Aprocitentan

Aprocitentan is a dual endothelin receptor antagonist and certified reference standard developed for the treatment of resistant hypertension. As the active pharmaceutical ingredient marketed as Tryvio®, Aprocitentan received FDA approval in March 2024 as the sixth novel drug approved that year. In pharmaceutical quality control contexts, Aprocitentan serves as the primary reference standard for impurity profiling, analytical method development, and regulatory submissions. Aprocitentan is indicated for use in combination with other antihypertensive drugs for adults with hypertension not adequately controlled by other medications. The drug substance Aprocitentan is available as oral tablets (12.5 mg, once daily) and can be taken with or without food. Furthermore, Aprocitentan functions as the major active metabolite of macitentan, demonstrating the therapeutic potential of this well-characterized molecular scaffold in cardiovascular disease management.

Product Parameters

Why Cosperpharm?

When your endothelin receptor antagonist research program or reference standard requirements demand uncompromising quality, Cosperpharm delivers Aprocitentan with the analytical rigor, documentation depth, and supply flexibility that pharmaceutical customers have come to trust.

Purity that drives research success. The dual ETA/ETB receptor antagonism of Aprocitentan is exquisitely sensitive to impurities. Cosperpharm's analytical release protocol for Aprocitentan includes HPLC purity verification (≥97%), appearance verification, and identity confirmation. Batch-specific chromatographic traceability ensures that your research or analytical method rests on a foundation of documented quality.

Documentation that supports your regulatory submission. As a recently FDA-approved novel drug, Aprocitentan reference standards are essential for generic development and quality control programs. Every reference-grade shipment from Cosperpharm includes a Certificate of Analysis (COA) with batch-specific purity data and full characterization.

Flexible supply across all research stages. Cosperpharm supplies Aprocitentan from milligram quantities for analytical reference standard use to gram-scale batches for process development. R&D samples ship within 5–7 business days; bulk orders ship within 2–3 weeks.

Global reach with transparent pricing. Cosperpharm ships to pharmaceutical manufacturers, CROs, and analytical laboratories worldwide, with full customs documentation included.

Product Advantages

 Dual Endothelin Receptor Antagonist

Aprocitentan functions as a dual ETA/ETB receptor antagonist, blocking both endothelin receptor subtypes. This balanced antagonism profile is essential for the therapeutic efficacy of Aprocitentan in lowering blood pressure in patients with resistant hypertension.

 FDA-Approved Novel Drug

Aprocitentan received FDA approval in March 2024 under the brand name Tryvio®, making it a well-characterized reference compound for hypertension research and generic development.

 Major Active Metabolite of Macitentan

Aprocitentan is the primary active metabolite of macitentan, providing a well-documented pharmacokinetic and pharmacodynamic profile. This metabolite-based mechanism positions Aprocitentan as a valuable tool compound for studying the endothelin system.

 Dual-Use: API and Reference Standard

Cosperpharm supplies Aprocitentan at high-purity grade for use in both research applications and as an analytical reference standard for method development and quality control programs.

 Well-Characterized Clinical Profile

Aprocitentan is approved in combination with other antihypertensive drugs for adult patients with hypertension not adequately controlled by other medications, validating its clinical utility.

FAQ

Q1: What is the mechanism of action of Aprocitentan?

A: Aprocitentan is a dual ETA/ETB endothelin receptor antagonist. It blocks both endothelin receptor subtypes, with pA₂ values of 6.7 (ETA) and 5.5 (ETB), and IC₅₀ values of 3.4 nM and 987 nM, respectively.

Q2: What are the primary therapeutic indications for Aprocitentan?

A: Aprocitentan is indicated for the treatment of resistant hypertension in adults, used in combination with other antihypertensive drugs for patients whose blood pressure is not adequately controlled by other medications.

Contact Us

Partner with Cosperpharm for Aprocitentan that delivers the purity, documentation, and supply reliability your research program requires. Whether you are advancing endothelin receptor research, developing analytical methods, or scaling up production, our team is ready to support your success.