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  • Title: The promises of PCSK9 inhibition.
    Author: Petrides F, Shearston K, Chatelais M, Guilbaud F, Meilhac O, Lambert G.
    Journal: Curr Opin Lipidol; 2013 Aug; 24(4):307-12. PubMed ID: 23817198.
    Abstract:
    PURPOSE OF REVIEW: In the past 10 years, the LDL receptor inhibitor proprotein convertase subtilisin kexin type 9 (PCSK9) has emerged as a validated target for lowering plasma LDL cholesterol levels. Here we review the most recent reports on PCSK9 out of a total of 500 publications published in print or online before March 2013 and indexed on PubMed. RECENT FINDINGS: All published in 2012, phase I and II clinical trials demonstrate that fully human monoclonal antibodies targeting PCSK9 dramatically reduce LDL-C and enable patients to reach their target goals, without severe or serious safety issues. SUMMARY: This review summarizes the discovery of PCSK9, its original mode of action as a secreted inhibitor of the LDL receptor, as well as its genetic regulation by statins. We then focus on the major results from the 2012 phase I and II PCSK9 inhibitor clinical trials. We also review the recent in-vivo studies demonstrating the potential cardiovascular benefits of long-term PCSK9 inhibition and discuss its potential side-effects.
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