As part of its endothelin receptor antagonist (ERA) program, Actelion has discovered an orally active, potent dual-acting ERA, suitable for development in specialty cardiovascular disorders.

Actelion is a leader in the field of endothelin receptor antagonism, with macitentan (Opsumit®), an orally available endothelin receptor antagonist (ERA) that resulted from a tailored drug discovery process in Actelion's laboratories.


Actelion's latest ERA  (ACT-132577) is evaluated in a Phase II prospective, multi-center, double-blind, double-dummy, randomized, placebo- and active-reference, parallel group, dose-finding study in patients with essential hypertension (grade 1 and 2) to establish a dose-effect relationship. The results from this study will form the basis for development decisions in specialty cardiovascular disorders. Patients will be randomized in the 6 groups in a 1:1:1:1:1:1 ratio: placebo; dose 1, dose 2, dose 3, dose 4 of Actelion's ERA; and lisinopril 20 mg.


Pharmacokinetic, pharmacodynamic, safety and tolerability data from a Phase I program support further exploration of ERA in patients with cardiovascular disorders.


2015 > Initiation of Phase II dose-response study

2014 > Initiation of Phase I clinical program


Iglarz M, et al. Clin Sci 2010; 119:453-63