Emerging innovative therapeutic approaches targeting PCSK9 to lower lipids

AUTHORS: GPS Shantha and JG Robinson
(Dr. Shantha is a Cardiology Fellow)

JOURNAL: Clinical Pharmacology & Therapeutics, 99(1):59–71, January 2016


Statins are established therapies for cardiovascular disease prevention and ezetimibe has recently been shown to modestly reduce cardiovascular events when added to background statin therapy. Yet here remains a clear unmet need for additional therapies aimed at lowering low density lipoprotein cholesterol (LDL-C) to further reduce cardiovascular risk. Multiple strategies targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibition have emerged as effective modalities for LDL-C lowering. PCSK9 monoclonal antibodies are the farthest along in clinical development and alirocumab and evolocumab were approved for clinical use by regulatory agencies in 2015. In addition to robust LDL-C lowering (nearly 50–65% from baseline), they improve other lipid parameters as well. Adverse events associated with these medications are minimal. Importantly, they improve clinical cardiovascular disease outcomes, although long-term study results are awaited. Cost may be an important limiting factor in their use and we propose two possible solutions which can potentially curtail cost.

Link to journal online: http://onlinelibrary.wiley.com/doi/10.1002/cpt.281/full

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