Trestolone or 7 alpha-methyl-19-nortestosterone (MENT) is a synthetic androgen that is ten times as potent as testosterone. MENT is not 5-alpha reduced to DHT. MENT provides adequate replacement therapy for most androgen-dependant functions. MENT has a faster metabolic clearance rate than testosterone and, in contrast to testosterone, MENT does not bind to sex hormone binding globulin (SHBG). MENT remains capable of aromatisation (to 7-alpha-methyl-estradiol) preserving the benefits of estrogen imparts on male physiology.
Trestolone was first described in 1963. However, it was not subsequently studied again until 1990. Development of trestolone for potential use in male hormonal contraception and androgen replacement therapy was started by 1993, and continued thereafter.
Trestolone is an agonist of the androgen receptor (AR), similarly to androgens like testosterone and dihydrotestosterone (DHT). Trestolone is not a substrate for 5α-reductase and hence is not potentiated or inactivated in so-called “androgenic” tissues like the skin, hair follicles, and prostate gland. As such, it has a high ratio of anabolic to androgenic activity, similarly to other nandrolone derivatives. Trestolone is a substrate for aromatase and hence produces the estrogen 7α-methylestradiol as a metabolite. The aromatizing effects can be controlled with an AI.
Sufficient regular doses of Trestolone cause severe oligozoospermia or azoospermia, and therefore infertility, in most men. However, Trestolone-induced infertility has been found to be quickly reversible upon discontinuation.
The Population Council has investigated MENT [specifically MENT Acetate (MENT Ac)] for long-term clinical use for contraceptive purposes and hormone replacement therapy. Initial trials suggest it may be an ideal candidate since it is a non-5-alpha reducible androgen and requires lower doses due to its significantly increased potency over testosterone.
Various forms of MENT in human pharmaceutical preparations and devices for contraception and hormone therapy, specifically MENT Ac implant and MENT transdermal gel and patch formulations, are currently under clinical investigation. MENT is absorbed transdermally up to three times the rate of testosterone – 17 methyl testosterone and 17-α methyl testosterone.
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