Department of Cardiology, The Second Hospital of Shanxi Medical University, Taiyuan, Shanxi, China.
Shanxi Medical University, Taiyuan, Shanxi, China.
J Clin Hypertens (Greenwich). 2023 Jul;25(7):587-590. doi: 10.1111/jch.14686. Epub 2023 Jun 19.
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.
随着开始抗高血压治疗的血压阈值降低，患有难治性高血压（RH）的患者群体相应扩大。尽管有已知的降压药物，但针对 RH 管理的治疗选择仍存在明显的空白。目前，阿普西坦（aprocitentan）是唯一一种正在开发的用于应对这一紧迫临床挑战的内皮素受体拮抗剂（ERA）。阿普西坦（ACT-132577）作为马西替坦的代谢物产生其活性形式，作为一种双重内皮素（ET）受体拮抗剂具有口服效力。该化合物可有效阻止内皮素-1（ET-1）与 ETA 和 ETB 受体结合，表现出 1:16 的抑制效力比。阿普西坦的临床研究已推进到 3 期试验，初步结果令人鼓舞。
