RU-5135

RU-5135

RU-5135 is a synthetic steroidal antiandrogen that was developed in the 1970s. It is a derivative of progesterone and is known for its ability to block the effects of androgens, such as testosterone, in the body. Although it was never marketed for clinical use, RU-5135 has been studied for its potential applications in treating conditions related to androgen excess.

Chemical Structure and Properties

RU-5135 is chemically classified as a steroidal antiandrogen. Its structure is based on the steroid nucleus, which is a characteristic feature of compounds in this class. The molecular formula of RU-5135 is C23H31ClO3, and it has a molecular weight of 390.94 g/mol.

The compound is characterized by the presence of a chlorine atom, which is a key feature that contributes to its antiandrogenic activity. The presence of this halogen atom is thought to enhance the binding affinity of RU-5135 to androgen receptors, thereby inhibiting the action of endogenous androgens.

Mechanism of Action

RU-5135 functions as an antiandrogen by competitively binding to androgen receptors in target tissues. By occupying these receptors, RU-5135 prevents endogenous androgens, such as testosterone and dihydrotestosterone (DHT), from exerting their biological effects. This blockade of androgen action can lead to a reduction in androgen-dependent processes, such as prostate growth and sebum production.

Potential Applications

Although RU-5135 was never brought to market, its antiandrogenic properties have been of interest in several potential therapeutic areas:

• Prostate Cancer: Antiandrogens are commonly used in the treatment of prostate cancer, as the growth of prostate cancer cells is often driven by androgens. RU-5135, like other antiandrogens, could theoretically be used to inhibit the progression of androgen-dependent prostate cancer.

• Acne and Seborrhea: Androgens play a significant role in the development of acne and seborrhea by stimulating sebaceous gland activity. RU-5135 could potentially reduce sebum production and improve these conditions.

• Hirsutism: In women, excess androgen activity can lead to hirsutism, a condition characterized by excessive hair growth. Antiandrogens like RU-5135 could be used to manage this condition by reducing androgenic stimulation of hair follicles.

Research and Development

RU-5135 was developed by Roussel Uclaf, a French pharmaceutical company, during the 1970s. Despite its promising pharmacological profile, it did not progress to clinical trials or commercial development. The reasons for this are not well-documented, but it is possible that other compounds with more favorable properties were prioritized.

Also see

• Antiandrogen
• Androgen receptor antagonist
• Prostate cancer treatment
• Hirsutism
• Acne vulgaris