Bezafibrate (BM15075) is an antilipemic agent that lowers CHOLESTEROL and TRIGLYCERIDES. It decreases LOW-DENSITY LIPOPROTEINS and increases HIGH-DENSITY LIPOPROTEINS.

PPARγ (murine):55 μM, PPARδ (murine):110 μM, PPARα (murine):90 μM, PPARδ (human):20 μM, PPARγ (human):60 μM, PPARα (human):50 μM

Bezafibrate significantly decreases plasma triglyceride and leptin levels without altering the expression of PPARγ in white adipose tissue or the ob gene. Treatment with Bezafibrate resulted in much smaller gonadal fat stores in wild-type and PPARβ-null mice (2.8 and ~2.6 times less, respectively) than in controls, while PPARα-null mice did not exhibit this effect. Bezafibrate altered the expression of mRNAs coding for lipid metabolism enzymes, such as AOX, CYP4A, LPL, ACS, and LCAD, in wild-type, PPARβ-null, and PPARα-null mice. It induced the expression of UCPs in rat epididymal white adipose tissue and altered energy balance by directly inducing aco gene expression (14.5-fold increase on day 7) and peroxisomal fatty acid beta-oxidation. Bezafibrate treatment upregulated mRNA levels of M-CPT-I (4.5-fold), fatty acid translocase (2.6-fold), and Pref-1 (5.6-fold) in rat epididymal white adipose tissue. Compared to controls, Bezafibrate significantly increased liver weight in wild-type and PPARβ-null mice, with no change observed in PPARα-null mice.

Bezafibrate exhibits an EC50 of 5 μM when binding to xPPARβ. Additionally, Bezafibrate activates the transcription of Xenopus PPARβ with an EC50 of 1 μM.