clascoterone topical (Rx)

>10%

Adverse effects listed below for the drug were similar to those for the vehicle cream in clinical trials

Erythema/redness (12.2%)

Scaling/dryness (10.5%)

1-10%

Adverse effects listed below for the drug were similar to those for the vehicle cream in clinical trials

Pruritus (7.7%)

Stinging/burning (4.2%)

Edema (3.6%)

Striae rubrae (2.5%)

Skin atrophy (1.6%)

Telangiectasia (1.2%)

Frequency Not Defined

Metabolism: Hyperkalemia

Reproductive: Polycystic ovaries, amenorrhea

Contraindications

None

Cautions

May induce local irritation (eg, erythema, redness, pruritus, scaling, dryness); limit concomitant use with other potentially irritating topical products that have a strong drying effect or have high concentrations of alcohol, astringents, spices, or lime

HPA axis suppression

• Hypothalamic-pituitary-adrenal (HPA) axis suppression observed in clinical trials; may occur during or after treatment
• Conditions that increase systemic absorption include use over large surface areas, prolonged use, and occlusive dressings
• If HPA axis suppression develops, attempt to withdraw the drug
• Pediatric patients may be more susceptible to systemic toxicity

Pregnancy

No data are available on use in pregnant females to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

Animal studies

• Subcutaneous administration to pregnant rats and rabbits during organogenesis at doses 8 or 39 times the maximum recommended human dose, respectively, increased malformations in rats and postimplantation loss and resorptions in rabbits

Lactation

Data are not available regarding presence of clascoterone or metabolite in human milk, effects on breastfed infants, or effects on milk production

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Exact mechanism of action is unknown; laboratory studies suggest clascoterone competes with androgens, specifically dihydrotestosterone, for binding to the androgen receptors within the sebaceous gland and hair follicles

Absorption

Measured on Day 14 of BID dosing

Peak plasma concentration: 4.5 ng/mL

Average plasma concentration: 1.9 ng/mL

AUC: 37 ng⋅hr/mL

Steady-state achieved on Day 5

Distribution

Protein bound: 84-89%

Metabolism

Plasma concentrations of cortexolone, a possible primary metabolite, were detectable and generally below or near the lower limit of quantitation (0.5 ng/mL)

Elimination

Excretion: Not characterized

Topical Administration

For topical use only; not for ophthalmic, oral, or vaginal use

Gently cleanse affected area; after skin is dry, apply thin uniform layer of cream to affected area(s) twice per day (morning and evening)

Do not apply to cuts, abrasions, or eczematous or sunburned skin

Avoid concomitant use of other potentially irritating topical products

Avoid accidental transfer of cream into eyes, mouth, or other mucous membranes; if this occurs, rinse thoroughly with water

Storage

Before dispensing: Refrigerate at 36-46ºF (2-8ºC)

After dispensing to patient: Store at room temperature of 68-77ºF (20-25ºC); discard unused product 180 days after dispensing or 1 month after first opening, whichever is sooner

Do not freeze