• Arch Med Sci · Jun 2017

    PCSK9 inhibitors - from discovery of a single mutation to a groundbreaking therapy of lipid disorders in one decade.

    • Krzysztof Jaworski, Piotr Jankowski, and Dariusz A Kosior.
    • 2 Department of Coronary Artery Disease, Institute of Cardiology, Warsaw, Poland.
    • Arch Med Sci. 2017 Jun 1; 13 (4): 914929914-929.

    AbstractHypercholesterolemia is one of the main risk factors for coronary heart disease and significantly contributes to the high mortality associated with cardiovascular diseases. Statin therapy represents the gold standard in the reduction of low-density lipoprotein cholesterol concentration. Nevertheless, many patients still cannot achieve the recommended target levels, due to either inadequate effectiveness or intolerance of these drugs. Monoclonal antibodies that inhibit proprotein convertase subtilisin/kexin type 9 (PCSK9) have emerged as a promising option in lipid-lowering treatment. After confirmation of their efficacy and safety in clinical trials, evolocumab and alirocumab received approval from the US Food and Drug Administration (FDA) and European Medicines Agency (EMA) for introduction into clinical practice. In this review, we present a history of the development and mechanisms of action, as well as the results of the most important studies concerning PCSK9 inhibitors.

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