Ezetimibe | Cholesterol absorption inhibitor

Ezetimibe (163222-33-1) inhibits cholesterol absorption in the intestine by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter.¹ Undergoes rapid glucuronidation in the intestine where its glucuronide binds NPC1L1.² Inhibits dengue virus infection in Huh-7 cells by blocking cholesterol transport.³ Ameliorates steatohepatitis by activation of autophagy and inhibition of NLRP3 inflammasome.⁴

References/Citations

1) Wang et al. (2007), Regulation of intestinal cholesterol absorption; Annu. Rev. Physiol., 69 221
2) Garcia-Calvo et al. (2005), The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1); Proc. Natl. Acad. Sci. USA, 102 8132
3) Osuna-Ramos et al. (2018), Ezetimibe inhibits dengue virus infection in Huh-7 cells by blocking the cholesterol transporter Niemann-Pick C1-like 1 receptor; Regulat. Curr. Opin. Cell Biol., 160 151
4) Kim et al. (2017), Ezetimibe ameliorates steatohepatitis via AMP activated protein kinase-TFEB-mediated activation of autophagy and NLRP3 inflammasome inhibition; Autophagy, 13 1767