Pharmacokinetic Study of Oral 14C-Radiolabeled Hyzetimibe, A New Cholesterol Absorption Inhibitor.

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Date: May 28, 2021
Publisher: Frontiers Research Foundation
Document Type: Report
Length: 426 words
Lexile Measure: 1540L

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Author(s): Jianwei Liao, Xin Wang, Zhenyu Li, Dongsheng Ouyang

<bold>Background and objectives:</bold> Hyzetimibe is a candidate drug being investigated as the second-in-class cholesterol absorption inhibitor; it lowers plasma levels of low-density lipoprotein cholesterol (LDL-C) by blocking the Niemann-Pick C1-like 1 protein, a transporter mainly expressed in the intestine that allows dietary cholesterol to enter the body from the intestinal lumen. Previous studies on the metabolism of hyzetimibe in healthy volunteers were not enough to show the biotransformation and excretion pathway; in particular, whether hyzetimibe maintains pharmacological action for duration sufficient to pass through the hepatic-intestinal circulation remains unknown. Furthermore, it remains unclear whether the differences between...

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Gale Document Number: GALE|A663437235