For research use only.
Catalog No.S1729 Synonyms: CI-719
CAS No. 25812-30-0
Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
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|Description||Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.|
Gemfibrozil exerts a minimal inhibitory effect on CYP3A-mediated simvastatin hydroxy acid (SVA) oxidation, but does inhibit SVA glucuronidation in dog and human liver microsomes.  Gemfibrozil markedly inhibits M-23 formation, with a K(i) (IC(50)) value of 69 (95) mM, whereas inhibition of M-1 formation is weaker with a K(i) (IC(50)) value of 273 mM in human liver microsomes.  Gemfibrozil strongly and competitively inhibits CYP2C9 activity, with a K(i) (IC(50)) value of 5.8 (9.6) mM. Gemfibrozil exhibits somewhat smaller inhibitory effects on CYP2C19 and CYP1A2 activities, with K(i) (IC(50)) values of 24 (47) mM and 82 (136) mM, respectively.  Gemfibrozil, a lipid-lowering drug, inhibits cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373MG astroglial cells and primary astrocytes. Gemfibrozil induces peroxisome proliferator-responsive element (PPRE)-dependent luciferase activity, which is inhibited by the expression of DeltahPPAR-alpha, the dominant-negative mutant of human PPAR-alpha. Gemfibrozil strongly inhibits the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of gamma-activation site (GAS) in cytokine-stimulated astroglial cells. 
|In vivo||Gemfibrozil treatment significantly reduces (2-3-fold) the plasma clearance of SVA and the biliary excretion of SVA glucuronide (together with its cyclization product SV), but not the excretion of a major oxidative metabolite of SVA in dogs. |
|In vitro||DMSO||50 mg/mL (199.73 mM)|
|Ethanol||50 mg/mL (199.73 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03832595||Enrolling by invitation||Other: Intervention Arm|Other: Usual Care||Chronic Kidney Diseases||University of Pittsburgh|Vanderbilt University Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)||May 1 2019||Not Applicable|
|NCT01736254||Completed||Drug: Evacetrapib|Drug: Gemfibrozil||Healthy Volunteers||Eli Lilly and Company||December 2012||Phase 1|
|NCT01797198||Completed||Drug: ASP3652|Drug: Gemfibrozil|Drug: Repaglinide||Drug-Drug Interaction (DDI)|Healthy Subjects||Astellas Pharma Europe B.V.|Astellas Pharma Inc||April 2012||Phase 1|
|NCT01913379||Completed||Drug: MDV3100|Drug: Gemfibrozil|Drug: Itraconazole||Healthy Subjects|Pharmacokinetics|Drug-Drug Interaction||Astellas Pharma Europe B.V.|Medivation Inc.|Astellas Pharma Inc||August 2011||Phase 1|
|NCT01083212||Completed||Drug: AZD1656|Drug: Gemfibrozil|Drug: Placebo||Type 2 Diabetes Mellitus||AstraZeneca||March 2010||Phase 1|
|NCT00566865||Completed||Drug: placebo for gemfibrozil|Drug: gemfibrozil||Type 2 Diabetes Mellitus||Elixir Pharmaceuticals||November 2007||Phase 1|
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