title: Monoclonal Antibodies for Lipid Management.
abstract: In recent years, biochemical and genetic studies have identified proprotein convertase subtilisin/kexin type 9 (PCSK9) as a major mediator of low-density lipoprotein cholesterol (LDL-c) levels and thereby a potential novel target for reducing risk of coronary heart disease (CHD). These observations led to the development of PCSK9 inhibitors, which lower LDL-c levels more than any other non-invasive lipid-lowering therapy presently available. The PCSK9 inhibitors furthest along in clinical trials are subcutaneously injected monoclonal antibodies. These PCSK9 inhibitors have demonstrated LDL-c-lowering efficacy with acceptable safety in phase III clinical trials and may offer a useful therapy in addition to maximally tolerated HMG-CoA reductase inhibitors (statins) in certain patient groups. Longer-term data are required to ensure sustained efficacy and safety of this new class of medications. This review provides an overview of the biology, genetics, development, and clinical trials of monoclonal antibodies designed to inhibit PCSK9.
authors.affiliation: Division of Cardiovascular Diseases, Department of Medicine, Northwestern University Feinberg School of Medicine, Chicago, IL, USA.|Department of Preventive Medicine, Northwestern University Feinberg School of Medicine, Chicago, IL, USA.
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Feinstein
authors.affiliation: Division of Cardiovascular Diseases, Department of Medicine, Northwestern University Feinberg School of Medicine, Chicago, IL, USA. dlj@northwestern.edu.|Department of Preventive Medicine, Northwestern University Feinberg School of Medicine, Chicago, IL, USA. dlj@northwestern.edu.
authors.forename: Donald M
authors.initials: DM
authors.lastname: Lloyd-Jones
mesh_terms: D000818:Animals; D000911:Antibodies, Monoclonal / Q000627:therapeutic use*; D002784:Cholesterol / Q000378:metabolism; D002986:Clinical Trials as Topic; D003327:Coronary Disease / Q000517:prevention & control; D006801:Humans; D050356:Lipid Metabolism / Q000187:drug effects*; D000091362:PCSK9 Inhibitors; D000071449:Proprotein Convertase 9 / Q000235:genetics / Q000378:metabolism
chemical_list: D000911:Antibodies, Monoclonal; D000091362:PCSK9 Inhibitors; D002784:Cholesterol; C472125:PCSK9 protein, human; D000071449:Proprotein Convertase 9
keywords: Cholesterol; Coronary heart disease; LDL cholesterol; PCSK9; Statins