Minoxidil: a comprehensive review

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/beta-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.