Description
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.
References
Skrypnyk N, Chen X, Hu W, et al. PPARα activation can help prevent and treat non-small cell lung cancer. Cancer Res. 2014 Jan 15;74(2):621-31. PMID: 24302581.
Zhong X, Xiu LL, Wei GH, et al. Bezafibrate enhances proliferation and differentiation of osteoblastic MC3T3-E1 cells via AMPK and eNOS activation. Acta Pharmacol Sin. 2011 May;32(5):591-600. PMID: 21499286.
Tenenbaum A, Motro M, Fisman EZ, et al. Bezafibrate for the secondary prevention of myocardial infarction in patients with metabolic syndrome. Arch Intern Med. 2005 May 23;165(10):1154-60. PMID: 15911729.
Tenenbaum A, Motro M, Fisman EZ, et al. Peroxisome proliferator-activated receptor ligand bezafibrate for prevention of type 2 diabetes mellitus in patients with coronary artery disease. Circulation. 2004 May 11;109(18):2197-202. PMID: 15123532.
Bezafibrate Infarction Prevention (BIP) study. Secondary prevention by raising HDL cholesterol and reducing triglycerides in patients with coronary artery disease. Circulation. 2000 Jul 4;102(1):21-7. PMID: 10880410.
