Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
WINLEVI vs ERLEADA
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
WINLEVI (clascoterone) is a topical androgen receptor inhibitor. It binds to the androgen receptor, preventing androgen-mediated signaling in sebocytes and inflammatory cells, thereby reducing sebum production and inflammation.
Erleada (apalutamide) is an androgen receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR, preventing AR nuclear translocation, DNA binding, and transcription of AR target genes. It also inhibits AR-mediated tumor growth and reduces prostate-specific antigen (PSA) levels.
FDA-approved for the topical treatment of acne vulgaris in patients aged 12 years and older.
Treatment of non-metastatic castration-resistant prostate cancer (nm CRPC),Treatment of metastatic castration-sensitive prostate cancer (m CSPC)
WINLEVI (clascoterone) topical cream 1%: Apply a thin layer to the affected skin areas twice daily, in the morning and evening.
240 mg orally once daily on an empty stomach, taken at least 1 hour before or 2 hours after a meal. Swallow tablets whole.
Terminal elimination half-life is approximately 7.3 hours following topical application of clascoterone 1% cream. This supports twice-daily dosing for maintaining therapeutic drug levels.
Terminal elimination half-life is approximately 20 hours (range 16-24 hours) at steady state, supporting once-daily dosing.
Clascoterone is metabolized primarily by CYP3A4 and CYP2C8 to its major metabolite, cortexolone. It undergoes extensive first-pass metabolism if absorbed systemically.
Primarily metabolized by CYP2C8 and CYP3A4 to form active metabolites (N-desmethyl apalutamide). It is also a strong inducer of CYP3A4 and CYP2C9, and has moderate effects on CYP2C19 and UGTs.
Primarily fecal (approximately 84% of the dose) and renal (approximately 2.5% of the dose) following intravenous administration. Unchanged drug accounts for less than 1% in urine and feces.
Fecal (87.4%) as unchanged drug and metabolites; renal (2.4%) as unchanged drug.
Approximately 72% bound to plasma proteins (mainly albumin and alpha-1-acid glycoprotein).
Highly protein bound (97%) primarily to albumin and α1-acid glycoprotein (AAG).
Following intravenous administration, volume of distribution is approximately 1.8 L/kg, indicating extensive tissue distribution.
Apparent volume of distribution (Vd/F) is approximately 157 L (about 2.2 L/kg for a 70 kg adult), indicating extensive extravascular distribution.
Systemic bioavailability is minimal after topical application of clascoterone 1% cream, with plasma concentrations typically below the limit of quantitation; the exact percentage is not determined, but systemic exposure is negligible (<1% of applied dose).
Oral bioavailability is not determined due to lack of intravenous formulation; after oral administration, absorption is rapid with Tmax of 2 hours under fasting conditions; food increases Cmax by 2- to 4-fold and AUC by 2-fold.
No dosage adjustment required for renal impairment, as systemic absorption is minimal.
No dose adjustment required for mild to moderate renal impairment (Cr Cl ≥30 m L/min). Not studied in severe renal impairment (Cr Cl <30 m L/min) or end-stage renal disease; use with caution.
No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C); use with caution.
Mild hepatic impairment (Child-Pugh A): no dose adjustment. Moderate (Child-Pugh B): reduce dose to 120 mg once daily. Severe (Child-Pugh C): not recommended.
Approved for patients aged 12 years and older. Same dosing as adults: apply a thin layer of 1% cream twice daily to affected areas. Safety and efficacy in children under 12 years have not been established.
Safety and efficacy not established in pediatric patients; no specific pediatric dosing available.
No specific dosage adjustment needed. However, elderly patients may have more sensitive skin; monitor for local irritation. Systemic exposure is minimal.
No specific dose adjustment required based on age alone; monitor for adverse effects (e.g., falls, hypertension) more frequently in elderly patients.
None.
No boxed warning.
Local skin reactions including erythema, pruritus, and scaling may occur. Avoid contact with eyes, mouth, and mucous membranes. Not for oral, ophthalmic, or intravaginal use. Discontinue if signs of systemic toxicity or hypersensitivity develop. Use in pregnancy only if clearly needed; no adequate and well-controlled studies exist.
Seizure: Increased risk, especially in patients with predisposing factors; discontinue if seizure occurs.,Falls and fractures: Increased incidence in clinical trials; assess fall and fracture risk.,Cardiovascular effects: Hypertension, especially in patients with pre-existing cardiovascular disease.,Thyroid dysfunction: Monitor thyroid function tests periodically.,Hypercholesterolemia: Monitor lipid profile and manage accordingly.,Hypersensitivity reactions: Including angioedema; discontinue if severe.
Hypersensitivity to clascoterone or any component of the formulation.
Pregnancy: Apalutamide can cause fetal harm and is contraindicated in pregnant women.,Severe hypersensitivity to apalutamide or any component of the formulation.
No specific food interactions are known. No dietary restrictions are required.
Grapefruit and grapefruit juice may increase apalutamide concentrations; avoid consumption. No other food interactions known.
WINLEVI (clascoterone) is a topical androgen receptor inhibitor. No adequate and well-controlled studies in pregnant women. In animal reproduction studies, no evidence of fetal harm was observed following topical administration of clascoterone during organogenesis at doses up to 2.5 mg/kg/day in rats (systemic exposure ~27 times the MRHD based on AUC) and 50 mg/kg/day in rabbits (systemic exposure 4 times the MRHD). However, because systemic absorption is minimal, the risk is considered low. Per FDA labeling, use during pregnancy only if clearly needed. No known fetal risks by trimester; avoid use on large areas of broken skin.
