Affiliation:
1. Department of Cardiology The Second Hospital of Shanxi Medical University Taiyuan Shanxi China
2. Shanxi Medical University Taiyuan Shanxi China
Abstract
AbstractAs the blood pressure threshold for commencing antihypertensive treatment diminishes, the cohort suffering from resistant hypertension (RH) correspondingly expands. Notwithstanding the availability of known antihypertensive medications, there exists a conspicuous lacuna in therapeutic options specifically intended for the management of RH. Currently, aprocitentan is the sole endothelin receptor antagonist (ERA) under development for addressing this pressing clinical challenge. Aprocitentan (ACT‐132577), deriving its active form as a metabolite of macitentan, demonstrates oral potency as a dual endothelin (ET) receptor antagonist. This compound effectively obstructs the binding of endothelin‐1 (ET‐1) to both ETA and ETB receptors, exhibiting an inhibitory potency ratio of 1:16. Clinical investigation of aprocitentan has advanced to phase 3 trials, yielding promising preliminary outcomes.
Subject
Cardiology and Cardiovascular Medicine,Endocrinology, Diabetes and Metabolism,Internal Medicine
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