Bezafibrate

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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 YesY
UNII Y9449Q51XH YesY
KEGG D01366 YesY
ChEBI CHEBI:47612 YesY
ChEMBL CHEMBL264374 YesY
Chemical data
Formula C19H20ClNO4 
Mol. mass 361.819 g/mol
SMILES eMolecules & PubChem
 YesY (what is this?)  (verify)

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.

Contents

[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

  1. ^ "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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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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