Introduction Uses How it works Dosage and administration Benefits Disadvantages Contraindications
Topical clascoterone cream 1% (Winlevi®) is a novel androgen receptor inhibitor used for the treatment of acne vulgaris in patients aged 12 years and older.
Clascoterone was approved by the US Food and Drug Administration (FDA) in August 2020 for the treatment of acne vulgaris, but is not yet available in some countries including Australia and New Zealand at the time of writing.
There have been several trials to date demonstrating the efficacy and safety of clascoterone cream 1% for moderate-to-severe acne vulgaris.
Clascoterone has also been suggested to be an effective treatment for androgenetic alopecia from preliminary studies, although it is not currently approved for use in this context.
The proposed mechanism of action is through antagonizing dihydrotesterone’s effects on dermal papilla cells, reducing the production of prostaglandin D2 and interleukin 6 (IL-6), regulating secretion of sebum, and reducing hair miniaturisation.
Clascoterone or cortexolone 17α-propionate is the first of its kind — a topical treatment targeting the hormonal pathogenesis of acne vulgaris.
It is postulated that clascoterone competes with androgens such as dihydrotestosterone (DHT) for androgen receptors, inhibiting the downstream signalling pathways of androgen receptor-regulated gene transcription in sebaceous glands and dermal papilla cells responsible for acne pathogenesis.
Clascoterone is currently available as a 1% (10mg/g) cream. A thin, uniform layer to the affected area twice a day: morning and evening is recommended.
Targeting androgen inhibition is a known effective treatment for acne vulgaris, as is seen in current utilisation of the anti-androgenic effects of spironolactone and some oral contraceptives. These, however, can cause systemic adverse effects and are also contraindicated in males.
Clascoterone 1% cream has selective topical activity, limiting systemic androgenic effects. Clascoterone is also highly potent, and found to be four times more potent than progesterone.
The reported adverse effects of clascoterone cream 1% are mild and infrequent. Clascoterone has a similar safety profile to vehicle cream from existing studies.
Local skin reactions may include:
Reported treatment-emergent adverse events (<2%) included:
There are currently no known contraindications from the existing studies.
There is, however, a lack of safety evidence available for the use of clascoterone in patients less than 12 years of age, in pregnancy, during lactation (breastfeeding), and in those over 65 years of age.
Approved datasheets are the official source of information for medicines, including approved uses, doses, and safety information. Check the individual datasheet in your country for information about medicines.
We suggest you refer to your national drug approval agency such as the Australian Therapeutic Goods Administration (TGA), US Food and Drug Administration (FDA), UK Medicines and Healthcare products regulatory agency (MHRA) / emc, and NZ Medsafe, or a national or state-approved formulary eg, the New Zealand Formulary (NZF) and New Zealand Formulary for Children (NZFC) and the British National Formulary (BNF) and British National Formulary for Children (BNFC).
