›› 2018, Vol. 38 ›› Issue (2): 212-.doi: 10.3969/j.issn.1674-8115.2018.02.018

• Review • Previous Articles     Next Articles

Clinical research of PCSK9 inhibitors in reducing low density lipoprotein cholesterol

JI Hai-ying, YOU Sha-sha, CAO Hui-min, HE Bin   

  1. Department of Anesthesiology and SICU, Xinhua Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China
  • Online:2018-02-28 Published:2018-03-09
  • Supported by:
    National Natural Science Foundation of China, 81470390; Shanghai Municipal Education Commission—Gaofeng Clinical
    Medicine Grant Support, 20152218; Clinical Research Plan of Shanghai Hospital Development Center, 16CR3006A; Program of Science and Technology Commission of Shanghai Municipality, 17411954700

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Abstract: Elevated low density lipoprotein cholesterol (LDL-C) is a major risk factor for cardiovascular disease. Studies show that proprotein convertase subtilisin/kexin type 9 (PCSK9) is a circulation enzyme and serves a pivotal function in the degradation of low density lipoprotein receptor, which contributes to the decrease in hepatic cholesterol uptake and increase in circulating LDL-C. PCSK9 inhibitor can significantly elevate the surface of low density lipoprotein receptor of liver cells and bond more LDL-C to decrease the level of LDL-C. Thus PCSK9 has emerged as a popular target for the development of new cholesterol lowering drugs and therapeutic intervention of cardiovascular disease. In this article, the history, mechanism of action, metabolic effects of PCSK9 and the clinical outcomes of PCSK9 inhibitors will be briefly reviewed.

Key words:  proprotein convertase subtilisin/kexin type 9 (PCSK9), low density lipoprotein receptor, cardiovascular disease, PCSK9 inhibitor, clinical trial