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Description: A fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
Drug Type: Small Molecule; Approved
Pharmacology: Clofibrate is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction (Sf 20-400) rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III hyperlipoproteinemia. Several investigators have observed in their studies that clofibrate may produce a decrease in cholesterol linoleate but an increase in palmitoleate and oleate, the latter being considered atherogenic in experimental animals. The significance of this finding is unknown at this time. Reduction of triglycerides in some patients treated with clofibrate or certain of its chemically and clinically similar analogs may be associated with an increase in LDL cholesterol. Increase in LDL cholesterol has been observed in patients whose cholesterol is initially normal. Animal studies suggest that clofibrate interrupts cholesterol biosynthesis prior to mevalonate formation.
Mechanism of Action: Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Clofibrate also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL.
Indication: For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet.
Half Life: Half-life in normal volunteers averages 18 to 22 hours (range 14 to 35 hours) but can vary by up to 7 hours in the same subject at different times.
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Individual Studies
  • Rat liver response to Clofibrate,Valproate and Diethylhexyl phthalate

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    The project had 2 goals: 1) To evaluate the transcriptional response of 3 prototypical toxicants (Clofibrate, VPA, and DEHP) on rat lever. 2) To evaluate the impact pooling samples has on data analysis.

    Authors: Jolly RA, Goldstein KM, Wei T et al.

    Organization: Eli Lilly & Co. Integrative Biology 2001…

  • Time-course of rat liver response to prototypical toxicants

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    Transcription profiling of rat liver pooled vs. individual samplesf rom a single-dose time-course rat study in response to the prototypical toxicants Clofibrate, Diethylhexyl phthalate, and valproic acid,

    Source: NextBio Library/Pharmacology and Toxicology

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Thought leaders and organizations working on research involving Clofibrate.

  • Wei-Qun Ding
  • Michael J Santostefano
  • Doris M Benbrook
  • José E Manautou
  • Antonella Trombetta
  • National Heart, Lung, and Blood Institute (NHLBI)
  • Christiana Care Health Services
  • Biovail Laboratories International SRL
  • Department of Veterans Affairs
  • University of Pennsylvania
  • University of Connecticut
  • Martin-Luther-University Halle-Wittenberg
  • Medical College of Georgia
  • University of Oklahoma Health Sciences Center
  • Università di Torino
  • Coronary Drug Project

    conditions: Cardiovascular Diseases ; Coronary Disease ; Heart Diseases ; Myocardial Infarction ; Myocardial Ischemia

    interventions: estrogen ; clofibrate clofibrate ; dextrothyroxine sodium ; niacin

  • Coronary Drug Project Mortality Surveillance

    conditions: Cardiovascular Diseases ; Coronary Disease ; Heart Diseases ; Myocardial Infarction ; Myocardial Ischemia

    interventions: estrogen ; clofibrate ; dextrothyroxine sodium ; niacin

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