Volibris | 合法藥品大搜索

Volibrisisindicatedfortreatmentofpulmonaryarterialhypertension(PAH)inadultpatientsofWHOFunctionalClass(FC)IItoIII,includinguseincombination​ ...

Pharmacotherapeutic group: Anti-hypertensives, other anti-hypertensives, ATC code: C02KX02

Mechanism of action

Ambrisentan is an orally active, propanoic acid-class, ERA selective for the endothelin A (ETA) receptor. Endothelin plays a significant role in the pathophysiology of PAH.

Ambrisentan is an ETA antagonist (approximately 4 000-fold more selective for ETA as compared to ETB).

Ambrisentan blocks the ETA receptor subtype, localised predominantly on vascular smooth muscle cells and cardiac myocytes. This prevents endothelin-mediated activation of second messenger systems that result in vasoconstriction and smooth muscle cell proliferation.

The selectivity of ambrisentan for the ETA over the ETB receptor is expected to retain ETB receptor mediated production of the vasodilators nitric oxide and prostacyclin.

Clinical efficacy and safety

Two randomised, double-blind, multi-centre, p...