Aprocitentan

Keywords:

corresponding

Rodrigo Souza

Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University
of Rio de Janeiro, Rio de Janeiro, Brazil

Aprocitentan, sold under the brand name Tryvio (Idorsia), is a medication used for the treatment of hypertension (high blood pressure). It has been approved by the FDA to treat hypertension in combination with other antihypertensive medications in adults who can’t adequately control their blood pressure with existing therapies. Aprocitentan is an endothelin receptor antagonist that inhibits the binding of endothelin (ET)-1 to ETA and ETB receptors. The effects of ET-1 bear many similarities with the pathophysiology of hypertension, and ET-1 is a major driver of aldosterone production. Until the approval of TRYVIO, no systemic antihypertensive medications targeted the ET pathway, as approved antihypertensive therapies focus on the regulation of salt and water (diuretics), antagonism of the renin–angiotensin–aldosterone (RAAS) system, reduction of influx of extracellular calcium into the cell (calcium channel blockers), sympatholytic activity (beta blockers, central alpha-agonist agents), or non-selective vasodilatory effects.


Idorsia was formed through a spinoff after J&J’s $30 billion buyout of Actelion in 2017. The Swiss biotech started off with CH ...