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Description: A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. These decreases occur primarily in the VLDL fraction and less frequently in the LDL fraction. Gemfibrozil increases HDL subfractions HDL2 and HDL3 as well as apolipoproteins A-I and A-II. Its mechanism of action has not been definitely established. [PubChem]
Drug Type: Small Molecule; Approved
Pharmacology: Gemfibrozil, a fibric acid antilipemic agent similar to clofibrate, is used to treat hyperlipoproteinemia and as a second-line therapy for type IIb hypercholesterolemia. It acts to reduce triglyceride levels, reduce VLDL levels, reduce LDL levels (moderately), and increase HDL levels (moderately).
Mechanism of Action: Gemfibrozil 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. Gemfibrozil also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL.
Indication: For treatment of adult patients with very high elevations of serum triglyceride levels (types IV and V hyperlipidemia) who are at risk of developing pancreatitis (inflammation of the pancreas) and who do not respond adequately to a strict diet.
Half Life: 1.5 hours
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Data Correlations | 6 studies

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Genes category icon Genes
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LPL 100 100
545481 100 100
STAC3 94 94
CIDEA 90 90
ELOVL6 83 83
NR1D2 83 83
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Biogroups category icon Biogroups
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PPAR Signaling Pathway 100 100
Propanoate Metabolism 99 99
Glycerolipid Metabolism 98 98
Alpha/beta hydrolase fold-1 98 98
Bile Acid Biosynthesis 98 98
Nuclear Receptors 98 98
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Individual Studies

  • Drug-Induced Renal Tubular Toxicity

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    These data support the publication titled "A Gene Expression Signature that Predicts the Future Onset of Drug-Induced Renal Tubular Toxicity"

    Authors: Fielden MR, Eynon BP, Natsoulis G et al.

    Organization: Iconix Pharmaceuticals 325 E Middlefield…

  • Drug target sets for approved compounds

    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…
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Associated Researchers

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Thought leaders and organizations working on research involving gemfibrozil.

View All Author iconAuthors
  • Dorothea Collins
  • Pertti J Neuvonen
  • Janne T Backman
  • Sander J Robins
  • Aleksi Tornio
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • National Heart, Lung, and Blood Institute (NHLBI)
  • National Institute of Diabetes and Digestive and Kidney Diseases (NIDD…
  • National Institutes of Health Clinical Center (CC)
  • Department of Veterans Affairs
  • Stanford University
View All Affiliations icon Organizations
  • University of Helsinki and Helsinki University Central Hospital
  • Helsinki University Central Hospital
  • Center for Chronic Disease Outcomes Research
  • Rush University Medical Center
  • Baker Heart Research Institute

Clinical Trials | 105 trials

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