Clofibrate

Clofibrate

File:Clofibrate.svg
Systematic (IUPAC) name
ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy category	AU: B1 US: C (Risk not ruled out)
Legal status	US: Discontinued
Routes of administration	Oral
Pharmacokinetic data
Protein binding	Variable, 92–97% at therapeutic concentrations
Metabolism	Hydrolyzed to clofibric acid; hepatic glucuronidation
Biological half-life	Highly variable; average 18–22 hours. Prolonged in renal failure
Excretion	Renal, 95 to 99%
Identifiers
CAS Number	637-07-0 Y
ATC code	C10AB01 (WHO)
PubChem	CID: 2796
IUPHAR/BPS	2667
DrugBank	DB00636 Y
ChemSpider	2694 Y
UNII	HPN91K7FU3 Y
KEGG	D00279 Y
ChEBI	CHEBI:3750 Y
ChEMBL	CHEMBL565 Y
Chemical data
Formula	C12H15ClO3
Molecular mass	242.698 g/mol
SMILES Clc1ccc(OC(C(=O)OCC)(C)C)cc1
InChI InChI=1S/C12H15ClO3/c1-4-15-11(14)12(2,3)16-10-7-5-9(13)6-8-10/h5-8H,4H2,1-3H3 Y Key:KNHUKKLJHYUCFP-UHFFFAOYSA-N Y
Physical data
Boiling point	148 °C (298 °F)
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Clofibrate (tradename Atromid-S) is an organic compound. It is marketed as a fibrate. It is a lipid-lowering agent used for controlling the high cholesterol and triacylglyceride level in the blood. It increases lipoprotein lipase activity to promote the conversion of VLDL to LDL, and hence reduce the level of VLDL. It can increase the level of HDL as well.

Complications and controversies

It can induce SIADH, syndrome of inappropriate secretion of antidiuretic hormone ADH (vasopressin). Clofibrate can also result in formation of cholesterol stones in the gallbladder.

The World Health Organization Cooperative Trial on Primary Prevention of Ischaemic Heart Disease using clofibrate to lower serum cholesterol observed excess mortality in the clofibrate-treated group despite successful cholesterol lowering (47% more deaths during treatment with clofibrate and 5% after treatment with clofibrate) than the non-treated high cholesterol group. These deaths were due to a wide variety of causes other than heart disease, and remain "unexplained".

Clofibrate was discontinued in 2002 due to adverse effects.