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雄激素与痤疮:首个局部应用的雄激素受体拮抗剂——氯螺内酯的相关研究

Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist.

机构信息

Dermatology, Icahn School of Medicine at Mount Sinai, New York, NY, USA.

出版信息

Expert Opin Pharmacother. 2021 Sep;22(13):1801-1806. doi: 10.1080/14656566.2021.1918100. Epub 2021 Apr 27.

DOI:10.1080/14656566.2021.1918100
PMID:33906537
Abstract

: Increased circulating androgens are key to the multifactorial pathogenesis of acne. Clascoterone is the first topical androgen antagonist developed to treat acne in both male and female patients and the first such agent to receive U.S. Food and Drug Administration (FDA) approval for treatment of acne. Androgens directly stimulate sebaceous gland growth and increased sebum production, creating a nourishing medium in which anaerobic ( bacteria flourish. Androgens may directly contribute to inflammation in the sebaceous gland.: In this review, the author assesses clascoterone's potential role in the management of acne. With a 4-ring backbone identical to dihydrotestosterone (DHT) and spironolactone, topically applied clascoterone binds androgen receptors (ARs) in the sebaceous glands and hair follicles, interfering with the pathogenesis of acne and reducing acne lesions with no reported systemic effects.: Phase III study results confirmed the safety and efficacy of topical clascoterone for acne, with considerable reductions in absolute non-inflammatory and inflammatory lesion counts at week 12. The approval of a first-in-class topical androgen antagonist is indeed a 'game-changer' for acne management. This topical agent is expected to be quickly adopted in clinical practice, likely within combination regiments, yet to be formally evaluated.

摘要

: 循环雄激素水平升高是痤疮多因素发病机制的关键。克拉屈滨是第一种开发用于治疗男性和女性痤疮的局部雄激素拮抗剂,也是第一种获得美国食品和药物管理局 (FDA) 批准用于治疗痤疮的此类药物。雄激素直接刺激皮脂腺生长和皮脂分泌增加,创造了一种有利于厌氧细菌生长的滋养介质。雄激素可能直接导致皮脂腺炎症。在这篇综述中,作者评估了克拉屈滨在痤疮治疗中的潜在作用。与二氢睾酮 (DHT) 和螺内酯具有相同的 4 元环骨架,局部应用的克拉屈滨与皮脂腺和毛囊中的雄激素受体 (AR) 结合,干扰痤疮的发病机制,并减少痤疮病变,无报道的全身作用。III 期研究结果证实了局部克拉屈滨治疗痤疮的安全性和有效性,在第 12 周时绝对非炎症性和炎症性病变计数显著减少。第一种局部雄激素拮抗剂的批准确实是痤疮管理的“游戏规则改变者”。这种局部药物有望在临床实践中迅速被采用,可能在尚未正式评估的联合治疗方案中使用。

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Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist.雄激素与痤疮:首个局部应用的雄激素受体拮抗剂——氯螺内酯的相关研究
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