Minoxidil: a comprehensive review

Abstract

Topical minoxidil (5% foam, 5% solution, and 2% solution) is FDA-approved for androgenetic alopecia (AGA) in men and women.

Mechanism of action: Minoxidil acts through multiple pathways (vasodilator, anti-inflammatory agent, inducer of the Wnt/β-catenin signaling pathway, an antiandrogen), and may also affect the length of the anagen and telogen phases.

Pharmacokinetics: Approximately 1.4% of topical minoxidil is absorbed through the skin. Minoxidil is a prodrug that is metabolized by follicular sulfotransferase to minoxidil sulfate (active form). Those with higher sulfotransferase activity may respond better than patients with lower sulfotransferase activity.

Clinical efficacy (topical minoxidil): In a five-year study, 2% minoxidil exhibited peak hair growth in males at year one with a decline in subsequent years. Topical minoxidil causes hair regrowth in both frontotemporal and vertex areas. The 5% solution and foam were not significantly different in efficacy from the 2% solution.

Oral and Sublingual minoxidil (not FDA approved; off-label): After 6 months of administration, minoxidil 5 mg/day was significantly more effective than topical 5% and 2% in male AGA. Low-dose 0.5–5 mg/day may also be safe and effective for female pattern hair loss and chronic telogen effluvium. Sublingual minoxidil may be safe and effective in male and female pattern hair loss.

Keywords:

• Hair loss
• androgenetic alopecia
• AGA
• minoxidil
• topical
• oral
• sublingual
• Rogaine

Disclosure statement

AKG is a consultant for Bausch Health, Ortho Dermatologics, and Moberg Pharma. Mediprobe Research Inc. is a not-for-profit, noncommercial research group, thus MT, MV, MAB have no conflict of interest to declare.