title: New therapeutic principles in dyslipidaemia: focus on LDL and Lp(a) lowering drugs.
abstract: Dyslipidaemias play a key role in determining cardiovascular risk; the discovery of statins has contributed a very effective approach. However, many patients do not achieve, at the maximal tolerated dose, the recommended goals for low-density lipoprotein-cholesterol (LDL-C), non-high-density lipoprotein-cholesterol, and apolipoprotein B (apoB). Available agents combined with statins can provide additional LDL-C reduction, and agents in development will increase therapeutic options impacting also other atherogenic lipoprotein classes. In fact, genetic insights into mechanisms underlying regulation of LDL-C levels has expanded potential targets of drug therapy and led to the development of novel agents. Among them are modulators of apoB containing lipoproteins production and proprotein convertase subtilisin/kexin type-9 inhibitors. Alternative targets such as lipoprotein(a) also require attention; however, until we have a better understanding of these issues, further LDL-C lowering in high and very high-risk patients will represent the most sound clinical approach.
authors.affiliation: Department of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Via Balzaretti 9, 20133 Milan, Italy. danilo.norata@unimi.it
authors.forename: Giuseppe Danilo
authors.initials: GD
authors.lastname: Norata
authors.forename: Christie M
authors.initials: CM
authors.lastname: Ballantyne
authors.forename: Alberico Luigi
authors.initials: AL
authors.lastname: Catapano
mesh_terms: D001384:Azetidines / Q000627:therapeutic use; D001562:Benzimidazoles / Q000627:therapeutic use; D001569:Benzodiazepines / Q000627:therapeutic use; D002352:Carrier Proteins / Q000037:antagonists & inhibitors; D008078:Cholesterol, LDL / Q000037:antagonists & inhibitors / Q000187:drug effects*; D003998:Dicarboxylic Acids / Q000627:therapeutic use; D050171:Dyslipidemias / Q000188:drug therapy*; D000069438:Ezetimibe; D005227:Fatty Acids / Q000627:therapeutic use; D006801:Humans; D000960:Hypolipidemic Agents / Q000627:therapeutic use*; D017270:Lipoprotein(a) / Q000037:antagonists & inhibitors / Q000187:drug effects*; D009841:Oligonucleotides / Q000627:therapeutic use; D023303:Oxazolidinones / Q000627:therapeutic use; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases / Q000037:antagonists & inhibitors; D012697:Serine Endopeptidases
chemical_list: D001384:Azetidines; C473731:BMS201038; D001562:Benzimidazoles; D002352:Carrier Proteins; D008078:Cholesterol, LDL; D003998:Dicarboxylic Acids; D005227:Fatty Acids; D000960:Hypolipidemic Agents; D017270:Lipoprotein(a); D009841:Oligonucleotides; D023303:Oxazolidinones; C106092:microsomal triglyceride transfer protein; D001569:Benzodiazepines; C581236:8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid; C568301:evacetrapib; C524142:mipomersen; C472125:PCSK9 protein, human; D000071449:Proprotein Convertase 9; D043484:Proprotein Convertases; D012697:Serine Endopeptidases; D000069438:Ezetimibe; C530884:anacetrapib
keywords: Apolipoprotein B; Dyslipidaemia; PCSK9; Pharmacology