The Peroxisome proliferator activated receptor α (PPARα) is a ligand activated transcription factor that belongs to the family of nuclear receptors. PPARα is activated by polyunsaturated fatty acids and synthetic drugs like fibrates. After hetrodimerization with its partner RXRα, PPARα plays a central role in fatty acid oxidation and uptake in tissues like liver, heart, skeletal muscle and kidney. In addition, PPARα is also expressed in endothelial cells, vascular smooth muscle cells and macrophages where it exerts anti-inflammatory and anti-oxidative effects. PPARα agonists decrease the progression of diseases like atherosclerosis and the metabolic syndrome by controlling dyslipidemia, inflammation and glucose intolerance, underscoring PPARα as an important pharmacological target.