Bezafibrate
| Systematic (IUPAC) name | |
|---|---|
| 2-(4-{2-[(4-chlorobenzoyl)amino]ethyl}phenoxy)-2-methylpropanoic acid | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a682711 |
| Pregnancy cat. | ? |
| Legal status | POM (UK) ℞-only (US) |
| Routes | Oral |
| Identifiers | |
| CAS number | 41859-67-0 |
| ATC code | C10AB02 |
| PubChem | CID 39042 |
| DrugBank | DB01393 |
| ChemSpider | 35728 |
| UNII | Y9449Q51XH |
| KEGG | D01366 |
| ChEBI | CHEBI:47612 |
| ChEMBL | CHEMBL264374 |
| Chemical data | |
| Formula | C19H20ClNO4 |
| Mol. mass | 361.819 g/mol |
| SMILES | eMolecules & PubChem |
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Bezafibrate (marketed as Bezalip and various other brand names) is a fibrate drug used for the treatment of hyperlipidaemia. It helps to lower LDL cholesterol and triglyceride in the blood, and increase HDL.
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[edit] History
Bezafibrate was first introduced by Boehringer Mannheim in 1977.
[edit] Mode of action
Like the other fibrates, bezafibrate is an agonist of PPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well.
[edit] Uses
Bezafibrate improves markers of combined hyperlipidemia, effectively reducing LDL and triglycerides and improving HDL levels.[1] The main effect on cardiovascular morbidity is in patients with the metabolic syndrome, the features of which are attenuated by bezafibrate.[2] Studies show that in patients with impaired glucose tolerance, bezafibrate may delay progress to diabetes[3], and in those with insulin resistance it slowed progress in the HOMA severity marker.[4]
[edit] Side-effects
The main toxicity is hepatic (abnormal liver enzymes), and myopathy and rarely rhabdomyolysis have been reported.
[edit] Other uses
The Australian biotech company Giaconda combines bezafibrate with chenodeoxycholic acid in an anti-hepatitis C drug combination called Hepaconda.
[edit] References
- ^ "Secondary prevention by raising HDL cholesterol and reducing triglycerides in patients with coronary artery disease: the Bezafibrate Infarction Prevention (BIP) study". Circulation 102 (1): 21–7. 2000. PMID 10880410.
- ^ Tenenbaum, A; Motro, M; Fisman, EZ; Tanne, D; Boyko, V; Behar, S (2005). "Bezafibrate for the secondary prevention of myocardial infarction in patients with metabolic syndrome". Archives of internal medicine 165 (10): 1154–60. doi:10.1001/archinte.165.10.1154. PMID 15911729.
- ^ Tenenbaum, A; Motro, M; Fisman, EZ; Schwammenthal, E; Adler, Y; Goldenberg, I; Leor, J; Boyko, V et al (2004). "Peroxisome proliferator-activated receptor ligand bezafibrate for prevention of type 2 diabetes mellitus in patients with coronary artery disease". Circulation 109 (18): 2197–202. doi:10.1161/01.CIR.0000126824.12785.B6. PMID 15123532.
- ^ Tenenbaum, A; Fisman, EZ; Boyko, V; Benderly, M; Tanne, D; Haim, M; Matas, Z; Motro, M et al (2006). "Attenuation of progression of insulin resistance in patients with coronary artery disease by bezafibrate". Archives of internal medicine 166 (7): 737–41. doi:10.1001/archinte.166.7.737. PMID 16606809.
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