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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.
 |
|
Substance name
|
Trestolone acetate [USAN];
Orgasteron acetate; 7
alpha-Methyl-19-nortestosterone |
| Chemical name |
17 beta-hydroxy-7
alpha-methylestr-4-en-3-one acetate |
| Systematic name |
IUPAC:
[(7R,9S,14S,17S)-7,13-dimethyl-3-oxo-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]
acetate |
| CAS number |
6157-87-5; 3764-87-2 (base) |
| Merck Index Number |
|
| Molecular formula |
C21-H30-O3 |
| Molecular weight |
330.465 g/mol |
| Pregnancy category |
X |
| Legal status |
Illegal (US); DEA Schedule III (US) |
| Routes of administration |
Transdermal, Intramuscular |
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.
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