Clascoterone

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Clascoterone
Cortexolone 17α-propionate.svg
Clinical data
SynonymsCB-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
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.210.810 Edit this at Wikidata
Chemical and physical data
FormulaC24H34O5
Molar mass402.531 g/mol g·mol−1
3D model (JSmol)

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 2019, the drug has finished phase III clinical trials for acne vulgaris with a NDA expected for the first half of 2019 and is expected to start phase III clinical trials for androgenic alopecia.[3]

See also[edit]

References[edit]

  1. ^ "Cassiopea Announces Very Positive Top-Line Phase 3 Results for Winlevi® (Clascoterone) cream in Treating Acne". www.cassiopea.com. Retrieved 2018-07-18.
  2. ^ "Cassiopea Announces Very Positive Interim Analysis Phase 2 Results for Breezula® (Clascoterone) in Treating Androgenetic Alopecia". www.cassiopea.com. Retrieved 2018-07-18.
  3. ^ a b http://adisinsight.springer.com/drugs/800026561
  4. ^ 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.
  5. ^ 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[edit]