Clascoterone
Brand name: Winlevi
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical name: [(8R,9S,10R,13S,14S,17R)-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] propanoate
Molecular formula: C24H34O5
CAS number: 19608-29-8
Introduction
Clascoterone, an androgen receptor inhibitor, is a skin or mucous membrane agent.
Uses for Clascoterone
Clascoterone has the following uses:
Clascoterone cream is indicated for the topical treatment of acne vulgaris in patients 12 years of age and older.
Clascoterone Dosage and Administration
General
Clascoterone is available in the following dosage form(s) and strength(s):
Cream, 1%.
Dosage
It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:
Pediatric Patients
Dosage and Administration
-
Adolescents ≥12 years of age: Apply a thin layer (approximately 1 gram) to affected area twice daily (morning and evening). Avoid contact with eyes, mouth, and mucous membranes.
-
For topical use only. Not for ophthalmic, oral or vaginal use.
Adults
Dosage and Administration
-
Apply a thin layer (approximately 1 gram) to affected area twice daily (morning and evening). Avoid contact with eyes, mouth, and mucous membranes.
-
For topical use only. Not for ophthalmic, oral or vaginal use.
Cautions for Clascoterone
Contraindications
None.
Warnings/Precautions
Local Skin Reactions
Clascoterone cream may induce local irritation (erythema/redness, pruritus, scaling/ dryness). Concomitant use with other potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect and products with high concentrations of alcohol, astringents, spices or lime) should be limited.
The product should not be applied to cuts, abrasions, eczematous or sunburned skin.
Hypothalamic-Pituitary-Adrenal (HPA) Axis Suppression
Hypothalamic-pituitary-adrenal (HPA) axis suppression was observed and may occur during or after treatment with clascoterone. In the PK trial, all subjects returned to normal HPA axis function at follow-up 4 weeks after stopping treatment. Conditions which augment systemic absorption include use over large surface areas, prolonged use, and the use of occlusive dressings.
If HPA axis suppression develops, an attempt should be made to withdraw the drug.
Pediatric patients may be more susceptible to systemic toxicity.
Specific Populations
Pregnancy
Risk Summary: There are no available data on clascoterone cream use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, subcutaneous administration of clascoterone to pregnant rats and rabbits during organogenesis at doses 8 or 39 times the maximum recommended human dose (MRHD), respectively, increased malformations in rats and post-implantation loss and resorptions in rabbits.
The background risk of major birth defects and miscarriage for the indicated population is unknown. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Animal Data: In an embryofetal development study, clascoterone was administered subcutaneously to pregnant rats at doses of 1, 5, or 25 mg/kg per day during the period of organogenesis. No clascoterone-related maternal toxicity or effects on uterine parameters were noted at doses up to 25 mg/kg perday (336 times the MRHD based on AUC comparison). Clascoterone-related malformations were noted at all dose levels, without a dose relationship. Omphalocele was noted in a single fetus at each dose level. External and visceral malformations (severe dilation of the lateral and third cerebral ventricles; thin skin, small size, and protruding tongue) were noted in two additional fetuses at 1 mg/kg per day (8 times the MRHD based on AUC comparison).
In an embryofetal development study, clascoterone was administered subcutaneously to pregnant rabbits at doses of 0.1, 0.4, or 1.5 mg/kg per day during the period of organogenesis. Post-implantation loss and resorptions were increased at 1.5 mg/kg per day (39 times the MRHD based on AUC comparison). No developmental toxicity was noted at doses up to 0.4 mg/kg per day (12 times the MRHD based on AUC comparison). No clascoterone-related maternal toxicity or fetal malformations were noted at doses up to 1.5 mg/kg per day (39 times the MRHD based on AUC comparison).
In a prenatal and postnatal development study, clascoterone was administered subcutaneously to pregnant rats at doses of 0.5, 2.5, and 12.5 mg/kg per day beginning on gestation day 6 and continuing through lactation day 20. No significant maternal or developmental toxicity was observed at doses up to 12.5 mg/kg per day (163 times the MRHD based on AUC comparison).
Lactation
Risk Summary: There are no data regarding the presence of clascoterone or metabolite in human milk, the effects on the breastfed infant or the effects on milk production. The lack of clinical data during lactation precludes a clear determination of the risk of clascoterone to an infant during lactation; therefore, the developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for clascoterone and any potential adverse effects on the breastfed child from clascoterone or from the underlying maternal condition.
Pediatric Use
Safety and effectiveness of clascoterone cream for the topical treatment of acne vulgaris have been established in 641 pediatric patients, aged 12 to 18 years in two identical multicenter, randomized, double-blind, vehicle-controlled, 12-week trials and 2 open-label pharmacokinetic studies.
Safety and effectiveness of clascoterone cream for the topical treatment of acne vulgaris has not been established in pediatric patients under 12 years of age.
Hypothalamic-pituitary-adrenal (HPA) axis suppression was observed in 2/22 (9%) adolescent subjects. All subjects returned to normal HPA axis function at follow-up 4 weeks after stopping the treatment. Children may be more susceptible to systemic toxicity when treated with clascoterone.
Geriatric Use
Clinical studies of clascoterone cream did not include sufficient numbers of subjects aged 65 years of age and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Common Adverse Effects
Most common adverse reactions occurring in 7 to 12% of patients are erythema/reddening, pruritus and scaling/dryness. Additionally, edema, stinging, and burning occurred in >3% of patients and were reported in a similar percentage of subjects treated with vehicle.
Drug Interactions
Specific Drugs
It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:
Please see product labeling for drug interaction information.
Actions
Mechanism of Action
Clascoterone is an androgen receptor inhibitor. The mechanism of action of clascoterone cream for the topical treatment of acne vulgaris is unknown.
Advice to Patients
-
Advise the patient to read the FDA-approved patient labeling (Patient Information).
-
Avoid applying clascoterone cream to damaged skin (such as cuts, abrasions), eczematous areas, and sunburned skin.
-
Avoid concomitant use of other potentially irritating topical products (medicated or not).
Additional Information
AHFSfirstRelease™. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Topical |
Cream |
1% |
Winlevi |
Sun Pharmaceutical Industries Inc. |
AHFS Drug Information. © Copyright 2023, Selected Revisions October 18, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
Reload page with references included
More about clascoterone topical
- Check interactions
- Side effects
- Dosage information
- During pregnancy
- Drug class: topical acne agents
- En español