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维立西呱,一种被批准用于治疗心力衰竭的可溶性鸟苷酸环化酶刺激剂。

Vericiguat, a Soluble Guanylate Cyclase Stimulator Approved for Heart Failure Treatment.

作者信息

Kallash Mohammed, Frishman William H

机构信息

From the Department of Medicine, New York Medical College, School of Medicine, Valhalla, NY.

Department of Medicine, Westchester Medical Center, Valhalla, NY.

出版信息

Cardiol Rev. 2025 Jun 20. doi: 10.1097/CRD.0000000000000963.

Abstract

Heart failure (HF) is an emerging, global epidemic associated with substantial morbidity and mortality. In recent years, significant advancements have been made in the development of pharmacotherapies that provide mortality benefits in HF. Research into the pathophysiology of HF with reduced ejection fraction (HFrEF) has identified significant abnormalities in the critical nitric oxide (NO)-soluble guanylate cyclase (sGC)-cyclic guanosine monophosphate (cGMP) cascade. In HFrEF, there is reduced NO bioavailability, impaired sGC activity, and upregulation of phosphodiesterase activity, all causing a significant decrease in cGMP, impairing vasodilation and increasing cardiac fibrosis and hypertrophy. Vericiguat, an sGC stimulator, was developed to potentially harness the therapeutic efficacy of this pathway. In a major clinical trial, vericiguat use in patients with HFrEF on guideline-directed medical therapy and recent worsening of HF resulted in a significant decrease in the composite of death from cardiovascular causes or first hospitalization for HF compared with placebo. Current American Heart Association guidelines recommend that in selected high-risk patients with HFrEF and recent worsening of HF already on guideline-directed medical therapy, initiation of the oral sGC stimulator vericiguat may be considered to reduce HF hospitalization and cardiovascular death. However, while vericiguat represents a major accomplishment in capitalizing on the therapeutic potential of the NO-sGC-cGMP pathway, there remain significant challenges regarding the personalization of therapy and identification of the phenotype of the HFrEF population that most benefits from vericiguat therapy. Further research is currently underway to identify vericiguat's potential role in the treatment of chronic stable HFrEF without recent worsening of HF.

摘要

心力衰竭(HF)是一种正在出现的全球性流行病,与高发病率和死亡率相关。近年来,在开发对HF具有降低死亡率益处的药物治疗方面取得了重大进展。对射血分数降低的心力衰竭(HFrEF)病理生理学的研究已经确定,关键的一氧化氮(NO)-可溶性鸟苷酸环化酶(sGC)-环磷酸鸟苷(cGMP)级联存在显著异常。在HFrEF中,NO生物利用度降低、sGC活性受损以及磷酸二酯酶活性上调,所有这些都会导致cGMP显著减少,损害血管舒张并增加心脏纤维化和肥大。维立西呱是一种sGC刺激剂,旨在潜在地利用该途径的治疗效果。在一项主要临床试验中,与安慰剂相比,在接受指南指导药物治疗且近期HF病情恶化的HFrEF患者中使用维立西呱,导致心血管原因死亡或首次因HF住院的复合终点显著降低。美国心脏协会目前的指南建议,对于已经接受指南指导药物治疗且近期HF病情恶化的选定高危HFrEF患者,可以考虑启动口服sGC刺激剂维立西呱,以减少HF住院和心血管死亡。然而,虽然维立西呱在利用NO-sGC-cGMP途径的治疗潜力方面代表了一项重大成就,但在治疗个性化以及确定最能从维立西呱治疗中获益的HFrEF人群表型方面,仍然存在重大挑战。目前正在进行进一步研究,以确定维立西呱在治疗慢性稳定HFrEF且近期HF无恶化情况中的潜在作用。

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