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Update on the use of fibrates: focus on bezafibrate
Ilan Goldenberg1, Michal Benderly, Uri Goldbourt
1Heart Institute, Shiba Medical Center Tel Hashomer, Israel. ilan.goldenberg@heart.rochester.edu
Insights
Fibrates effectively treat high triglycerides and low HDL-C, improving cardiovascular health. This review details their mechanisms and clinical trial efficacy for dyslipidemia.
Area of Science:
- Cardiovascular Medicine
- Lipid Metabolism
- Pharmacology
Background:
- Low-density lipoprotein-cholesterol (LDL-C) is a known coronary heart disease (CHD) risk factor, but its predictive ability is limited.
- Elevated triglycerides with low high-density lipoprotein-cholesterol (HDL-C) dyslipidemia is a significant cardiovascular risk factor, independent of LDL-C.
- Fibric acid derivatives (fibrates) have been used for over two decades to manage dyslipidemia.
Purpose of the Study:
- To review the mechanism of action and metabolic effects of fibrates.
- To summarize clinical trial data on the efficacy of fibrate therapy for dyslipidemia.
- To detail findings from the Bezafibrate Infarction Prevention trial.
Main Methods:
- Review of existing literature on fibrate mechanisms and clinical trials.
- Analysis of data from primary and secondary prevention trials.
- Examination of subgroup analyses from the Bezafibrate Infarction Prevention trial.
Main Results:
- Fibrates decrease triglyceride levels and increase HDL-C levels.
- Fibrates impact apolipoprotein synthesis, lipoprotein metabolism, fibrinolysis, and inflammation via PPARα.
- Clinical trials demonstrate fibrate efficacy in patients with raised triglycerides-low HDL-C dyslipidemia.
Conclusions:
- Fibrates are effective in managing dyslipidemia characterized by high triglycerides and low HDL-C.
- Fibrate therapy offers significant metabolic and long-term cardiovascular benefits.
- Bezafibrate therapy shows promising metabolic and cardiovascular effects.
Abstract:
Low-density lipoprotein-cholesterol (LDL-C) is a well established coronary heart disease (CHD) risk factor. However, the ability of this metabolic risk factor alone to identify individuals at rigk for future CHD events is limited. The raised triglycerides-low high-density lipoprotein-cholesterol (HDL-C) dyslipidaemia was shown to be an important cardiovascular risk factor independently of LDL-C levels. Fibric acid derivatives (fibrates) have been used in clinical practice for more than 2 decades as a class of agents known to decrease triglyceride levels while substantially increasing HDL-C levels. Through peroxisome proliferator-activated alpha-receptors, fibrates have a significant impact on the synthesis of several apolipoproteins and enzymes of lipoprotein metabolism as well as on the expression of several genes involved in fibrinolysis and inflammation. Data from recent primary and secondary prevention clinical trials demonstrate the efficacy of fibrate therapy in patients with the raised triglycerides-low HDL-C dyslipidaemia. This review summarizes current data regarding mechanism of action and the metbolic effects of fibrates, as well as results from major clinical trials on the efficacy of this mode of lipid lowering therapy. In addition, recent data from subgroup analyses of the Bezafibrate Infarction Prevention trial, demonstrating several important metabolic and long-term cardiovascular effects of bezafibrate therapy, are detailed.
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