Inocoterone acetate

Overview of the antiandrogen drug Inocoterone acetate

Inocoterone acetate
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Inocoterone acetate is a nonsteroidal antiandrogen (NSAA) that was developed for the treatment of androgen-dependent conditions such as acne, androgenic alopecia, and hirsutism. It is a topical medication that acts by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) in the skin.

Mechanism of Action

Inocoterone acetate works by competitively inhibiting the binding of androgens to the androgen receptors in the skin. This prevents the activation of androgen receptors by testosterone and DHT, thereby reducing the effects of these hormones on target tissues. As a result, the growth of sebaceous glands and hair follicles is reduced, which helps in managing conditions like acne and hirsutism.

Pharmacokinetics

Inocoterone acetate is applied topically, and its absorption through the skin is minimal. This localized application helps in reducing systemic side effects that are commonly associated with oral antiandrogens. The drug is metabolized in the skin to its active form, inocoterone, which then exerts its antiandrogenic effects.

Clinical Use

Inocoterone acetate has been primarily investigated for use in treating acne and hirsutism. Its efficacy in reducing acne lesions and hair growth has been demonstrated in clinical trials, although it is not as widely used as other treatments like spironolactone or finasteride.

Side Effects

The side effects of inocoterone acetate are generally mild due to its topical application. Some patients may experience local skin irritation, redness, or dryness at the site of application. Unlike systemic antiandrogens, it does not cause significant hormonal changes in the body.

Development and Availability

Inocoterone acetate was developed in the 1990s, but it has not been widely marketed or approved for use in many countries. Its development was primarily focused on providing a topical alternative to systemic antiandrogens for dermatological conditions.

Related pages

• Antiandrogen
• Androgen receptor
• Acne
• Hirsutism
• Androgenic alopecia

Inocoterone_acetate

• 
  Inocoterone acetate chemical structure