tcsc2687 Aprocitentan

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.

In Vitro: Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3)^[1].

In Vivo: Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat^[1]. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%^[2].