Skip to main content

Table 1 PPAR agonists and their treatment of type II diabetes and obesity

From: Applications of metabolomics for understanding the action of peroxisome proliferator-activated receptors (PPARs) in diabetes, obesity and cancer

Drug class Target Mode of action Examples Concerns
Fibrates PPARα Target cholesterol metabolism
Increase fatty acid oxidation
Clofibrate, gemfibrozil, ciprofibrate, bezafibrate, fenofibrate Increased risk of cancer (especially liver)
Thiazolidinediones PPARγ Insulin resistance is decreased, adipocyte differentiation is increased, leptin decreased and adiponectin increased Rosiglitazone (Avandia®)
pioglitazone (Actos®)
troglitazone (Rezulin®)
Rosiglitazone - concern over cardiovascular events; pioglitazone - concerns over bladder cancer; troglitazone withdrawn due to increased drug-induced hepatitis
PPAR-delta agonists PPARδ Stimulate fatty acid oxidation in skeletal muscle and adipose tissue, decrease insulin resistance, stimulate glucose metabolism None currently on the market They have been linked with increased and decreased risks of cancer; drug-induced myopathy
Dual agonists and PPARpana agonists Two or all three receptors A combination of the effects of the pure agonists Aleglitazar, muraglitazar and tesaglitazar Increased risk of certain cancers; increased risk of myocardial infarction
  1. This table shows some of the different types of drugs that are used to treat type II diabetes and obesity by targeting at least one of the PPAR receptors. Given the wide range of drugs that fall into this class of compounds, the list is not comprehensive but used to illustrate the diverse range of drugs available. aA PPARpan drug targets all three PPAR receptors.