17알파프로피오네이트

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• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H341：유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재)

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  P281：요구되는 개인 보호구를 착용하시오

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17알파프로피오네이트 화학적 특성, 용도, 생산

• 개요

  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.

• 화학적 성질

  Clascoterone is a white to almost white powder, practically insoluble in water. The compound has the empirical formula C24H34O5 andmolecular weight of 402.5 g/mol.

• 용도

  Clascoterone (cortexolone 17α-propionate, CB-03-01) is a novel antagonist of androgen receptors. It binds to androgen receptors with high affinity. By competing with androgens for binding to androgen receptors, clascoterone works by blocking the androgen receptor signalling cascades that promote acne pathogenesis, such as sebaceous gland proliferation, excess sebum production, and inflammatory pathways. In August 2020, FDA approved clascoterone for the first-in-class topical treatment of acne (acne vulgaris) in male and female patients 12 years and older. Clascoterone is also being investigated as a novel treatment for androgenetic alopecia.

• 생물학적 활성

  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).

• 부작용

  Clascoterone topical application may cause serious side effects: severe itching, burning, peeling, or redness of treated skin; high blood potassium--nausea, weakness, tingly feeling, chest pain, irregular heartbeats, loss of movement; or decreased adrenal gland hormones--nausea, vomiting, stomach pain, loss of appetite, feeling tired or light-headed, muscle or joint pain, skin discoloration, craving salty foods.

• Safety

  Clascoterone(Winlevi) is the only topical acne product with a warning about hypothalamic-pituitary-adrenal (HPA) axis suppression. This may result when Winlevi is used over large surface areas or if use is prolonged. In addition, pediatric patients may be more susceptible. This adverse event was not observed in the pivotal studies or in the long-term open-label extension study. However, it was observed in a small group of patients on Day 14 in a pharmacokinetic study. Normal HPA axis function was observed at follow-up at 4 weeks after end of treatment.

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