Trestolone
Encyclopedia
Trestolone is a synthetic androgen
Androgen
Androgen, also called androgenic hormone or testoid, is the generic term for any natural or synthetic compound, usually a steroid hormone, that stimulates or controls the development and maintenance of male characteristics in vertebrates by binding to androgen receptors...

 as a potential candidate drug for use in hormonal male contraceptive
Male contraceptive
Male contraceptives include condoms, withdrawal , and vasectomy. In other animals, castration is commonly used for contraception...

 methods. In males, regular administration of sufficient quantities of trestolone induces a state of temporary infertility
Infertility
Infertility primarily refers to the biological inability of a person to contribute to conception. Infertility may also refer to the state of a woman who is unable to carry a pregnancy to full term...

.

Trestolone is an experimental contraceptive treatment and is not yet available commercially. It is currently being evaluated for safety and effectiveness in scientific studies, supported by the Population Council
Population Council
The Population Council is an international, nonprofit, non-governmental organization. The Council conducts biomedical, social science, and public health research and helps build research capacities in developing countries. One-third of its research relates to HIV and AIDS; its other major program...

.

Mechanism of action

As a derivative of the anabolic steroid
Anabolic steroid
Anabolic steroids, technically known as anabolic-androgen steroids or colloquially simply as "steroids", are drugs that mimic the effects of testosterone and dihydrotestosterone in the body. They increase protein synthesis within cells, which results in the buildup of cellular tissue ,...

 hormone nandrolone
Nandrolone
Nandrolone is an anabolic steroid that may be present naturally in the human body, albeit in minute quantities of less than 0.4 ng/ml. Nandrolone is most commonly sold commercially as its decanoate ester and less commonly as a phenylpropionate ester...

, trestolone's viability as a male contraceptive is twofold.

Inhibition of sperm production

Spermatozoa are produced in the testes of males in a process called spermatogenesis
Spermatogenesis
Spermatogenesis is the process by which male primary germ cells undergo division, and produce a number of cells termed spermatogonia, from which the primary spermatocytes are derived. Each primary spermatocyte divides into two secondary spermatocytes, and each secondary spermatocyte into two...

. In order to render a man infertile, a hormone-based male contraceptive method must stop spermatogenesis by interrupting the release of gonadotropins from the pituitary gland
Pituitary gland
In vertebrate anatomy the pituitary gland, or hypophysis, is an endocrine gland about the size of a pea and weighing 0.5 g , in humans. It is a protrusion off the bottom of the hypothalamus at the base of the brain, and rests in a small, bony cavity covered by a dural fold...

. Even in low concetrations, trestolone is a potent inhibitor of the release of the gonadotropin hormones, luteinizing hormone
Luteinizing hormone
Luteinizing hormone is a hormone produced by the anterior pituitary gland. In females, an acute rise of LH called the LH surge triggers ovulation and development of the corpus luteum. In males, where LH had also been called interstitial cell-stimulating hormone , it stimulates Leydig cell...

 (LH) and follicle stimulating hormone (FSH).

In order for spermatogenesis to occur in the testes, both FSH and the male hormone testosterone
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...

  must be present. By inhibiting release of FSH, trestolone creates an endocrine environment in which conditions for spermatogenesis are not ideal. Manufacture of sperm is further impaired by the suppression of LH, which in turn drastically cutails the production of testosterone. Sufficient regular doses of trestolone cause severe oligozoospermia or azoospermia
Azoospermia
Azoospermia is the medical condition of a male not having any measurable level of sperm in his semen. It is associated with very low levels of fertility or even sterility, but many forms are amenable to medical treatment...

, and therefore infertility, in most male patients.

Trestolone-induced sterility has been found to be quickly reversible upon discontinuation.

Support of secondary sex characteristics

When LH release is inhibited, the amount of testosterone made in the testes declines dramatically. As a result of trestolone's gonadotropin-suppressing qualities, levels of serum testosterone fall sharply in patients. Testosterone is the primary hormone responsible for maintenance of male secondary sex characteristics.

Normally, inadequate testosterone levels cause undesirable effects, such as fatigue
Fatigue (physical)
Fatigue is a state of awareness describing a range of afflictions, usually associated with physical and/or mental weakness, though varying from a general state of lethargy to a specific work-induced burning sensation within one's muscles...

, loss of skeletal muscle
Skeletal muscle
Skeletal muscle is a form of striated muscle tissue existing under control of the somatic nervous system- i.e. it is voluntarily controlled. It is one of three major muscle types, the others being cardiac and smooth muscle...

 mass, reduced libido
Libido
Libido refers to a person's sex drive or desire for sexual activity. The desire for sex is an aspect of a person's sexuality, but varies enormously from one person to another, and it also varies depending on circumstances at a particular time. A person who has extremely frequent or a suddenly...

, and weight gain. However, the androgenic and anabolic properties of trestolone largely ameliorate this problem. Essentially, trestolone replaces testosterone's role as the primary male hormone in the body.

External links

  • MENT – project information from the Population Council
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