Clofibrate

Clofibrate (trade name Atromid-S) is a lipid-lowering agent used for controlling the high cholesterol and triacylglyceride level in the blood. It belongs to the class of fibrates. 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.

Clofibrate
Clinical data
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Pregnancy
category
  • AU: B1
  • US: C (Risk not ruled out)
    Routes of
    administration    		By mouth
    ATC code
    Legal status
    Legal status
    • US: Discontinued
    Pharmacokinetic data
    Protein bindingVariable, 92–97% at therapeutic concentrations
    MetabolismHydrolyzed to clofibric acid; hepatic glucuronidation
    Elimination half-lifeHighly variable; average 18–22 hours. Prolonged in renal failure
    ExcretionRenal, 95 to 99%
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.010.253
    Chemical and physical data
    FormulaC12H15ClO3
    Molar mass242.70 g·mol−1
    3D model (JSmol)
    Boiling point148 °C (298 °F)
      (verify)

    It was patented in 1958 by Imperial Chemical Industries and approved for medical use in 1963.[1] Clofibrate was discontinued in 2002 due to adverse effects.

    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".[2]

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    References
    1. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 474. ISBN 9783527607495.
    2. "WHO cooperative trial on primary prevention of ischaemic heart disease with clofibrate to lower serum cholesterol: final mortality follow-up. Report of the Committee of Principal Investigators". Lancet. 2 (8403): 600–4. September 1984. doi:10.1016/s0140-6736(84)90595-6. PMID 6147641.
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