Springer Nature, Mairangi Bay, Private Bag 65901, Auckland, 0754, New Zealand.
Drugs. 2020 Nov;80(16):1745-1750. doi: 10.1007/s40265-020-01417-6.
Clascoterone (Winlevi) is an androgen receptor inhibitor being developed as a topical cream and solution by Cassiopea (a spin-out company of Cosmo Pharmaceuticals) for the treatment of androgen-dependent skin disorders, including androgenetic alopecia and acne vulgaris. Although the exact mechanism of action of clascoterone for the topical treatment of acne vulgaris is unknown, the drug is believed to compete with the androgen dihydrotestosterone for binding to androgen receptors in the sebaceous gland and hair follicles to attenuate signalling necessary for acne pathogenesis. In August 2020, clascoterone cream 1% received its first approval in the USA for the topical treatment of acne vulgaris in patients 12 years of age or older. Clinical studies of a different formulation of clascoterone (a solution containing a higher concentration of the drug) for the treatment of androgenetic alopecia are underway in Germany and the USA. This article summarizes the milestones in the development of clascoterone leading to this first approval for the topical treatment of acne vulgaris.
卡索培阿（Cassiopea）是 Cosmo 制药的一个衍生公司，正在开发雄激素受体抑制剂氯螺内酯（Clascoterone，Winlevi）作为一种乳膏和溶液，用于治疗雄激素依赖性皮肤疾病，包括雄激素性脱发和寻常痤疮。虽然氯螺内酯治疗寻常痤疮的确切作用机制尚不清楚，但该药被认为与雄激素二氢睾酮竞争，与皮脂腺和毛囊中的雄激素受体结合，从而减弱痤疮发病机制所需的信号传导。2020 年 8 月，氯螺内酯乳膏 1%在美国首次获批用于治疗 12 岁及以上患者的寻常痤疮。德国和美国正在进行不同配方的氯螺内酯（一种含有更高浓度药物的溶液）治疗雄激素性脱发的临床研究。本文总结了导致氯螺内酯首次获批用于寻常痤疮局部治疗的开发里程碑。
