From WikiMD's Food, Medicine & Wellness Encyclopedia

2-Hydroxyflutamide is a pharmaceutical compound that acts as a potent antiandrogen, primarily used in the treatment of prostate cancer. It is an active metabolite of flutamide, a synthetic, nonsteroidal antiandrogen that was first introduced in the 1980s for medical use. 2-Hydroxyflutamide works by competitively inhibiting the action of androgens (male hormones) by binding to the androgen receptors in the target tissues, preventing the stimulation of these receptors by natural androgens. This mechanism of action is crucial in the treatment of prostate cancer, as the growth of most prostate cancers is stimulated by androgens.

Pharmacology[edit | edit source]

The pharmacological significance of 2-Hydroxyflutamide lies in its ability to inhibit the action of androgens. Androgens, such as testosterone and dihydrotestosterone (DHT), play a pivotal role in the development and maintenance of male characteristics. However, they also contribute to the growth of prostate cancer cells. By blocking these hormones from binding to their receptors, 2-Hydroxyflutamide can slow down or even shrink the growth of prostate cancer.

Clinical Use[edit | edit source]

2-Hydroxyflutamide is primarily used in the management of advanced prostate cancer, often in combination with other therapies such as gonadotropin-releasing hormone (GnRH) analogs or surgical castration to achieve maximum androgen blockade. This combination therapy is known as combined androgen blockade (CAB) or total androgen blockade (TAB). The goal of CAB is to block androgens from stimulating prostate cancer cells by both reducing the production of androgens and blocking their action at the receptor level.

Side Effects[edit | edit source]

Like all medications, 2-Hydroxyflutamide can cause side effects. The most common side effects associated with its use include gastrointestinal disturbances, liver toxicity, and gynecomastia (enlargement of male breast tissue). Liver function tests are recommended regularly for patients taking 2-Hydroxyflutamide due to the risk of hepatotoxicity.

Chemistry[edit | edit source]

Chemically, 2-Hydroxyflutamide is classified as a nonsteroidal antiandrogen. Its structure is similar to that of other nonsteroidal antiandrogens, with a hydroxyl group at the 2-position, which is essential for its antiandrogenic activity.

Conclusion[edit | edit source]

2-Hydroxyflutamide plays a significant role in the treatment of prostate cancer by inhibiting the action of androgens. Its use, particularly in combination with other therapies, has been a cornerstone in the management of advanced prostate cancer. Despite its effectiveness, the potential for side effects, especially liver toxicity, necessitates careful monitoring of patients undergoing treatment with this medication.


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Contributors: Prab R. Tumpati, MD