Gemfibrozil

Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Gemfibrozil is a peroxisome proliferator-activated receptor α (PPARα) and PPARγ agonist (EC50s = 193.3 and 147.8 μM, respectively, in transactivation assays).In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia. Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) inApoE-/-mice. Formulations containing gemfibrozil have been used in the treatment of high cholesterol.
White Crystalline Powder
ChEBI: Gemfibrozil is an aromatic ether. It has a role as an antilipemic drug. It is functionally related to a valeric acid.
Gemfibrozil, 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid (Lopid), is a congener of clofibratethat was used first in the treatment of hyperlipoproteinemia inthe mid-1970s. Its mechanism of action and use are similar tothose of clofibrate. Gemfibrozil reduces plasma levels ofVLDL triglycerides and stimulates clearance of VLDL fromplasma. The drug has little effect on cholesterol plasma levelsbut does cause an increase of HDL.Gemfibrozil is absorbed quickly from the gut and excretedunchanged in the urine. The drug has a plasma half-life of1.5 hours, but reduction of plasma VLDL concentration takesbetween 2 and 5 days to become evident. The peak effect of its hypolipidemic action may take up to 4 weeks to becomemanifest.