Development of vericiguat: The first soluble guanylate cyclase (sGC) stimulator launched for heart failure with reduced ejection fraction (HFrEF)

被引：21
作者：
Xia, Juan [1 ]
Hui, Nan [2 ]
Tian, Lei [2 ]
Liang, Chengyuan [2 ]
Zhang, Jie [2 ]
Liu, Jifang [2 ]
Wang, Jun [2 ,3 ]
Ren, Xiaodong [4 ]
Xie, Xiaolin [5 ]
Wang, Kun [6 ]
机构：
[1] Guangdong Med Univ, Lab Hematol Dis, Affiliated Hosp, Zhanjiang 524001, Peoples R China
[2] Shaanxi Univ Sci & Technol, Fac Pharm, Xian 710021, Peoples R China
[3] Qinghai Prov Drug Inspect & Testing Inst, Key Lab Tradit Chinese & Tibetan Med Qinghai Prov, Xining 810000, Peoples R China
[4] Guizhou Univ, Med Coll, Guiyang 550025, Peoples R China
[5] Shaanxi Panlong Pharmaceut Grp Co Ltd, Xian 710025, Peoples R China
[6] Qingdao Univ, Affiliated Taian City Centeral Hosp, Childrens Ctr, Tai An 271000, Shandong, Peoples R China
来源：
BIOMEDICINE & PHARMACOTHERAPY | 2022年 / 149卷
基金：
中国国家自然科学基金; 中国博士后科学基金;
关键词：
Drug discovery; Heart failure (HF); Structure-activity relationship (SAR); Soluble guanylate cyclase (sGC) stimulator; Vericiguat; NITRIC-OXIDE; DOUBLE-BLIND; INDEPENDENT STIMULATION; CRYSTAL-STRUCTURE; DRUG DISCOVERY; BAY; 63-2521; CYCLIC-GMP; RIOCIGUAT; ACTIVATORS; PHARMACOKINETICS;
D O I：
10.1016/j.biopha.2022.112894
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
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.
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页数：12
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