, is now used to treat alopecia by acting as a prodrug that requires conversion to minoxidil sulphate via hepatic sulphation. This review highlights the role of the SULT1A1 enzyme in treatment response, suggesting personalized strategies for alopecia therapy. Despite challenges like low solubility and a narrow therapeutic index, new pharmaceutical technologies such as minitablets and modified release systems aim to improve absorption and reduce side effects. The integration of various scientific disciplines is expected to enhance the reliability and effectiveness of oral minoxidil as a treatment for alopecia.

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