Epitiostanol

Epitiostanol is an androgen and anabolic steroid (AAS) medication and derivative of dihydrotestosterone (DHT) that is used in Japan to treat breast cancer. It is taken by mouth.

Medical uses

Epitiostanol is used in the treatment of breast cancer. It has been found to be effective in the treatment of estrogen receptor-positive breast cancer, particularly in postmenopausal women. The drug works by inhibiting the effects of estrogen in the breast tissue, which can help to slow or stop the growth of certain types of breast cancer cells that require estrogen to grow.

Pharmacology

Pharmacodynamics

As a derivative of dihydrotestosterone, epitiostanol has both androgenic and anabolic effects. It acts as an antiestrogen by its mechanism of action, competing with estrogen for receptor sites in target organs such as the breast. This competition can inhibit estrogen-mediated processes, including the growth of certain types of breast cancer cells. Unlike many other AAS, epitiostanol does not undergo aromatization, meaning it does not convert to estrogen in the body, which is beneficial in the context of treating estrogen receptor-positive breast cancer.

Pharmacokinetics

The pharmacokinetics of epitiostanol, including its absorption, distribution, metabolism, and excretion, are not well-documented in the scientific literature. However, as an oral medication, it is assumed to undergo first-pass metabolism in the liver, which may affect its bioavailability and overall effectiveness.

Adverse effects

The adverse effects of epitiostanol are similar to those of other androgen and anabolic steroid medications. These can include masculinization, acne, and changes in liver function tests. Due to its antiestrogenic effects, it may also cause symptoms related to estrogen deficiency, such as hot flashes or osteoporosis, particularly with long-term use.

Chemistry

Epitiostanol is a synthetic derivative of dihydrotestosterone, specifically, it is a 2α,3α-epithio derivative of DHT. This modification confers its antiestrogenic activity and distinguishes it from other AAS in terms of its mechanism of action and therapeutic use.

History

Epitiostanol was developed and introduced for medical use in Japan. It has been used in the treatment of breast cancer for several decades and has contributed to the therapeutic options available for managing this disease, particularly in cases where estrogen plays a role in cancer progression.

Society and culture

Legal status

In Japan, epitiostanol is approved for medical use in the treatment of breast cancer. Its legal status in other countries may vary, and it is not widely used or available outside of Japan.

See also

• List of androgen esters
• Selective estrogen receptor modulator
• Antiestrogen

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