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Emerging innovative therapeutic approaches targeting PCSK9 to lower lipids
Author(s) -
Shantha GPS,
Robinson JG
Publication year - 2016
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt.281
Subject(s) - alirocumab , evolocumab , pcsk9 , ezetimibe , medicine , proprotein convertase , kexin , statin , clinical trial , adverse effect , disease , pharmacology , cholesterol , lipoprotein , ldl receptor , apolipoprotein a1
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.