Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
WINLEVI vs RELPAX
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.
Selective 5-HT1B/1D receptor agonist; causes vasoconstriction of intracranial arteries, inhibits trigeminal nerve activation, and reduces neurogenic inflammation.
FDA-approved for the topical treatment of acne vulgaris in patients aged 12 years and older.
Acute treatment of migraine with or without aura in adults,Acute treatment of migraine in children aged 6-17 years (FDA-approved for ≥40 kg)
WINLEVI (clascoterone) topical cream 1%: Apply a thin layer to the affected skin areas twice daily, in the morning and evening.
20-40 mg orally once; maximum 80 mg per 24 hours. Single dose may be repeated after 2 hours if migraine recurs.
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 6.2 hours (range 4.7–8.1 hours) in healthy adults; prolonged in renal impairment (up to 9.5 hours).
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 CYP3A4; less than 10% excreted unchanged in urine.
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.
Approximately 60% of the dose is excreted in urine (primarily as metabolites, with ~14% unchanged) and 40% in feces via biliary elimination.
Approximately 72% bound to plasma proteins (mainly albumin and alpha-1-acid glycoprotein).
Approximately 30% bound to plasma proteins (mainly albumin).
Following intravenous administration, volume of distribution is approximately 1.8 L/kg, indicating extensive tissue distribution.
Vd is 3.0 L/kg (range 2.1–4.0 L/kg), indicating extensive tissue distribution (extravascular).
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 50% (range 40–60%) due to first-pass metabolism; no other routes available.
No dosage adjustment required for renal impairment, as systemic absorption is minimal.
No dose adjustment required for mild to moderate renal impairment (Cr Cl 30-80 m L/min). Contraindicated in severe renal impairment (Cr Cl <30 m L/min).
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.
Contraindicated in severe hepatic impairment (Child-Pugh C). No dose adjustment for mild to moderate (Child-Pugh A/B).
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.
Not recommended for patients <18 years of age; safety and efficacy not established.
No specific dosage adjustment needed. However, elderly patients may have more sensitive skin; monitor for local irritation. Systemic exposure is minimal.
Use with caution. No specific dose adjustment, but increased sensitivity; start at 20 mg.
None.
Do not administer to patients with ischemic heart disease, coronary artery vasospasm (including Prinzmetal variant angina), or other significant underlying cardiovascular disease.
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.
Risk of myocardial ischemia, infarction, and coronary vasospasm,Cerebrovascular events (e.g., stroke, cerebral hemorrhage),Serotonin syndrome (especially with SSRIs, SNRIs, MAOIs),Risk of medication overuse headache with frequent use,Severe hepatic impairment (Child-Pugh C): contraindicated,Peripheral ischemia and gastrointestinal ischemia
Hypersensitivity to clascoterone or any component of the formulation.
Ischemic heart disease, history of myocardial infarction, coronary artery vasospasm,Cerebrovascular disease (e.g., stroke, transient ischemic attack),Uncontrolled hypertension (≥180/110 mm Hg),Hemiplegic or basilar migraine,Concurrent use of ergotamine derivatives or other 5-HT1 agonists,Concurrent MAO inhibitor use or within 2 weeks of discontinuation,Severe hepatic impairment (Child-Pugh C),Hypersensitivity to eletriptan or any component of the formulation,Prophylactic use for migraine
No specific food interactions are known. No dietary restrictions are required.
No significant food interactions. Grapefruit may increase eletriptan levels; avoid grapefruit juice.
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.
Pregnancy Category C. Eletriptan (RELPAX) has shown embryotoxicity and fetotoxicity in animal studies at maternally toxic doses. There are no adequate and well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus. First trimester: limited data suggest no major malformations; however, definitive conclusions cannot be drawn. Second and third trimesters: risk unknown; avoid use due to potential uteroplacental vasoconstriction and decreased uterine blood flow.
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.
Eletriptan is excreted into human breast milk. The milk-to-plasma ratio is approximately 0.14 for the parent drug and 0.33 for the active metabolite. Concentration in milk is low (mean relative infant dose approximately 0.02% of maternal weight-adjusted dose). Caution is advised, particularly in infants with impaired renal function. Monitor infant for potential adverse effects such as drowsiness or feeding difficulties.
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.
Physiologic changes in pregnancy (increased plasma volume, renal clearance, and hepatic metabolism) may alter eletriptan pharmacokinetics. However, specific dose adjustment recommendations are not established due to lack of data. Use lowest effective dose. Start with 20 mg; may repeat after 2 hours if migraine recurs, not to exceed 40 mg/day. Avoid use in severe hypertension or preeclampsia due to vasoconstrictive properties.
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.
Relpax (eletriptan) is a 5-HT1B/1D receptor agonist used for acute migraine. Avoid within 24 hours of other triptans or ergotamines. Contraindicated in patients with ischemic heart disease, uncontrolled hypertension, or hemiplegic/basilar migraine. Onset of action can be as early as 30 minutes. Maximum dose is 40 mg per 24 hours; single dose of 20 mg is effective for many. Consider shorter triptan half-life (4 hours vs sumatriptan's 2) for patients needing rapid clearance. Not effective for migraine prophylaxis.
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 at the first sign of migraine; do not use for prevention.,Do not take more than one dose within 24 hours; maximum 40 mg.,Avoid within 24 hours of other triptans or ergotamine-containing medications.,Seek emergency care if chest pain, shortness of breath, or severe allergic reaction occurs.,Do not use if you have a history of heart disease, stroke, or uncontrolled high blood pressure.,May cause dizziness or drowsiness; avoid driving until you know how it affects you.
No interactions on record
No interactions on record
Common clinical questions about WINLEVI vs RELPAX, 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.. RELPAX is a Triptan (Serotonin Agonist) that works by Selective 5-HT1B/1D receptor agonist; causes vasoconstriction of intracranial arteries, inhibits trigeminal nerve activation, and reduces neurogenic inflammation.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between WINLEVI and RELPAX 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 RELPAX is: 20-40 mg orally once; maximum 80 mg per 24 hours. Single dose may be repeated after 2 hours if migraine recurs.. 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 RELPAX 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. RELPAX is classified as Category C. Pregnancy Category C. Eletriptan (RELPAX) has shown embryotoxicity and fetotoxicity in animal studies at maternally toxic doses. There are no adequate and well-controlled studies i. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.