Mesterolone is an oral synthetic androgen, chemically 1α-methyl-5α-androstan-17β-ol-3-one, a methylated form of dihydrotestosterone (DHT). It was made by Schering and sold as Proviron, and it was studied in the 1980s as a treatment for male infertility. We found no mesterolone product approved in the US.
Also known as: Proviron, 1α-methyl-DHT.
We found no mesterolone product in FDA's Drugs@FDA database, so there are no US label strengths to list. The infertility trials below used 75 mg and 150 mg a day. These are study protocols, not a recommendation.
Mesterolone has no FDA label for people that we could find. It is a Schedule III controlled substance in the US: the federal list of anabolic steroids names it as mesterolone (1α-methyl-17β-hydroxy-5α-androstan-3-one) in 21 CFR 1308.13(f)(45), so having it without a valid prescription is illegal. WADA lists it among anabolic androgenic steroids (S1.1), banned in sport at all times.
In a World Health Organization trial at 7 centres (1989), 248 infertile couples were randomized to 75 mg or 150 mg of mesterolone a day or placebo for the man for 6 months. Pregnancy rates 8 months later were 9% on placebo, 12% on 75 mg and 16% on 150 mg, differences too uncertain to show a benefit, and semen quality did not change apart from a rise in sperm count at 3 months that was largest on placebo. In a 12-month trial of 52 men (Gerris 1991), pregnancy rates were 26% on 150 mg a day versus 48% on placebo; the authors said this cast doubt on its use for infertility.
Published case reports describe liver injury caused by mesterolone (2019) and mania in a person with no prior mental illness (2012).
We found no published human study giving mesterolone's half-life or time to peak that we could cite, so we do not list one.
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