Clascoterone

What is clascoterone?

Clascoterone 1% cream (Winlevi®) is a first-in-class topical androgen receptor inhibitor indicated for the treatment of acne vulgaris in patients aged 12 years and older.

Clascoterone first received approval from the US Food and Drug Administration (FDA) in 2020, followed by approvals in other regions such as Canada (2023), Australia (2024), New Zealand (2024), and the United Kingdom (2025).

What is clascoterone used for?

Acne vulgaris

The efficacy and safety of clascoterone 1% cream in acne vulgaris have been demonstrated in multiple clinical trials, leading to its inclusion in several acne treatment guidelines.

• Two phase III trials demonstrated that patients using clascoterone 1% achieved statistically significantly higher treatment success rates (defined as a ≥2 point reduction in Investigator Global Assessment severity scores) compared to those using a placebo vehicle cream after 12 weeks of treatment. They also found:
  • A significant reduction in all lesion counts compared to placebo.
  • Safety was comparable to the vehicle cream.
• An open-label, long-term extension study demonstrated that clascoterone maintained its safety and efficacy for up to 12 months in patients aged 12 years and older with facial and/or truncal acne vulgaris.

A 2024 systematic review and meta-analysis comparing recent topical treatments found no significant differences in efficacy between clascoterone, trifarotene, and tazarotene after 12 weeks of use for moderate-to-severe acne.

Comedonal and papulopustular acne suitable for clascoterone therapy 

Androgenetic alopecia

Clascoterone is under investigation in phase III clinical trials for the treatment of androgenetic alopecia (AGA) under the brand name Breezula®.

In phase II clinical trials of AGA, the clascoterone group showed significant clinical improvement compared to the vehicle group. These benefits are attributed to clascoterone’s antagonism of androgen receptors in scalp dermal papilla cells. Clascoterone is thought to reduce the production of prostaglandin D2 and interleukin 6 (IL-6), thereby regulating sebum secretion and mitigating hair miniaturisation.

Hair shaft diameter variability in androgenetic alopecia (MPHL-patient1)

What are the contraindications for clascoterone?

Clascoterone is contraindicated in anyone with a known hypersensitivity to the drug or its excipients.

The safety and efficacy of clascoterone have not been established in:

• Paediatric patients less than 12 years of age
• Patients aged 65 years and older
• Pregnancy or breastfeeding.

How does clascoterone work?

Though the exact mechanism is unclear, clascoterone exerts its effects through competitive antagonism of androgen receptors. Blocking the action of androgens (such as dihydrotestosterone) on sebocytes leads to a reduction in sebum production and inflammation, both of which are involved in acne pathogenesis.

What is the dosage and administration?

Clascoterone is available as a 1% (10 mg/g) cream. It should be applied as a thin, uniform layer to the area affected by acne (rather than just individual spots) twice daily, in the morning and evening.

What are the benefits of clascoterone?

• Minimal systemic exposure
  • Clascoterone is quickly metabolised in the skin to an inactive metabolite (cortexolone), limiting its presence in the bloodstream
• Reduced feminising side effects
  • Unlike oral anti-androgen acne treatments.
• Does not require routine laboratory monitoring
• Lower discontinuation rates
  • Compared to some topical retinoids eg, trifarotene, tazarotene, or tretinoin.

What are the disadvantages of clascoterone?

• Generally more expensive compared to other acne treatments.
• Should be stored in the fridge until opened for use.

What are the adverse effects of clascoterone?

The majority of reported adverse effects are mild and infrequent.

Local effects may include:

• Erythema
• Pruritus
• Scaling/dryness
• Oedema
• Skin atrophy
• Irritation (stinging or burning)
• Striae rubrae
• Telangiectasia.

Other reported adverse effects include:

• Nasopharyngitis
• Headache
• Oropharyngeal pain.

Hypothalamic-pituitary-adrenal (HPA) axis suppression:

• Mild, asymptomatic, reversible HPA suppression was observed in some subjects after 14 days of maximum-use exposure
• All cases resolved within 4 weeks after discontinuation
• Risk is increased in children and adolescents, application over a large body surface area, use of occlusive dressings, and prolonged use
• If HPA axis suppression is suspected, treatment should be stopped or the dose reduced.

Hyperkalaemia (clinical trial finding of unknown significance):

• Observed in both clascoterone and vehicle-treated patients
• Causality for this clinical trial finding was not be established
• Potassium monitoring is not required.

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).