Drug intelligence / Profile preview

gemfibrozil

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Gemfibrozil is an oral lipid-regulating agent in the fibrate class used to reduce serum triglycerides and cholesterol levels. It is primarily indicated for patients with very high triglyceride levels (Types IV and V hyperlipidemia), especially those at risk of pancreatitis who do not respond adequately to dietary therapy. Gemfibrozil is also used in patients with combined low HDL ("good cholesterol"), high LDL ("bad cholesterol"), and elevated triglycerides to reduce the risk of coronary heart disease when other interventions have failed[1][3][4][5]. Its mechanism of action involves activation of peroxisome proliferator-activated receptor-alpha (PPARα), leading to increased activity of lipoprotein lipase (LPL), enhanced peripheral lipolysis, decreased hepatic extraction of free fatty acids, reduced production and increased clearance of very-low-density lipoprotein (VLDL), inhibition of apolipoprotein B synthesis, and increased HDL subfractions[4][5]. The drug has been shown in clinical trials such as the Helsinki Heart Study to significantly lower the incidence of coronary heart disease events in dyslipidemic men[7][10].

Brand names
Lopid
Other names
2,2-dimethyl-5-(2,5-dimethylphenoxy)pentanoic acid2,2-dimethyl-5-(2,5-xylyloxy)valeric acidgemfibrozilum
02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)

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