Gemfibrozil is a fibrate that activates peroxisome proliferator-activator α (PPARα, EC50 = 193 μM) with 100% efficacy. It also activates PPARγ (EC50 = 148 μM), but with only 79% efficacy. Presumably through its effects on PPARα, gemfibrozil lowers triglycerides and increases high density lipoprotein cholesterol levels and is used in the context of atherogenic dyslipidemia. Gemfibrozil strongly binds liver fatty acid-binding protein (Ki = 1.8 μM). Phase II metabolites of gemfibrozil inhibit certain cytochrome P450 isoforms, increasing drug-drug interaction risks.
