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
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.
引用
收藏
页数:12
相关论文
共 121 条
  • [61] Soluble guanylate cyclase stimulation on cardiovascular remodeling in angiotensin II-induced hypertensive rats
    Masuyama, Hiroyuki
    Tsuruda, Toshihiro
    Kato, Johji
    Imamura, Takuroh
    Asada, Yujiro
    Stasch, Johannes-Peter
    Kitamura, Kazuo
    Eto, Tanenao
    [J]. HYPERTENSION, 2006, 48 (05) : 972 - 978
  • [62] Pressure-independent effects of pharmacological stimulation of soluble guanylate cyclase on fibrosis in pressure-overloaded rat heart
    Masuyama, Hiroyuki
    Tsuruda, Toshihiro
    Sekita, Yoko
    Hatakeyama, Kinta
    Imamura, Takuroh
    Kato, Johji
    Asada, Yujiro
    Stasch, Johannes-Peter
    Kitamura, Kazuo
    [J]. HYPERTENSION RESEARCH, 2009, 32 (07) : 597 - 603
  • [63] Improving outcomes in heart failure: a personal perspective
    McMurray, John J. J. V.
    [J]. EUROPEAN HEART JOURNAL, 2015, 36 (48) : 3467 - 3470
  • [64] Baseline characteristics and treatment of patients in Prospective comparison of ARNI with ACEI to Determine Impact on Global Mortality and morbidity in Heart Failure trial (PARADIGM-HF)
    McMurray, John J. V.
    Packer, Milton
    Desai, Akshay S.
    Gong, Jianjian
    Lefkowitz, Martin
    Rizkala, Adel R.
    Rouleau, Jean L.
    Shi, Victor C.
    Solomon, Scott D.
    Swedberg, Karl
    Zile, Michael R.
    [J]. EUROPEAN JOURNAL OF HEART FAILURE, 2014, 16 (07) : 817 - 825
  • [65] August 2017 at a glance: tailored treatment, acute heart failure and cardiac resynchronization
    Metra, Marco
    [J]. EUROPEAN JOURNAL OF HEART FAILURE, 2017, 19 (08) : 969 - 970
  • [66] Crystal structure of the cofactor-binding domain of the human phase II drug-metabolism enzyme UDP-glucuronosyltransferase 2B7
    Miley, Michael J.
    Zielinska, Agnieszka K.
    Keenan, Jeffrey E.
    Bratton, Stacie M.
    Radominska-Pandya, Anna
    Redinbo, Matthew R.
    [J]. JOURNAL OF MOLECULAR BIOLOGY, 2007, 369 (02) : 498 - 511
  • [67] A-350619: A novel activator of soluble guanylyl cyclase
    Miller, LN
    Nakane, M
    Hsieh, GC
    Chang, RJ
    Kolasa, T
    Moreland, RB
    Brioni, JD
    [J]. LIFE SCIENCES, 2003, 72 (09) : 1015 - 1025
  • [68] Discovery of Riociguat (BAY 63-2521): A Potent, Oral Stimulator of Soluble Guanylate Cyclase for the Treatment of Pulmonary Hypertension
    Mittendorf, Joachim
    Weigand, Stefan
    Alonso-Alija, Cristina
    Bischoff, Erwin
    Feurer, Achim
    Gerisch, Michael
    Kern, Armin
    Knorr, Andreas
    Lang, Dieter
    Muenter, Klaus
    Radtke, Martin
    Schirok, Hartmut
    Schlemmer, Karl-Heinz
    Stahl, Elke
    Straub, Alexander
    Wunder, Frank
    Stasch, Johannes-Peter
    [J]. CHEMMEDCHEM, 2009, 4 (05) : 853 - 865
  • [69] Structure and Signaling Mechanism of Per-ARNT-Sim Domains
    Moeglich, Andreas
    Ayers, Rebecca A.
    Moffat, Keith
    [J]. STRUCTURE, 2009, 17 (10) : 1282 - 1294
  • [70] Effect of YC-1, an NO-independent, superoxide-sensitive stimulator of soluble guanylyl cyclase, on smooth muscle responsiveness to nitrovasodilators
    Mulsch, A
    Bauersachs, J
    Schafer, A
    Stasch, JP
    Kast, R
    Busse, R
    [J]. BRITISH JOURNAL OF PHARMACOLOGY, 1997, 120 (04) : 681 - 689