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Cortexolone 17α-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro

Abstract
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 AGA is an androgen-dependent hair disorder with strong genetic links, and that the testosterone metabolite, dihydrotestosterone (DHT), plays a causal role in its development. DHT binds to the androgen receptor (AR) in scalp dermal papilla cells (DPC) to induce AR-mediated transcription of genes that contribute to AGA in genetically predisposed individuals. Several studies have established that clascoterone is a potent antiandrogen that is well tolerated and has selective topical activity. The study described herein elucidates a potential mechanism of clascoterone in AGA. Clascoterone was found to inhibit AR-regulated transcription in a reporter cell line with similar efficacy to the 5α-reductase inhibitor, finasteride. More importantly, when compared with another direct AR antagonist, enzalutamide, clascoterone was significantly better at inhibiting IL-6 synthesis from DHT-stimulated primary cultures of human scalp DPC. Therefore, clascoterone may be an excellent candidate to be the first topical antiandrogen for treating AGA. J Drugs Dermatol. 2019;18(2):197-201.
AuthorsCaridad Rosette, Niccolette Rosette, Alessandro Mazzetti, Luigi Moro, Mara Gerloni
JournalJournal of drugs in dermatology : JDD (J Drugs Dermatol) Vol. 18 Issue 2 Pg. 197-201 (Feb 01 2019) ISSN: 1545-9616 [Print] United States
PMID30811143 (Publication Type: Journal Article)
Chemical References
  • Androgen Receptor Antagonists
  • Propionates
  • Receptors, Androgen
  • Cortodoxone
  • Clascoterone
Topics
  • Administration, Topical
  • Alopecia (drug therapy, metabolism)
  • Androgen Receptor Antagonists (pharmacology)
  • Cell Line
  • Cells, Cultured
  • Cortodoxone (analogs & derivatives, pharmacology)
  • Hair Follicle (drug effects, metabolism)
  • Humans
  • Propionates (pharmacology)
  • Receptors, Androgen (metabolism)

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