Bezafibrate is a PPARα agonist that is clinically used to lower LDL and triglyceride levels and to increase HDL levels. Bezafibrate exhibits anti-hyperlipidemic, cardioprotective, anti-diabetic, anti-osteoporotic, and anticancer chemotherapeutic activities. When administered clinically, bezafibrate decreases risk of myocardial infarction and cardiac mortality; it also decreases the incidence and delays the onset of type 2 diabetes. Bezafibrate promotes bone formation by activating proliferation and differentiation of osteoblasts in vitro in an AMPK- and PPARβ-dependent manner. In animal models of non-small cell lung cancer (NSCLC), bezafibrate decreases angiogenesis and tumor growth through downregulation of Cyp2c expression or activity.