7α-Thiospironolactone

7α-Thiospironolactone is a steroidal antiandrogen and the major active metabolite of spironolactone. It is also known as 7α-TS and 7α-thiospirolactone. It is specifically a competitive antagonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT).

Pharmacology

7α-Thiospironolactone is a potent antagonist of the androgen receptor (AR). It competes with androgens for binding to the AR, and prevents them from exerting their biological effects in the body. This is the mechanism by which it produces its antiandrogen effects.

Pharmacokinetics

Following oral administration, spironolactone is rapidly and extensively metabolized in the liver. The major metabolites of spironolactone are 7α-thiospironolactone, canrenone, and 6β-hydroxy-7α-thiospironolactone. These metabolites are responsible for the pharmacological activity of spironolactone.

Clinical significance

7α-Thiospironolactone is the major active metabolite of spironolactone, a medication that is widely used in the treatment of hyperaldosteronism, heart failure, liver cirrhosis, and hypertension. It is also used off-label for its antiandrogen effects in the treatment of androgen-dependent conditions like acne, seborrhea, hirsutism, and androgenic alopecia.

See also

• Spironolactone
• Canrenone
• 6β-Hydroxy-7α-thiospironolactone