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Clin Pharmacol Ther. 2010 Jan;87(1):117-21. doi: 10.1038/clpt.2009.209. Epub 2009 Nov 11.

Transporters as drug targets: discovery and development of NPC1L1 inhibitors.

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  • 1Section on Lipid Sciences, Department of Pathology, Wake Forest University School of Medicine, Winston-Salem, North Carolina, USA.

Erratum in

  • Clin Pharmacol Ther. 2010 Jun;87(6):759.


The potent cholesterol absorption inhibitor ezetimibe was developed as a first-in-class drug for treating hypercholesterolemia even before its molecular target, Niemann-Pick C1-like 1 (NPC1L1), had been identified. The NPC1L1 protein mediates sterol transport across the enterocyte brush border membrane and is essential for intestinal cholesterol absorption, a major pathway controlling whole-body cholesterol homeostasis. An elucidation of the mechanism underlying NPC1L1-dependent cholesterol absorption would greatly facilitate the discovery and development of new cholesterol-lowering agents for treating hypercholesterolemia and other cholesterol-related metabolic disorders.

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