Bezafibrate

Systematic (IUPAC) name
2-(4-{2-[(4-chlorobenzoyl)amino]ethyl}phenoxy)-2-methylpropanoic acid
Identifiers
CAS number	41859-67-0
ATC code	C10AB02
PubChem	39042
ChemSpider	35728
Chemical data
Formula	C19H20ClNO4
Mol. mass	361.819 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status	POM(UK) ℞-only(US)
Routes	Oral
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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.

Contents 1 History 2 Mode of action 3 Uses 4 Side-effects 5 Other uses 6 References

[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 2000;102:21-7. PMID 10880410.
2. ^ Tenenbaum A, Motro M, Fisman EZ, Tanne D, Boyko V, Behar S. Bezafibrate for the secondary prevention of myocardial infarction in patients with metabolic syndrome. Arch Intern Med 2005;165:1154-60. PMID 15911729.
3. ^ Tenenbaum A, Motro M, Fisman EZ, Schwammenthal E, Adler Y, Goldenberg I, Leor J, Boyko V, Mandelzweig L, Behar S. Peroxisome proliferator-activated receptor ligand bezafibrate for prevention of type 2 diabetes mellitus in patients with coronary artery disease. Circulation 2004;109:2197-202. PMID 15123532
4. ^ Tenenbaum A, Fisman EZ, Boyko V, Benderly M, Tanne D, Haim M, Matas Z, Motro M, Behar S. Attenuation of progression of insulin resistance in patients with coronary artery disease by bezafibrate. Arch Intern Med 2006;166:737-41. PMID 16606809.

v • d • e Lipid modifying agents (C10) GI tract Cholesterol absorption inhibitor, NPC1L1 Ezetimibe • SCH-48461 Bile acid sequestrants/resins (LDL) Cholestyramine • Colestipol • Colestilan • Colextran • Colesevelam Liver Statins (HMG-CoA reductase, LDL) Simvastatin# • Atorvastatin • Fluvastatin • Lovastatin • Mevastatin • Pitavastatin • Pravastatin • Rosuvastatin • Cerivastatin‡ Niacin and derivatives (HDL and LDL) Niceritrol • Niacin • Nicofuranose • Aluminium nicotinate • Nicotinyl alcohol • Acipimox Blood vessels Fibrates (PPAR) Clofibrate‡ • Bezafibrate • Aluminium clofibrate • Gemfibrozil • Fenofibrate • Simfibrate • Ronifibrate • Ciprofibrate • Etofibrate • Clofibride • Clinofibrate CETP inhibitors (HDL) Anacetrapib† • Torcetrapib§ • JTT-705 Combinations Niacin/lovastatin • Niacin/simvastatin • Ezetimibe/simvastatin • Niacin/laropiprant Other Dextrothyroxine • Probucol • Tiadenol • Benfluorex • Meglutol • Omega-3-triglycerides • Magnesium pyridoxal 5-phosphate glutamate • Policosanol • Lapaquistat§ • Alipogene tiparvovec #WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III