Hyzetimibe is a pharmaceutical drug that inhibits cholesterol absorption. It targets the NPC1-like intracellular cholesterol transporter 1.

It reduces plasma levels of low-density lipoprotein cholesterol (LDL-C) by blocking the Niemann-Pick C1-like 1 protein, a transporter mainly found in the intestine that allows dietary cholesterol to enter the body from the intestinal lumen.

In China, it is used as a lipid-lowering agent and it has efficacy similar to ezetimibe.