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Enclomiphene

  • CAS no: 15690-57-0
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Enclomiphene is a selective estrogen receptor modulator (SERM) commonly used to treat low testosterone levels in men (low testosterone), especially low testosterone problems due to hypotesticular function (secondary low testosterone). Enclomiphene is a non-steroidal compound that indirectly increases testosterone levels by stimulating the release of gonadotropins in the body.

 

Enclomiphene Mechanism of action:

Enclomiphene reduces the negative feedback effect of estrogen on the hypothalamic-pituitary-gonadal axis (HPTA) by blocking estrogen receptors in the hypothalamus. In this way, it prompts the hypothalamus to secrete gonadotropin-releasing hormone (GnRH), which stimulates the pituitary to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

LH stimulates testosterone production in the testicles, while FSH is involved in sperm production.

What is the difference between Enclomiphene vs Clomiphene?

Enclomiphene and Clomiphene are both drugs used to promote testosterone production and treat low testosterone levels in men, but they differ in their chemical structure and mechanism of action. They are selective estrogen receptor modulators (SERMs), but Enclomiphene is a pure active isomer of Clomiphene, and the clinical effects and side effects of the two differ.

The main differences are:

Enclomiphene vs Clomiphene Composition and structure:

Clomiphene is a mixture containing two isomers: Enclomiphene and Zuclomiphene. The two isomers have different pharmacological properties.

Enclomiphene is the active isomer of Clomiphene, which is mainly used to stimulate the hypothalamus to release gonadotropin, thereby increasing testosterone levels.

Zuclomiphene is another isomer of Clomiphene, and although it is less effective in treatment, it has the potential to cause some side effects, such as a stronger stimulant effect on estrogen receptors.

Enclomiphene vs Clomiphene Mechanism of action:

Enclomiphene mainly acts as an anti-estrogen, promoting the release of gonadotropin by blocking the estrogen receptor in the hypothalamus, thereby increasing testosterone levels. It does not have a significant estrogen-like effect, so there are fewer estrogen-related side effects when used in men.

Clomiphene has certain estrogen-like effects because it contains Zuclomiphene, especially Zuclomiphene, which has a long half-life and can cause some estrogen-related side effects in the body, such as water retention and mood swings.

Enclomiphene vs Clomiphene Half-life:

Enclomiphene has a short half-life and is generally metabolized quickly in the body, making it easier to control and adjust doses with fewer side effects.

Clomiphene has a long half-life, especially Zuclomiphene, which stays in the body longer and can have long-term side effects.

Enclomiphene vs Clomiphene Side effects:

Enclomiphene, because it has no estrogen-like effect, has fewer side effects and is safer, especially in men. It does not cause the side effects associated with estrogen, such as mood swings, feminized breasts (mammary gland development), water retention, etc.

Clomiphene may cause a number of side effects, especially those associated with Zuclomiphene. Men who use Clomiphene for a long time sometimes experience mood swings, feminized breasts, and decreased libido.

Enclomiphene vs Clomiphene Uses and preferences:

Enclomiphene is commonly used to treat low testosterone in men because it is effective in increasing testosterone levels and has few side effects, especially when used for long periods of time.

Clomiphene can also be used to treat low testosterone in men, but because of its estrogen-like effects, it is more commonly used for ovulation induction therapy in women. In men, doctors may prefer to choose Enclomiphene to avoid the possible side effects of Zuclomiphene in Clomiphene.

It is used in the treatment of low testosterone in men, but its side effects may be more, and it is more commonly used in the treatment of ovulation in women.

 

How does Enclomiphene treat low testosterone?

Enclomiphene is a selective estrogen receptor modulator (SERM) for the treatment of men with low testosterone (low testosterone levels). It stimulates the natural production of testosterone by regulating the endocrine feedback mechanism in the body. Unlike traditional testosterone replacement therapy (TRT), Enclomiphene does not directly supplement testosterone, but restores natural testosterone production by activating endogenous mechanisms in the body.

