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Trestolone (MENT) is an experimental androgen/anabolic steroid (AAS), selective androgen receptor modulator (SARM), and progestogen drug that’s being researched for potential use as a male hormonal contraception methodology and to deal with hypogonadism. (1, 2, 3, 4)
It has by no means been accepted for medical use, although.
Trestolone is a potent 19-nortestosterone by-product from the identical class of steroids as nandrolone and trenbolone, and is an agonist of the androgen receptor, the organic goal of androgens equivalent to testosterone. (5)
Being an artificial progestogen, or progestin, it additionally acts as an agonist on the progesterone receptor, which is the organic goal of progesterone.
Trestolone has antigonadotropic results because of its androgenic and progestognenic motion. (1, 5)
Trestolone has contraceptive results on males because of these results, which causes reversible suppression of sperm manufacturing. (1)
Desk of Contents:
- Chemical info
- Anabolic exercise
- Androgen alternative remedy
- Dosage
- Half life
- Results on the prostate
- Male contraceptive
Chemical Data
- Different Names: MENT, MENTR, RU-27333, 7α-Methylnandrolone, 7α-Methyl-19-nortestosterone, 7α-Methylestr-4-en-17β-ol-3-one
- CAS Quantity: 3764-87-2
- Chemical Construction: 7α-Methylestr-4-en-17β-ol-3-one
- Class: Anabolic Androgenic Steroid, Selective Androgen Receptor Modulator, Progestogen, Antigonadotropin
- Anabolic/Androgenic Ratio: 2300:650
- Molecular Weight: 288.431 g·mol−1
Anabolic Exercise
Trestolone has a myotrophic motion that’s about 10 occasions than that of testosterone.
Trestolone has an anabolic to androgenic ratio of 2300:650 (for comparability the ranking is 100:100 for testosterone and 500:500 for trenbolone). (6, 10)
Not many different AAS have greater anabolic scores, certainly one of which often called methyltrienolone (metribolone) is rated at roughly 12000:6000.
It’s so potent that it serves because the gold customary for all lab assays that consider androgen receptor binding.
Androgen Substitute Remedy
Trestolone is the one AAS at the moment being produced that appears to be able to sustaining regular male physiology, together with sexual perform, within the absence of any testosterone. (1, 8)
Many anecdotal studies recommend that trestolone gives a euthymic and assured feeling.
The molecule is just not vulnerable to metabolism by the 5-reductase enzyme however does aromatise offering estrogenic results. (7)
It doesn’t straight influence estradiol. It aromatises into 7α-Methylestradiol (7α-Me-E2).
Researchers found that trestolone has anabolic efficacy that’s 10 occasions greater than testosterone whereas additionally being 12 occasions extra suppressive to the HTPA. (10)
Though it’s classed as a progestin, it is proven to have minimal affinity for the progesterone and mineralocorticoid receptors, regardless of trestolone being a 19-nortestosterone by-product. (9)
Dosage
400-700mcg of trestolone each day is sufficient to obtain the identical outcomes as the common male’s each day manufacturing of 4-7mg of testosterone.
4-7mg of testosterone is important to keep up muscular progress and sexual perform.
One, two, and 4 patches that delivered 400mcg per day every had been utilized in a scientific analysis on contraception to create the efficient each day dosages.
- 1 patch: 400mcg (0.4mg)
- 2 patches: 800mcg (0.8mg)
- 4 patches: 1600mcg (1.6mg)
Scientific investigations with doses as little as 400-700mcg and as excessive as 1-2mg found a dosage that was fairly just like testosterone alternative dosages.
Half-Life
The estimated half-life of an intravenous injection of unesterified trestolone is simply ~40 minutes for 500mcg. (13)
As a result of extended absorption interval of intramuscular injection, a examine utilizing trestolone IM injection found an extended half-life of ~224 minutes.
About one to 2 hours after the injections, peak trestolone concentrations, which had been dose-dependent, had been attained. (12)
Esterified variations of trestolone, equivalent to trestolone acetate or decanoate, had been examined to be used because of their longer half lives.
Results on the Prostate
Quite a few research help trestolone to be a prostate-safe androgen and present absence of 5α-reductase metabolism. (3, 7)
Androgen restriction remedy is primarily used to deal with prostate most cancers, which is androgen-dependent.
In these conditions, trestolone has potential to be a safer different to testosterone whereas offering related advantages, equivalent to lowering the danger of Alzheimers illness. (11)
As a result of its exercise within the prostate is just not magnified, a dosage of trestolone enough to keep up regular functioning, muscle mass and gonadotrophin manufacturing is not going to trigger the prostate to develop into overstimulated.
In consequence, trestolone might be given to males with the data that it’s going to have a decrease threat of inflicting prostatic hyperplasia or prostate most cancers than testosterone. (3)
Trestolone might also be thought-about to be used in circumstances of prostatic hyperplasia, muscular losing, and hypogonadism. (3)
It’s the first androgen that, compared to testosterone, has a optimistic well being impact, particularly on the prostate.
