生物活性

• 描述Androgens are C-19 steroids that provide major regulatory influences on male reproductive function^[2]. Cortexolone 17 alpha-propionate is a topical and peripherally selective androgen antagonist, which is used in treatment of acne and androgenic alopecia^[3]. Clascoterone 1% cream was very well tolerated, and was significantly better than placebo regarding TLC, ILC and ASI, and also clinically more effective than comparator. The product also induced a faster attainment of 50% improvement in all the above parameters^[4]. In vitro studies showed that clascoterone binds to androgen receptors with high affinity and inhibits DHT-stimulated signaling. Clascoterone dose-dependently inhibited DHT-induced lipid synthesis and infammatory cytokine production in human primary sebocytes^[5]. In hair follicle dermal papilla cells, clascoterone selectively inhibited androgen receptor-regulated pathways that impede hair follicle growth, without affecting the production and secretion of pro-follicle growth factors^[6]. Clascoterone cream did not afect the pharmacokinetics of drugs metabolized by CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 or 3A4 to a clinically meaningful extent^[7]
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01631474	Acne Vulgaris	Phase 2	Completed	-	United States, California ... more >> Dermatology Research Associates Los Angeles, California, United States, 90045 Therapeutics Clinical Research San Diego, California, United States, 92123 University Clinical Trials San Diego, California, United States, 92123 United States, Florida International Clinical Research - US, LLC Sanford, Florida, United States United States, Georgia Gwinnett Clinical Research Center, Inc. Snellville, Georgia, United States, 30078 United States, Illinois Altman Dermatology Associates Arlington Heights, Illinois, United States, 60005 United States, Indiana Indiana Clinical Trials Center Plainfield, Indiana, United States, 46168 United States, New York Marina I. Peredo, M.D., PC Smithtown, New York, United States United States, Pennsylvania Penn State Milton S. Hershey Medical Center - Dept. of Dermatology Hershey, Pennsylvania, United States, 17033 United States, Rhode Island Clinical Partners, LLC Johnston, Rhode Island, United States United States, Texas J & S Studies College Station, Texas, United States, 77845 UT Houston Health Science Center Houston, Texas, United States, 77030 United States, Virginia Virginia Clinical Research Norfolk, Virginia, United States, 23507 Collapse <<
  NCT02279823	Androgenetic Alopecia	Phase 2	Completed	-	United States, California ... more >> Therapeutics Clinical Research San Diego, California, United States, 92123 United States, Minnesota Minnesota Clinical Study Center Fridley, Minnesota, United States, 55432 United States, Texas DermResearch, Inc. Austin, Texas, United States, 78759 Collapse <<
  NCT01831960	Acne Vulgaris	Phase 2	Completed	-	United States, Idaho ... more >> Northwest Clinical Trials, Inc. Boise, Idaho, United States United States, Indiana Shideler Clinical Research Center Carmel, Indiana, United States United States, Michigan Michigan Center for Research Corp. Clinton Township, Michigan, United States Collapse <<

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• 参考文献

• [1] Celasco G, Moro L, et al. Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist. Arzneimittelforschung. 2004;54(12):881-6.

  [2] A K Roy,et al. Androgen action. Crit Rev Eukaryot Gene Expr. 1995. 5(2), 157-76.

  [3] Trifu V, et al. 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. 2011. 165(1), 177-83.

  [4] Celasco G, et al. Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist. Arzneimittelforschung. 2004. 54(12), 881-6.

  [5] Rosette C, Agan FJ, Mazzetti A, et al. Cortexolone 17alpha-propionate (clascoterone) is a novel androgen receptor antagonist that inhibits production of lipids and infammatory cytokines from sebocytes in vitro. J Drugs Dermatol. 2019. 18(5), 412–8.

  [6] Rosette C, et al. Cortexolone 17alpha-propionate (clascoterone) is an androgen receptor antagonist in dermal papilla cells in vitro. J Drugs Dermatol. 2019. 18(2), 197–201.

  [7] Cassiopea. Winlevi (clascoterone) cream: US prescribing information. 2020.

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