Fenofibrate

Fenofibrate is an agonist of peroxisome proliferator-activated receptor α (PPARα) with EC₅₀ values of 18 and 30 μM for mouse and human receptors, respectively, in a transactivation assay.¹ It is selective for PPARα over PPARγ (EC₅₀s = 300 and 200 μM for mouse and human receptors, respectively) and lacks activity at mouse and human PPARδ at a concentration of 100 μM. In vivo, fenofibrate (50-100 mg/kg) reduces plasma levels of triglycerides, C-reactive protein, and malondialdehyde (MDA) in mice with fructose-induced hypertriglycemia in a dose-dependent manner.² It decreases glomerular and tubular atrophy and necrosis induced by cisplatin (Item No. 13119) in rat kidney when administered at a dose of 100 mg/kg.³ Fenofibrate also reduces the number of pulmonary lesions induced by 4-nitroquinoline 1-oxide (4-NQO) in lung in Tsumura Suzuki obese diabetic (TSOD) mice.⁴

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1. Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J. Med. Chem. 43(4), 527-550 (2000).

2. Sun, B., Xie, Y., Jiang, J., et al. Pleiotropic effects of fenofibrate therapy on rats with hypertriglycemia. Lipids Health Dis. 14:27, (2015).

3. Helmy, M.M., Helmy, M.W., and El-Mas, M.M. Additive renoprotection by pioglitazone and fenofibrate against inflammatory, oxidative and apoptotic manifestations of cisplatin nephrotoxicity: Modulation by PPARs. PLoS One 10(11), e0142303 (2015).

4. Kuno, T., Hata, K., Takamatsu, M., et al. The peroxisome proliferator-activated receptor (PPAR) α agonist fenofibrate suppresses chemically induced lung alveolar proliferative lesions in male obese hyperlipidemic mice. Int. J. Mol. Sci. 15(5), 9160-9172 (2014).