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.
Keywords:
Apolipoprotein B; Dyslipidaemia; PCSK9; Pharmacology.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
-
Review
MeSH terms
-
Azetidines / therapeutic use
-
Benzimidazoles / therapeutic use
-
Benzodiazepines / therapeutic use
-
Carrier Proteins / antagonists & inhibitors
-
Cholesterol, LDL / antagonists & inhibitors
-
Cholesterol, LDL / drug effects*
-
Dicarboxylic Acids / therapeutic use
-
Dyslipidemias / drug therapy*
-
Ezetimibe
-
Fatty Acids / therapeutic use
-
Humans
-
Hypolipidemic Agents / therapeutic use*
-
Lipoprotein(a) / antagonists & inhibitors
-
Lipoprotein(a) / drug effects*
-
Oligonucleotides / therapeutic use
-
Oxazolidinones / therapeutic use
-
Proprotein Convertase 9
-
Proprotein Convertases / antagonists & inhibitors
-
Serine Endopeptidases
Substances
-
Azetidines
-
BMS201038
-
Benzimidazoles
-
Carrier Proteins
-
Cholesterol, LDL
-
Dicarboxylic Acids
-
Fatty Acids
-
Hypolipidemic Agents
-
Lipoprotein(a)
-
Oligonucleotides
-
Oxazolidinones
-
microsomal triglyceride transfer protein
-
Benzodiazepines
-
8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
-
evacetrapib
-
mipomersen
-
PCSK9 protein, human
-
Proprotein Convertase 9
-
Proprotein Convertases
-
Serine Endopeptidases
-
Ezetimibe
-
anacetrapib