Why the study?
Despite available antihypertensive medications, there is a conspicuous lack of therapeutic options specifically intended for the management of expanding cohorts with resistant hypertension.
Aprocitentan, a dual endothelin receptor antagonist, is under development as a novel therapeutic option for resistant hypertension.
May expand options for resistant hypertension; leaves open efficacy and safety pending Phase 3 data.
As 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.
No takes yet. Share an insight, caveat, or question.
Yao et al. (2023) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: