Xia Juan, Hui Nan, Tian Lei, Liang Chengyuan, Zhang Jie, Liu Jifang, Wang Jun, Ren Xiaodong, Xie Xiaolin, Wang Kun
Laboratory of Hematologic Diseases, Affiliated Hospital of Guangdong Medical University, Zhanjiang 524001, PR China.
Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an 710021, PR China.
Biomed Pharmacother. 2022 May;149:112894. doi: 10.1016/j.biopha.2022.112894. Epub 2022 Apr 1.
In recent years, with improvements in treatments for heart failure (HF), the survival period of patients has been extended. However, the emergence of some patients with repeated hospitalizations due to their worsening conditions and low survival rates followed. Currently, few drugs are available for such patients. Vericiguat was first drug approved for the treatment of symptomatic patients with chronic HF with reduced ejection fraction (HFrEF) to reduce the occurrence of worsening HF. This article provides comprehensive information about vericiguat in terms of drug design and development, structure-activity relationship (SAR), synthesis, pharmacological efficacy, and clinical practice. In addition, insights into the current vericiguat trials and treatments of HF are also discussed.
近年来，随着心力衰竭（HF）治疗方法的改进，患者的生存期得以延长。然而，随后出现了一些病情恶化且生存率低、反复住院的患者。目前，针对这类患者的药物很少。维立西呱是首个被批准用于治疗射血分数降低的慢性HF（HFrEF）症状性患者以减少HF恶化发生率的药物。本文提供了关于维立西呱在药物设计与开发、构效关系（SAR）、合成、药理作用以及临床实践方面的全面信息。此外，还讨论了对当前维立西呱治疗HF试验的见解。
