Clascoterone is a high-affinity androgen receptor (AR) antagonist (antiandrogen) that antagonizes testosterone-stimulated transcription activity (in reporter cells) as well as DHT-induced production of lipids and inflammatory cytokines (in human sebocytes) in cultures. When applied topically, clascoterone is as active as cyproterone acetate, and 2-, 3-, and 4-times, respectively, more active than finasteride, flutamide, and progesterone in vivo (local antiandrogenic activity in hamster′s flank organ; 100-400 μg/50 μL acetone/animal).
High-affinity androgen receptor (AR) antagonist with antiandrogenic efficacy in vitro and in vivo.
Journal of drugs in dermatology : JDD, 18(2), 197-201 (2019-02-28)
Cortexolone 17α-propionate (clascoterone) is a novel androgen antagonist that is currently being analyzed in a large phase 2 clinical trial for the topical treatment of androgenetic alopecia (AGA). While the pathogenesis of AGA is still debated, the consensus is that
Journal of drugs in dermatology : JDD, 18(5), 412-418 (2019-05-31)
Cortexolone 17α-propionate (clascoterone) is a novel topical androgen antagonist that is being analyzed for its ability to treat acne. The pathogenesis of acne is attributed to multiple factors, including altered sebum production, inflammatory processes, dysregulation of the hormone microenvironment, and
Cortexolone 17α-propionate for hidradenitis suppurativa.
Cortexolone-17α-propionate (CP) is a topically active antiandrogen useful in the treatment of skin disorders. In the solid state, three anhydrous forms of this drug (CPI, CPII and CPIII) occur, together with one hydrated crystal (CPW). The single crystal structure of
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