Clascoterone
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| Clinical data | |
|---|---|
| Other names | CB-03-01; 11-Deoxycortisol 17α-propionate; 17α-(Propionyloxy)- deoxycorticosterone; 21-Hydroxy-3,20-dioxopregn-4-en-17-yl propionate |
| Routes of administration | Topical (cream) |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.210.810 |
| Chemical and physical data | |
| Formula | C24H34O5 |
| Molar mass | 402.531 g/mol g·mol−1 |
| 3D model (JSmol) | |
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Clascoterone[1][2], 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).[3][4][5] It is the C17α propionate ester of 11-deoxycortisol (cortexolone);[4] 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.[4]
In rats, the drug has been found to possess strong local antiandrogen activity, but negligible systemic antiandrogen activity when administered via subcutaneous injection.[4] In addition, cortexolone 17α-propionate is not progonadotropic, suggesting that it is peripherally selective.[4] 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.[4]
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.[5] Moreover, its effectiveness was significantly greater than that of the active comparator, tretinoin 0.05% cream.[5] As of 2017, the drug is in phase III clinical trials for acne vulgaris and phase II clinical trials for androgenic alopecia.[3]
See also
- List of investigational hormonal agents § Androgenics
- 9,11-Dehydrocortexolone 17α-butyrate (CB-03-04)
- List of steroidal antiandrogens
References
- ^ "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.
- ^ a b http://adisinsight.springer.com/drugs/800026561
- ^ a b c d e f 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.
- ^ a b c 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.
External links
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