Clascoterone


Clascoterone, developmental code name CB-03-01 and tentative brand names Winlevi for acne and Breezula for hair loss, is an antiandrogen medication which is under development for the treatment of acne and scalp hair loss in both males and females. It is given as a cream by application to the skin, for instance the face and scalp.
Clascosterone is an antiandrogen, or antagonist of the androgen receptor, the biological target of androgens such as testosterone and dihydrotestosterone. It shows no systemic absorption when applied to skin.
The medication is under development by Cassiopea and Intrepid Therapeutics. As of 2019, it has completed phase III clinical trials for acne, with a New Drug Application expected for the first half of 2019, and is expected to start phase III clinical trials for androgen-dependent scalp hair loss.

Medical uses

A pilot clinical trial in 2011 of men treated with topical clascoterone 1% cream for acne found that the medication significantly reduced symptoms of acne and was well tolerated. Moreover, its effectiveness was significantly greater than that of the active comparator, tretinoin 0.05% cream.

Pharmacology

Pharmacodynamics

Clascoterone is an steroidal antiandrogen, or antagonist of the androgen receptor, the biological target of androgens such as testosterone and dihydrotestosterone. In a bioassay, the topical potency of the medication was greater than that of progesterone, flutamide, and finasteride and was equivalent to that of cyproterone acetate. Likewise, it is significantly more efficacious as an antiandrogen than other AR antagonists such as enzalutamide and spironolactone in scalp dermal papilla cells and sebocytes in vitro.

Pharmacokinetics

In rodents, clascoterone has been found to possess strong local antiandrogenic activity, but negligible systemic antiandrogenic activity when administered via subcutaneous injection. Along these lines, the medication is not progonadotropic in animals.

Chemistry

Clascosterone, also known as cortexolone 17α-propionate or 11-deoxycortisol 17α-propionate, as well as 17α,21-dihydroxyprogesterone 17α-propionate or 17α,21-dihydroxypregn-4-en-3,20-dione 17α-propionate, is a synthetic pregnane steroid and a derivative of progesterone and 11-deoxycortisol. It is specifically the C17α propionate ester of 11-deoxycortisol.
An analogue of clascoterone is 9,11-dehydrocortexolone 17α-butyrate.

History

C17α esters of 11-deoxycortisol were unexpectedly found to possess antiandrogenic activity. Clascoterone, also known as cortexolone 17α-propionate, was selected for development based on its optimal drug profile.

Society and culture

Generic names

Clascoterone is the generic name of the drug and its and.