title: [Lipid-lowering drugs and PCSK9].
abstract: PCSK9 is a protease, synthesized mainly in the liver, which promotes the hepatic degradation of the LDL receptor and consequently decreases LDL receptor density and clearance of LDL particles. Statins inhibit HMG-CoA-reductase activity, an enzyme that catalyses an important step in hepatic cholesterol biosynthesis. The decrease of the hepatic intracellular cholesterol pool produced by these drugs upregulates the activity of the SREBP2 transcription factor, which subsequently stimulates the expression of the LDL receptor gene, an effect that is followed by an increase in the serum concentration of PCSK9. This article aims to review the effects of different lipid-lowering drugs on plasma PCSK9 concentrations. Overall, statins increase blood PCSK9 levels, an effect that is enhanced by ezetimibe. In contrast, others drugs, such as fibrates and niacin, could decrease PCSK9 levels.
authors.affiliation: Unidad de Lípidos y Riesgo Vascular, Hospital General Universitario Gregorio Marañón, Madrid, España. Electronic address: jesus.millan@salud.madrid.org.
authors.forename: Jesús
authors.initials: J
authors.lastname: Millán Núñez-Cortés
authors.affiliation: Unidad de Lípidos, Servicio de Medicina Interna, Hospital Carlos III, Madrid, España.
authors.forename: José M
authors.initials: JM
authors.lastname: Mostaza Prieto
mesh_terms: D002784:Cholesterol / Q000378:metabolism; D000069438:Ezetimibe / Q000494:pharmacology; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000494:pharmacology*; D008099:Liver / Q000378:metabolism; D000071449:Proprotein Convertase 9 / Q000097:blood / Q000378:metabolism*; D011973:Receptors, LDL / Q000235:genetics / Q000378:metabolism*; D051782:Sterol Regulatory Element Binding Protein 2 / Q000378:metabolism
chemical_list: D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D000960:Hypolipidemic Agents; D011973:Receptors, LDL; C497390:SREBF2 protein, human; D051782:Sterol Regulatory Element Binding Protein 2; D002784:Cholesterol; C472125:PCSK9 protein, human; D000071449:Proprotein Convertase 9; D000069438:Ezetimibe
keywords: Estatinas; Fibrates; Fibratos; Fármacos; Lipid-lowering drugs; PCSK9; Statins; hipolipemiantes