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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 |
| Chemical and physical data | |
| Formula | C19H20ClNO4 |
| Molar mass | 361.82 g·mol−1 |
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Bezafibrate (marketed asBezalip and various other brand names) is afibratedrug used as alipid-lowering agent to treathyperlipidaemia. It helps to lowerLDL cholesterol andtriglyceride in theblood, and increaseHDL.
It was patented in 1971 and approved for medical use in 1978.[1]
Bezafibrate improves markers ofcombined hyperlipidemia, effectively reducing LDL and triglycerides and improving HDL levels.[2] The main effect on cardiovascular morbidity is in patients with themetabolic 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 withinsulin resistance it slowed progress in theHOMA 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]
The main toxicity ishepatic (abnormal liver enzymes);myopathy and on rare occasionsrhabdomyolysis have been reported.
The Australian biotech companyGiaconda combines bezafibrate withchenodeoxycholic acid in an anti-hepatitis C drug combination called Hepaconda.
Bezafibrate has been shown to reducetau proteinhyperphosphorylation and other signs oftauopathy intransgenic mice having human taumutation.[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]
Like the other fibrates, bezafibrate is an agonist ofPPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well.[9]
Further evidence that substantial bulk tolerance is available in the para position is given by the lipid lowering agent bezafibrate.
Thep-chlorobenzamide oftyramine undergoes aWilliamson ether synthesis with ethyl 2-bromo-2-methylpropionate to complete the synthesis. The ester group is hydrolyzed in the alkaline reaction medium.
Bezafibrate was first introduced byBoehringer Mannheim in 1977.
