Clascoterone

Clascoterone (CB-03-01) is a novel, peripherally selective androgen antagonist approved by the FDA in 2020 for the topical treatment of acne vulgaris in patients aged 12 years and older. As the first new class of acne therapy in decades, Clascoterone offers a mechanism distinct from retinoids, antibiotics, and benzoyl peroxide by competitively inhibiting androgen receptor binding in the skin, thereby suppressing hormonal signals that drive excess sebum production and inflammation. Clascoterone is formulated as a 1% cream (Winlevi®) and has demonstrated statistically significant superiority over placebo in reducing both inflammatory and non-inflammatory lesion counts, with a favorable tolerability profile. Beyond acne, Clascoterone is under clinical development as Breezula® at higher concentrations for the treatment of androgen-dependent scalp hair loss (androgenetic alopecia), showcasing the therapeutic versatility of this topical antiandrogen. Clascoterone also shows potential for managing dermatitis and eczema due to its anti-inflammatory and skin barrier–enhancing properties.

Product Parameters

Application

21-Hydroxy-17-(1-oxopropoxy)pregn-4-en-3,20-dione is used as an organic synthesis intermediate and pharmaceutical intermediate.

Bioactivity

Clascoterone (Winlevi, Cortexolone 17α-propionate, CB-03-01) is a topical and peripheral-selective androgen receptor (AR) antagonist.

Synthetic Route

Using 17α,21-dipropionate 102 as the starting material and lipase derived from Candida terrevisiae, a lipase-catalyzed selective transesterification reaction was carried out in toluene as the solvent. Reaction conditions: n-butanol was employed as the acyl acceptor; under these conditions, 17α,21-dipropionate 102 was converted to crizotinib (XV), with a yield of 99%.

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