Clascoterone
Cortexolone 17α-propionate (CB-03-01): the first FDA-approved TOPICAL androgen-receptor antagonist. Approved for acne (Winlevi 1% cream, 2020); in investigational phase for androgenetic alopecia (Breezula solution). Acts locally and is rapidly inactivated systemically.
Related comparisons
Clascoterone vs Pyrilutamide vs RU58841WHAT IS CLASCOTERONE?
Detailed overview
Clascoterone (cortexolone 17α-propionate, development code CB-03-01) is the first and so far only FDA-approved TOPICAL androgen-receptor antagonist. In the skin it competitively inhibits the binding of dihydrotestosterone (DHT) to the androgen receptor: in sebaceous gland cells (sebocytes) it reduces sebum production and inflammatory cytokines (acne), and in the dermal papilla cells of the hair follicle it reduces androgen-driven miniaturization (hair loss). After absorption it is rapidly hydrolyzed to the inactive cortexolone, so the systemic antiandrogen effect is minimal. For acne it received FDA approval in 2020 (Winlevi 1% cream) based on the two phase 3 trials (PMID 32320027, JAMA Dermatology, 1440 patients). For androgenetic alopecia the in vitro and phase 2 data are favorable (clascoterone is an AR antagonist in dermal papilla cells, PMID 30811143; AGA review PMID 32421862), and a phase 3 trial (SCALP2) is currently ongoing for male pattern hair loss (Breezula solution) – this indication is STILL INVESTIGATIONAL.
Development code / name
CB-03-01 · cortexolone 17α-propionate
Status
Acne: FDA-approved (Winlevi) · Hair (AGA): phase 3 investigational
Mechanism of action
Topical androgen-receptor antagonist (local anti-DHT)
Strengths
1% cream (acne) · 5-7.5% solution (investigational AGA)
Onset
4-12 weeks (acne); hair: months, during phase 3
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 4
- Local skin reactions: mild erythema, scaling, dryness, itching at the application site; in the phase 3 acne trials local reaction rates were similar to vehicle (well tolerated).
- Signal of transient HPA-axis suppression: in a dedicated PK/safety study with large-area use a few patients showed transient, reversible adrenal-axis suppression; clinically minor but noted on the label.
- With scalp application (investigational AGA solution): local irritation, itching, flaking; long-term data are still accruing as the AGA indication is in phase 3.
- Hypersensitivity reaction (rare): contact dermatitis or more pronounced irritation; discontinue if an allergic reaction occurs.
Contraindications · 4
- Known hypersensitivity to clascoterone or any excipient.
- Broken, inflamed or infected skin: absorption and irritation may increase; withhold until it heals.
- Large body-surface, prolonged use without HPA-axis monitoring: avoid due to the (rare, transient) adrenal-suppression risk, especially in children.
- Pregnancy/breastfeeding: although systemic exposure is minimal (rapid inactivation to cortexolone), use only after benefit/risk assessment and under medical supervision due to limited data.
Related Hair & Skin
Same therapeutic category
Studies
Related research and clinical findings
Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials
Hebert A, Thiboutot D, Stein Gold L, et al.
A Phase 2b, Randomized, Double-Blind Vehicle Controlled, Dose Escalation Study Evaluating Clascoterone 0.1%, 0.5%, and 1% Topical Cream in Subjects With Facial Acne
Eichenfield L, Hebert A, Gold LS, et al.
Cortexolone 17α-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro
Rosette C, Agan FJ, Mazzetti A, et al.
Clascoterone as a novel treatment for androgenetic alopecia
Dhillon S.
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