Gemfibrozil 1-O-β-Glucuronide

Gemfibrozil 1-O-β-Glucuronide is a metabolite of Gemfibrozil which irreversibly inhibits CYP2C8 (P450 2C8) in vitro. Studies indicate that the heme group of CYP2C8 (P450 2C8) binds to the benzylic carbon on the 2',5'-dimethylphenoxy group of Gemfibrozil 1-O-β-Glucuronide in a regiospecific way. In addition, Gemfibrozil 1-O-β-Glucuronide can be oxidized to a benzyl radical intermediate which binds to the γ-meso position of heme. Alternate studies indicate that it inhibits the formation of the montelukast metabolite M6 in liver microsomes. It is known that Gemfibrozil amplifies the activity of Peroxisome proliferator-activated receptor-alpha (PPARα), which increases the synthesis of lipoprotein lipase resulting in a decrease in the number of triglycerides.