The mechanism of action of Enclomiphene in the treatment of low testosterone

Blocking estrogen negative feedback mechanism:

Under normal physiological conditions, estrogen sends feedback signals to the brain by binding to estrogen receptors in the hypothalamus that inhibit the production of gonadotropin-releasing hormone (GnRH). This reduces the luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secreted by the pituitary gland, thereby inhibiting testosterone production.

Enclomiphene acts as an anti-estrogen, blocking the negative feedback effect of estrogen by binding to estrogen receptors in the hypothalamus and pituitary gland. This process increases the secretion of GnRH, which in turn stimulates the pituitary to release more LH and FSH.

Promotes the release of gonadotropin:

Increased LH and FSH act on Leydig cells and Sertoli cells in the testes, respectively.

LH stimulates the Leydig cells of the testes and promotes testosterone production.

FSH promotes sperm production and improves sperm quantity and quality.

In the process, Enclomiphene can improve testosterone levels by activating the natural reproductive endocrine axis (HPTA, hypothalamic-pituitary-testicular axis) in the body, and maintain the normal production of sperm.

Maintenance of endogenous testosterone production:

A key advantage of Enclomiphene is its ability to maintain the normal function of the testicles. Unlike exogenous testosterone replacement therapy (TRT), Enclomiphene does not inhibit testosterone production in the testes. TRT, by directly supplementing exogenous testosterone, will inhibit the body's gonadotropin secretion, leading to testicular function decline and even atrophy. Enclomiphene maintains the normal response of the testicles to LH and FSH, and AIDS in the natural production of testosterone and sperm.

The advantages of Enclomiphene for treating low testosterone levels

Avoid testicular atrophy:

Men who use traditional testosterone replacement therapy are often at risk for testicular atrophy because exogenous testosterone suppresses the production of LH and FSH, causing the testicles to stop working. Enclomiphene prevents testicular atrophy by promoting the secretion of LH and FSH and maintaining the natural function of the testosterone.

Maintain fertility:

TRT often leads to reduced spermatogenesis or even infertility in men because exogenous testosterone inhibits the spermatogenesis process. Enclomiphene helps in the normal production of sperm and preserves male fertility by maintaining or increasing FSH levels. Therefore, it is suitable for men who need to boost their testosterone levels but still want to preserve their fertility.

Avoid the side effects of exogenous testosterone:

TRT may cause a number of side effects, such as breast development, increased cardiovascular risk, and increased blood consistency. Enclomiphene avoids many of the problems caused by exogenous testosterone by stimulating the body's natural testosterone production.

Safer long-term use:

Because Enclomiphene works by maintaining the body's natural hormone feedback mechanism, it could be a safer treatment for long-term low testosterone. Compared to the potential side effects of long-term TRT use, Enclomiphene is more attractive for those who want to maintain natural testosterone production over the long term.

 

Does Enclomiphene cause estrogen-related side effects?

Enclomiphene is an anti-estrogen drug that blocks estrogen receptors in the hypothalamus and pituitary gland, thereby preventing negative estrogen feedback. This means that it does not stimulate estrogen receptors in the body, so the side effects associated with estrogen (such as breast development, edema, mood swings, etc.) are less likely to occur.

Comparison with Clomiphene:

Clomiphene consists of two isomers, including Zuclomiphene, which has certain estrogen-like effects and may trigger estrogen-related side effects. In contrast, Enclomiphene, which is primarily its active isomer, has a strong anti-estrogenic effect, thereby reducing the risk of estrogen-related side effects.

Possible side effects of Enclomiphene

Although Enclomiphene has fewer estrogen-related side effects, in individual cases, some side effects may still occur, mainly including:

Mild discomfort: Some men may experience slight breast sensitivity or discomfort when using Enclomiphene, but these are relatively rare and generally short-lived.

Mood changes: While uncommon, some users may experience mild mood swings.

Headache or nausea: These are also possible side effects, but are usually mild.

Name:Enclomiphene

Other names:Androxal, (E)-clomifene, RMI-16289, enclomid, enclomifene citrate, enclomiphene citrate

Cas Number: 15690-57-0

Formula: C26H28ClNO

Molar mass:405.97

Half-life: 10H