title: Alirocumab: targeting PCSK9 to treat hypercholesterolemia.
abstract: Lowering of low-density lipoprotein (LDL) cholesterol reduces coronary heart disease morbidity and mortality, not only in secondary but also in primary prevention. Statins are generally accepted as a treatment of choice for this. However, still many high-risk and very-high-risk patients fail to achieve target LDL cholesterol values. Therefore, a new class of lipid-lowering drugs was recently developed-inhibitors of proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab was the first drug in this class to be approved by the U.S. Food and Drug Administration (FDA) and recently also by the European Medicines Agency (EMA). Alirocumab has been shown to lower LDL cholesterol by up to 60% with a safety profile comparable to that of placebo. Large outcome studies are still on the way and their first results will be available in 2017. This review focuses on alirocumab, discussing currently available hard evidence on the beneficial effects of this drug in the treatment of hypercholesterolemia.
authors.affiliation: University Hospital Center Zagreb, Department of Internal Medicine, Kišpatićeva 12, Zagreb, Croatia; School of Medicine, University of Zagreb, Zagreb, Croatia.
authors.forename: I
authors.initials: I
authors.lastname: Pećin
authors.affiliation: University Hospital Center Zagreb, Department of Internal Medicine, Kišpatićeva 12, Zagreb, Croatia; School of Medicine, University of Zagreb, Zagreb, Croatia. zreiner@kbc-zagreb.hr.
authors.forename: Ž
authors.initials: Ž
authors.lastname: Reiner
mesh_terms: D000911:Antibodies, Monoclonal / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D061067:Antibodies, Monoclonal, Humanized; D008078:Cholesterol, LDL / Q000097:blood; D006801:Humans; D006937:Hypercholesterolemia / Q000188:drug therapy*; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases / Q000037:antagonists & inhibitors*; D012697:Serine Endopeptidases
chemical_list: D000911:Antibodies, Monoclonal; D061067:Antibodies, Monoclonal, Humanized; D008078:Cholesterol, LDL; C472125:PCSK9 protein, human; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases; D012697:Serine Endopeptidases; C571059:alirocumab
keywords: Alirocumab; Cardiovascular risk; Hypercholesterolemia; LDL cholesterol; Monoclonal antibody; PCSK9; SAR-236553/REGN-727