Novel Dual Endothelin Inhibitors in the Management of Resistant Hypertension

Author:

Boutari Chrysoula1ORCID,Siskos Fotios1ORCID

Affiliation:

1. 2nd Propedeutic Department of Internal Medicine, Medical School, Aristotle University of Thessaloniki, Hippokration General Hospital, 54642 Thessaloniki, Greece

Abstract

Resistant hypertension (RH) is defined as the failure to achieve blood pressure control despite using triple combination therapy with a renin-angiotensin system inhibitor (RAS-i), a calcium antagonist, and a diuretic. The endothelin (ET) system is implicated in the regulation of vascular tone, primarily through vasoconstriction, intervenes in cardiac contractility with inotropic effects, and contributes to water and sodium renal reabsorption. ET inhibitors, currently approved for the treatment of pulmonary hypertension, seem to be also useful for essential hypertension and RH as well. Studies into the development of new dual ET inhibitors, which inhibit both type A and B ET (ETA and ETB) receptors, present initial results of managing RH. Aprocitentan (ACT-132577) is a novel, orally active and well tolerated dual ET receptor antagonist, which has been examined in several experimental studies and clinical trials with promising results for RH control. The recent publication of the large PRECISION study in The Lancet journal provides further reassurance regarding the efficacy and safety of aprocitentan for RH, with the aim of overcoming unmet needs in the management of this difficult group of patients.

Publisher

MDPI AG

Subject

Paleontology,Space and Planetary Science,General Biochemistry, Genetics and Molecular Biology,Ecology, Evolution, Behavior and Systematics

Cited by 2 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. Advances on the Experimental Research in Resistant Hypertension;Current Hypertension Reports;2024-07-18

2. Hypertension and Heart Failure: From Pathophysiology to Treatment;International Journal of Molecular Sciences;2024-06-17

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