Bezafibrate
Chemical compound
From Wikipedia, the free encyclopedia
Bezafibrate (marketed as Bezalip and various other brand names) is a fibrate drug used as a lipid-lowering agent to treat hyperlipidaemia. It helps to lower LDL cholesterol and triglyceride in the blood, and increase HDL.
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| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a682711 |
| Routes of administration | Oral |
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| ECHA InfoCard | 100.050.498 |
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| Formula | C19H20ClNO4 |
| Molar mass | 361.82 g·mol−1 |
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It was patented in 1971 and approved for medical use in 1978.[1]
Medical uses
Bezafibrate improves markers of combined hyperlipidemia, effectively reducing LDL and triglycerides and improving HDL levels.[2] The main effect on cardiovascular morbidity is in patients with the metabolic syndrome, the features of which are attenuated by bezafibrate.[3] Studies show that in patients with impaired glucose tolerance, bezafibrate may delay progress to diabetes,[4] and in those with insulin resistance it slowed progress in the HOMA severity marker.[5] In addition, a prospective observational study of dyslipidemic patients with diabetes or hyperglycemia showed that bezafibrate significantly reduces haemoglobin A1c (HbA1c) concentration as a function of baseline HbA1c levels, regardless of concurrent use of antidiabetic drugs.[6]
Side effects
The main toxicity is hepatic (abnormal liver enzymes); myopathy and on rare occasions rhabdomyolysis have been reported.
Other uses
The Australian biotech company Giaconda combines bezafibrate with chenodeoxycholic acid in an anti-hepatitis C drug combination called Hepaconda.
Bezafibrate has been shown to reduce tau protein hyperphosphorylation and other signs of tauopathy in transgenic mice having human tau mutation.[7]
The combination of a cholesterol-lowering drug, bezafibrate, and a contraceptive steroid, medroxyprogesterone acetate, could be an effective, non-toxic treatment for a range of cancers, researchers at the University of Birmingham have found.[8]
Mode of action
Synthesis
Further evidence that substantial bulk tolerance is available in the para position is given by the lipid lowering agent bezafibrate.
The p-chlorobenzamide of tyramine undergoes a Williamson ether synthesis with ethyl 2-bromo-2-methylpropionate to complete the synthesis. The ester group is hydrolyzed in the alkaline reaction medium.
History
Bezafibrate was first introduced by Boehringer Mannheim in 1977.