Testosterone and its esters are widely used for androgen replacement therapy. Testosterone undergoes 5 alpha-reduction to dihydrotestosterone (DHT) in the prostate and other tissues leading to potentially undesirable consequences in adult males.
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. It inhibits gonadotrophin release, suppresses testosterone and sperm production. Yet, 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 aromatization (to 7-alpha-methyl-estradiol) preserving the benefits estrogen imparts on male physiology.
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.
MENT, as a transdermal and/or intramuscular preparation, will have application in a wide range of indications beyond androgen replacement therapy and contraception, including, without limitation, primary hypogonadism, testicular failure, ASIH, baldness, sarcopenia, loss of bone mass, muscle wasting and cachexia, BPH, prostate cancer and of course, bodybuilding and sports performance enhancement.
Trestolone acetate is the chemical name of active ingredient in MENT. MENT is a registered trademark of Population Council, Inc. in the United States and/or other countries.
References
Sundaram K, Numar K. 7alpha-methyl-19-nortestosterone (MENT): the optimal androgen for male contraception and replacement therapy. Int J Androl. 2000;23 Suppl 2:13-5.
Anderson, Richard A., A. Michael Wallace, Naveed Sattar, Narender Kumar, and Kalyan Sundaram. “Evidence for tissue selectivity of the synthetic androgen 7α-methyl-19-nortestosterone in hypogonadal men,” Journal of Clinical Endocrinology and Metabolism 88(6): 2784–2793.
von Eckardstein, Sigrid, Gabriela Noe, Vivian Brache, Eberhard Nieschlag, Horacio Croxatto, Francisco Alvarez, Alfred Moo-Young, Irving Sivin, Narender Kumar, Margaret Small, and Kalyan Sundaram, Population Council International Committee for Contraception Research. “A clinical trial of 7-α-methyl-19-nortestosterone implants for possible use as a long-acting contraceptive for men,” Journal of Clinical Endocrinology and Metabolism 88(11): 5232–5239.