Risk Category X. ERLEADA (apalutamide) can cause fetal harm when administered to a pregnant woman. Nonclinical studies have demonstrated teratogenicity, including skeletal abnormalities and reduced fetal weight, at exposures below the recommended human dose. As male patients exposed to ERLEADA may father a child, a pregnancy test should be conducted for female partners of reproductive potential prior to initiating therapy. Advise male patients to use effective contraception during treatment and for 3 months after the last dose. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, apprise the patient of the potential hazard to the fetus.
It is not known whether clascoterone is excreted in human milk after topical application. Systemically absorbed clascoterone is minimal; however, it is lipophilic and may partition into breast milk. No M/P ratio is available. Due to potential for serious adverse reactions in nursing infants, advise patients to avoid application to the breast area and to discontinue nursing or drug, taking into account importance of drug to mother.
No data available on the presence of apalutamide in human milk, its effects on the breastfed infant, or its effects on milk production. Because of the potential for serious adverse reactions in breastfed infants from ERLEADA, advise women not to breastfeed during treatment and for at least 3 months after the last dose. The milk-to-plasma ratio is unknown.
No dose adjustment required in pregnancy due to minimal systemic absorption and lack of pharmacokinetic changes reported. Use with caution for acne treatment during pregnancy; weigh benefit vs risk. Apply thin layer once daily; avoid use on large areas of damaged skin.
ERLEADA is contraindicated in pregnancy. No dose adjustment is recommended for non-pregnant patients; however, due to the risk of fetal harm, use is not recommended during pregnancy. Pharmacokinetic changes of apalutamide specifically during pregnancy have not been studied, and no dose adjustments are recommended as the drug is not used in pregnant women.
WINLEVI (clascoterone) is a topical androgen receptor inhibitor approved for acne vulgaris. Avoid use on broken or eczematous skin. Monitor for signs of hyperkalemia in patients with renal impairment or those taking medications affecting potassium. Application should be limited to 1 gram per day (approximately 4 pump actuations) to minimize systemic absorption. Can be used in conjunction with other topical acne therapies but may require adjustment of irritation potential.
ERLEADA (apalutamide) requires concomitant use with a Gn RH analog or bilateral orchiectomy. Monitor for hypertension, hypothyroidism, and hypercholesterolemia. Falls and fractures are increased; assess fracture risk. Use with caution in patients at risk for seizures, as clinical seizures occurred in 0.2% of patients. Dose adjustment for CYP3A4 substrates with narrow therapeutic index.
Apply a thin layer to clean, dry skin once daily in the morning or evening as directed.,Do not apply to broken, cut, or sunburned skin.,Avoid contact with eyes, lips, and mucous membranes; if contact occurs, rinse with water.,Use sunscreen and protective clothing as WINLEVI may increase sun sensitivity.,Inform your doctor if you have kidney problems or are taking potassium-sparing diuretics or ACE inhibitors due to risk of hyperkalemia.,Do not use more than the prescribed amount; overdose can lead to systemic androgen blockade.,Store at room temperature (20°C-25°C) and keep out of reach of children.
Take ERLEADA once daily at the same time each day, with or without food. Swallow tablets whole; do not crush or chew.,Use effective contraception during treatment and for 3 months after last dose. ERLEADA can cause fetal harm.,Report any signs of infection, falls, fractures, or seizures immediately. Risk of falls and fractures is increased.,Blood pressure, thyroid function, and cholesterol levels will be monitored regularly. Report symptoms of hypothyroidism like fatigue or cold intolerance.,Avoid grapefruit, grapefruit juice, or products containing grapefruit while on ERLEADA.
No interactions on record
No interactions on record
Common clinical questions about WINLEVI vs ERLEADA, answered by our medical review team.
WINLEVI is a Topical Androgen Receptor Inhibitor that works by WINLEVI (clascoterone) is a topical androgen receptor inhibitor. It binds to the androgen receptor, preventing androgen-mediated signaling in sebocytes and inflammatory cells, thereby reducing sebum production and inflammation.. ERLEADA is a Androgen Receptor Inhibitor Antineoplastic that works by Erleada (apalutamide) is an androgen receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR, preventing AR nuclear translocation, DNA binding, and transcription of AR target genes. It also inhibits AR-mediated tumor growth and reduces prostate-specific antigen (PSA) levels.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between WINLEVI and ERLEADA depend on the specific clinical indication. These are agents from distinct pharmacological classes and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of WINLEVI is: WINLEVI (clascoterone) topical cream 1%: Apply a thin layer to the affected skin areas twice daily, in the morning and evening.. The standard adult dose of ERLEADA is: 240 mg orally once daily on an empty stomach, taken at least 1 hour before or 2 hours after a meal. Swallow tablets whole.. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between WINLEVI and ERLEADA in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. WINLEVI is classified as Category C. WINLEVI (clascoterone) is a topical androgen receptor inhibitor. No adequate and well-controlled studies in pregnant women. In animal reproduction studies, no evidence of fetal har. ERLEADA is classified as Category C. Risk Category X. ERLEADA (apalutamide) can cause fetal harm when administered to a pregnant woman. Nonclinical studies have demonstrated teratogenicity, including skeletal abnormal. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.