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Review
. 2023 Jul;25(7):587-590.
doi: 10.1111/jch.14686. Epub 2023 Jun 19.

Aprocitentan: A new development of resistant hypertension

Yao Yao  1   2 , Bin Fan  2 , Bin Yang  1 , Zixuan Jia  2 , Bao Li  1
Affiliations
Review

Aprocitentan: A new development of resistant hypertension

Yao Yao et al. J Clin Hypertens (Greenwich). 2023 Jul.

Abstract

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.

Keywords: ACT-132577; PRECISION; aprocitentan; phase 3 clinical trials; resistant hypertension.

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Conflict of interest statement

We declare that we have no financial and personal relationships with other people or organizations that can inappropriately influence our work, there is no professional or other personal interest of any nature or kind in any product, service, and/or company that could be construed as influencing the position presented in, or the review of, the manuscript entitled.

Figures

FIGURE 1
FIGURE 1
Chemical structure of aprocitentan.
See this image and copyright information in PMC

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