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Alternate Names: N-Despropyl Macitentan, aprocitentanum, Tryvio (TN)
CAS No: 1103522-45-7
PubChem CID: 25099191
Mol Formula: C16H14Br2N6O4S
Mol Weight: 546.2 g/mol
IUPAC Name: 5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine
API Description: Aprocitentan is a dual antagonist of endothelin receptors A and B used for treatment-resistant hypertension. It is the active metabolite of [macitentan]. Approximately 10-15% of patients with hypertension have resistant hypertension, defined as uncontrolled high blood pressure despite the combined use of a renin-angiotensin system blocker, a calcium channel blocker, and a diuretic at maximally tolerated doses. Patients with resistant hypertension are at an increased risk of cardiovascular and renal events and have traditionally had limited additional treatment options. Endothelin receptor antagonism provides a novel therapeutic pathway for the management of patients with resistant hypertension. Aprocitentan was approved by the FDA in March 2024 for the treatment of hypertension in patients inadequately controlled with standard therapy. It was the first antihypertensive employing a novel mechanism to be approved in almost 40 years.
