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Targeting the peptidase PCSK9 to reduce cardiovascular risk: Implications for basic science and upcoming challenges
Author(s) -
Nishikido Toshiyuki,
Ray Kausik K.
Publication year - 2021
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.14851
Subject(s) - pcsk9 , medicine , statin , ldl receptor , ldl cholesterol , cholesterol , atherosclerotic cardiovascular disease , disease , pharmacology , lipoprotein
LDL cholesterol (LDL‐C) plays a central role in the progression of atherosclerosis. Statin therapy for lowering LDL‐C reduces the risk of atherosclerotic cardiovascular disease and is the recommended first‐line treatment for patients with high LDL‐C levels. However, some patients are unable to achieve an adequate reduction in LDL‐C with statins or are statin‐intolerant; thus, PCSK9 inhibitors were developed to reduce LDL‐C levels, instead of statin therapy. PCSK9 monoclonal antibodies dramatically reduce LDL‐C levels and cardiovascular risk, and promising new PCSK9 inhibitors using different mechanisms are currently being developed. The absolute benefit of LDL‐C reduction depends on the individual absolute risk and the achieved absolute reduction in LDL‐C. Therefore, PCSK9 inhibitors may provide the greatest benefits from further LDL‐C reduction for the highest risk patients. Here, we focus on PCSK9‐targeted therapies and discuss the challenges of LDL‐C reduction for prevention of atherosclerotic cardiovascular disease.