Cardiovascular Drugs and Therapy

, Volume 29, Issue 2, pp 159–169 | Cite as

Update of Clinical Trials of Anti-PCSK9 Antibodies

  • Na-Qiong Wu
  • Sha Li
  • Jian-Jun Li


Hyperlipidemia is a predominant risk factor for cardiovascular disease (CVD). Statins have been successfully used to treat patients with dyslipidemia and decrease the events of CVD in addition to application of various other non-statin-lowering cholesterol agents, such as ezetimibe and niacin. However, there are still residual risks in patients with atherosclerotic CVD. Recently, proprotein convertase subtilisin/kexin type 9 (PCSK9), which was first identified in 2003, has been suggested to play an important role in the metabolism of low-density lipoprotein cholesterol (LDL-C). PCSK9 degrades the LDL-receptor, which may be pharmacologically targeted to improve the lipoprotein profile and future cardiovascular outcomes in patients with dyslipidemia. Several approaches to inhibiting PCSK9 activity have been theoretically proposed. Among them, monoclonal antibodies have been considered as the most promising strategy because of their large effect on lowering lipids as monotherapy and in combination with statins or ezetimibe. In this review, we mainly focus on the current status of monoclonal antibodies of PCSK9 and clinical trial results for an update on clinical application of monoclonal antibodies of PCSK9. The particular effects of monoclonal antibodies of PCSK9 on lipid profiles are also discussed.


Proprotein convertase subtilisin/kexin type 9 Hyperlipidemia Cardiovascular diseases Antibodies Clinical trials 



This work was partly supported by the National Natural Scientific Foundation (81070171, 81241121), the Specialized Research Fund for the Doctoral Program of Higher Education of China (20111106110013), the Capital Special Foundation of Clinical Application Research (Z121107001012015), the Capital Health Development Fund (2011400302), and the Beijing Natural Science Foundation (7131014), which were awarded to Dr. Jian-Jun Li, MD, PhD.

Disclosure statement

The authors declare that they have no conflict of interest.


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© Springer Science+Business Media New York 2015

Authors and Affiliations

  1. 1.Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical SciencesPeking Union Medical CollegeBeijingChina

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