生物活性

• 描述Bezafibrate (BEZ) is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent^[3]. Bezafibrate was not cytotoxic against human retinal microvascular endothelial cells (HRMECs) and human retinal pigment epithelial cells (ARPE-19 cells) treated with <100 and 200μM bezafibrate, respectively. In HRMECs, the expression levels of tumor necrosis factor (TNF)-α-induced monocyte chemoattractant protein (MCP)-1, intercellular adhesion molecule (ICAM)-1, and vascular cell adhesion molecule (VCAM)-1 were significantly suppressed by bezafibrate in a dose-dependent manner. TNF-α-induced nuclear translocation of nuclear factor (NF)-κB p65 and cell migration were also significantly inhibited in bezafibrate-treated HRMECs. Furthermore, bezafibrate treatment significantly suppressed interleukin (IL)-1β-induced vascular endothelial growth factor (VEGF) production in ARPE-19 cells^[4]. BEZ ameliorates diabetes probably via reduced steatosis, enhanced hepatic mitochondrial mass, improved metabolic flexibility and elevated hepatic insulin sensitivity in TallyHo mice^[5]. Bezafibrate is a useful and well-tolerated lipid-modifying agent in the management of primary and secondary dyslipidaemia^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02584504	Hypercholesterolemia	Phase 3	Completed	-	Japan ... more >> Investigational Site Number 392028 Ageo-Shi, Japan Investigational Site Number 392007 Chuo-Ku, Japan Investigational Site Number 392029 Chuo-Ku, Japan Investigational Site Number 392014 Fukui-Shi, Japan Investigational Site Number 392023 Hachioji-Shi, Japan Investigational Site Number 392013 Itoshima-Shi, Japan Investigational Site Number 392010 Kanazawa-Shi, Japan Investigational Site Number 392024 Kasuga-Shi, Japan Investigational Site Number 392004 Kawanishi-Shi, Japan Investigational Site Number 392015 Kitakyushu-Shi, Japan Investigational Site Number 392005 Komatsu-Shi, Japan Investigational Site Number 392032 Matsudo-Shi, Japan Investigational Site Number 392017 Matsumoto-Shi, Japan Investigational Site Number 392003 Mito-Shi, Japan Investigational Site Number 392018 Morioka-Shi, Japan Investigational Site Number 392009 Moriya-Shi, Japan Investigational Site Number 392006 Nagoya-Shi, Japan Investigational Site Number 392011 Nagoya-Shi, Japan Investigational Site Number 392019 Nagoya-Shi, Japan Investigational Site Number 392025 Nagoya-Shi, Japan Investigational Site Number 392027 Osaka-Shi, Japan Investigational Site Number 392030 Sakura-Shi, Japan Investigational Site Number 392016 Shinagawa-Ku, Japan Investigational Site Number 392001 Shinjuku-Ku, Japan Investigational Site Number 392008 Shinjuku-Ku, Japan Investigational Site Number 392012 Shizuoka-Shi, Japan Investigational Site Number 392002 Suita-Shi, Japan Investigational Site Number 392031 Suita-Shi, Japan Investigational Site Number 392020 Toyonaka-Shi, Japan Investigational Site Number 392022 Yao-Shi, Japan Collapse <<
  NCT02584504	-	-	Completed	-	-
  NCT03031821	Prostate Cancer ... more >> Metabolic Syndrome Collapse <<	Phase 3	Not yet recruiting	June 1, 2023	Canada, British Columbia ... more >> BC Cancer Agency - Vancouver Cancer Centre Not yet recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Bernie Eigl, MD    604-877-6000    bernie.eigl@bccancer.bc.ca    Principal Investigator: Bernie Eigl, MD Collapse <<

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• 参考文献

• [1] Cabrero A, Alegret M, et al. Bezafibrate reduces mRNA levels of adipocyte markers and increases fatty acid oxidation in primary culture of adipocytes. Diabetes. 2001 Aug;50(8):1883-90.

  [2] Krey G, Braissant O, et al. Fatty acids, eicosanoids, and hypolipidemic agents identified as ligands of peroxisome proliferator-activated receptors by coactivator-dependent receptor ligand assay. Mol Endocrinol. 1997 Jun;11(6):779-91.

  [3] Willson TM, Brown PJ, Sternbach DD, Henke BR. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50

  [4] Usui-Ouchi A, Ouchi Y, Ebihara N. The peroxisome proliferator-activated receptor pan-agonist bezafibrate suppresses microvascular inflammatory responses of retinal endothelial cells and vascular endothelial growth factor production in retinal pigmented epithelial cells. Int Immunopharmacol. 2017 Nov;52:70-76

  [5] Franko A, Neschen S, Rozman J, Rathkolb B, Aichler M, Feuchtinger A, Brachthäuser L, Neff F, Kovarova M, Wolf E, Fuchs H, Häring HU, Peter A, Hrabě de Angelis M. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266

  [6] Goa KL, Barradell LB, Plosker GL. Bezafibrate. An update of its pharmacology and use in the management of dyslipidaemia. Drugs. 1996 Nov;52(5):725-53

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