CB-03-01; 11-Deoxycortisol 17α-propionate; 17α-(Propionyloxy)-|
deoxycorticosterone; 21-Hydroxy-3,20-dioxopregn-4-en-17-yl propionate
|Chemical and physical data|
|Molar mass||402.531 g/mol|
|3D model (JSmol)|
Clascoterone, or cortexolone 17α-propionate, or 11-deoxycortisol 17α-propionate, (developmental code name CB-03-01; tentative brand names Breezula (for androgenic alopecia), Winlevi (for acne)) is a synthetic steroidal antiandrogen – specifically, an androgen receptor antagonist – that is under development by Cassiopea and Intrepid Therapeutics for use as a topical medication in the treatment of androgen-dependent conditions including acne vulgaris and androgenic alopecia (male-pattern hair loss). It is the C17α propionate ester of 11-deoxycortisol (cortexolone); C17α esters of 11-deoxycortisol were unexpectedly found to possess antiandrogen activity, and cortexolone 17α-propionate was selected for development based on its optimum drug profile.
In rats, the drug has been found to possess strong local antiandrogen activity, but negligible systemic antiandrogen activity when administered via subcutaneous injection. In addition, cortexolone 17α-propionate is not progonadotropic, suggesting that it is peripherally selective. In a bioassay, the topical potency of the drug was greater than that of progesterone, flutamide, and finasteride and was equivalent to that of cyproterone acetate.
A pilot clinical trial in 2011 of men treated with topical cortexolone 17α-propionate 1% cream for acne found that the drug was very well-tolerated and significantly reduced symptoms of acne. Moreover, its effectiveness was significantly greater than that of the active comparator, tretinoin 0.05% cream. As of 2017, the drug is in phase III clinical trials for acne vulgaris and phase II clinical trials for androgenic alopecia.
- List of investigational hormonal agents § Androgenics
- 9,11-Dehydrocortexolone 17α-butyrate (CB-03-04)
- List of steroidal antiandrogens § Cortisol derivatives
- "Cassiopea Announces Very Positive Top-Line Phase 3 Results for Winlevi® (Clascoterone) cream in Treating Acne". www.cassiopea.com. Retrieved 2018-07-18.
- "Cassiopea Announces Very Positive Interim Analysis Phase 2 Results for Breezula® (Clascoterone) in Treating Androgenetic Alopecia". www.cassiopea.com. Retrieved 2018-07-18.
- Celasco G, Moro L, Bozzella R, Ferraboschi P, Bartorelli L, Quattrocchi C, Nicoletti F (2004). "Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist". Arzneimittelforschung. 54 (12): 881–6. doi:10.1055/s-0031-1297043. PMID 15646372.
- Trifu V, Tiplica GS, Naumescu E, Zalupca L, Moro L, Celasco G (2011). "Cortexolone 17α-propionate 1% cream, a new potent antiandrogen for topical treatment of acne vulgaris. A pilot randomized, double-blind comparative study vs. placebo and tretinoin 0·05% cream". Br. J. Dermatol. 165 (1): 177–83. doi:10.1111/j.1365-2133.2011.10332.x. PMID 21428978.