Aprocitentan 12.5 mg Suppliers & Bulk Manufacturers

Available Forms: Tablets

Available Strengths: 12.5 mg

Reference Brands: Tryvio (USA), Jeraygo (EU)

Category: Hypertension

Aprocitentan is a Hypertension product available as Tablets in strengths 12.5 mg. It corresponds to the reference brands Tryvio (USA), Jeraygo (EU). Verified GMP manufacturers and suppliers on PharmaTradz offer it in bulk for import worldwide, with regulatory documentation and dossier support available on request.

Product Description:

Aprocitentan (ACT-132577) is an orally active, dual endothelin-1 (ET-1) receptor antagonist that blocks ET-1 binding to both ETA and ETB receptors. It is the active metabolite of macitentan, an orphan drug used in pulmonary arterial hypertension, and is highly bound to plasma proteins with elimination via urine and feces. Aprocitentan is well tolerated at single doses up to 600 mg and multiple doses up to 100 mg once daily, with a half-life of approximately 44 hours, supporting convenient once-daily dosing. Its pharmacokinetic profile shows only minor variations across sex, age, renal function, and fed or fasted conditions.

In patients with resistant hypertension, Aprocitentan has demonstrated significant blood pressure reductions within 14 days, and its effects are enhanced when combined with other antihypertensives, including renin-angiotensin-system blockers. The drug has shown consistent efficacy in ambulatory blood pressure monitoring, aligning with surrogate markers for reduced cardiovascular risk. Currently under investigation in the PRECISION Phase III trial, Aprocitentan holds promise as a novel therapy for treatment-resistant hypertension, potentially expanding the antihypertensive options and providing broader cardiovascular protection for patients whose blood pressure remains uncontrolled despite standard therapy.