It could be used as a male contraceptive, and has potential purposes with a variety of problems, together with hypogonadism, prostatic hyperplasia, and muscle losing. (3)
Male Contraceptive
Trestolone was being developed as a quickly reversible oral or implant-based male contraceptive, it’s 12 occasions extra suppressive than testosterone. In 2013, the analysis got here to an abrupt finish with no clear purpose. (10)
Its efficacy as a male contraceptive may be very excessive, with 82% of sufferers azoospermic within the first six months and 100% had been azoospermic within the second six months of remedy.
Testosterone is commonly paired with a progestin equivalent to etonogestrel to additional suppress spermatogenesis.
Nevertheless, the outcomes of a examine point out that trestolone by itself is enough sufficient to suppress spermatogenesis, and likewise that its efficacy as use for androgen alternative is unaffected when paired with the second compound. (5)
Restoration of Spermatogenesis
A radical human investigation on male individuals evaluated the results of trestolone to testosterone on spermatogenesis, intercourse want, and security biomarkers associated to androgen utilization, each alone and together with the progestin etonogestrel. (13)
This was an intensive analysis with 29 individuals who underwent 48 weeks of testing.
8 Individuals acquired:
- Three 600mg testosterone pellets, one given each 12 weeks.
- Two trestolone pellets, every containing 135mg of trestolone acetate (predicted to launch 400mcg each day).
- Each teams acquired 68mg etonogestrel.
After 12 weeks of supplementation, 80% of each teams’ sperm manufacturing had considerably decreased, from a median of 55×106 mL to simply 1×106 mL.
Restoration of spermatogenesis occurred considerably sooner with trestolone than with testosterone.
Semen focus rose to over 20×106 mL over the 16-week restoration interval for the trestolone group, however azoospermia endured within the testosterone group till 28 weeks had handed.
References
This part incorporates hyperlinks to analysis, research, and sources of knowledge for this text, in addition to authors, contributors, and so forth. All sources, together with the article and info, are subjected to a sequence of high quality, reliability, and relevance checks.
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This evidence-based evaluation of trestolone options 13 references, listed beneath.
1. Nieschlag E, Kumar N, Sitruk-Ware R. 7α-methyl-19-nortestosterone (MENTR): the inhabitants council’s contribution to analysis on male contraception and remedy of hypogonadism. Contraception. (2013)
2. J. Elks. The Dictionary of Medication: Chemical Knowledge: Chemical Knowledge, Buildings and Bibliographies. Springer. (14 November 2014)
3. Sundaram Okay, Kumar N, Bardin CW. 7 alpha-methyl-nortestosterone (MENT): the optimum androgen for male contraception. Ann Med. (April 1993)
4. Corona G, Rastrelli G, Vignozzi L, Maggi M. Rising remedy for the remedy of male hypogonadism. Skilled Opin Emerg Medication. (2012)
5. García-Becerra R, Ordaz-Rosado D, Noé G, Chávez B, Cooney AJ, Larrea F. Comparability of 7α-methyl-19-nortestosterone effectiveness alone or mixed with progestins on androgen receptor mediated-transactivation. Replica. (2012)
6. Sinnesael M, Callewaert F, Morreels M, et al. 7α-methyl-19-nortestosterone vs. testosterone implants for hypogonadal osteoporosis: a preclinical examine within the aged male orchidectomized rat mannequin. Int J Androl. (2011)
7. LaMorte A, Kumar N, Bardin CW, Sundaram Okay. Aromatization of seven alpha-methyl-19-nortestosterone by human placental microsomes in vitro. J Steroid Biochem Mol Biol. (1994)
8. Sundaram Okay, Kumar N, Bardin CW. 7 alpha-Methyl-19-nortestosterone: a really perfect androgen for alternative remedy. Current Prog. Horm. Res. (1994)
9. Liu A, Carlson KE, Katzenellenbogen JA. Synthesis of excessive affinity fluorine-substituted ligands for the androgen receptor. Potential brokers for imaging prostatic most cancers by positron emission tomography. J Med Chem. (1992)
10. Kumar N, Didolkar AK, Monder C, Bardin CW, Sundaram Okay. The organic exercise of seven alpha-methyl-19-nortestosterone is just not amplified in male reproductive tract as is that of testosterone. Endocrinology. (1992) (Comparative Research)
11. Pike CJ, Carroll JC, Rosario ER, Barron AM. Protecting actions of intercourse steroid hormones in Alzheimer’s illness. Frontiers in Neuroendocrinology. (2009, Jul)
12. Walton, Melanie J., et al. 7α-methyl-19-nortestosterone (MENT) vs Testosterone in Mixture With Etonogestrel Implants for Spermatogenic Suppression in Wholesome Males. Journal of Andrology. (2007)
13. Kumar N, Suvisaari J, Tsong YY, et al. Pharmacokinetics of seven alpha-methyl-19-nortestosterone in males and cynomolgus monkeys. J Androl. (1997)
✔ Citations with a tick point out the data is from a trusted supply.
The knowledge supplied on this article is just not supposed to exchange skilled medical recommendation, analysis, or remedy. All the time search the steerage of a doctor or different competent skilled earlier than following recommendation or taking any complement. See our phrases and situations.
We strictly don’t advise anybody to make use of, or think about using, any exogenous hormone or chemical equivalent to trestolone, except suggested or prescribed to take action by a certified physician. Doing so might lead to severe and long-term antagonistic results.