Drug intelligence / Profile preview

hybutimibe

Development stage
Phase 3
Lead developer
Hanhui Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Hybutimibe is a small molecule cholesterol absorption inhibitor developed as an analog of ezetimibe. It selectively inhibits the absorption of cholesterol from dietary and biliary sources in the small intestine, thereby reducing the transport of cholesterol to the liver, limiting hepatic storage, and increasing clearance from blood. Its mechanism is similar to ezetimibe but features a structural modification (hydroxyl group) that enhances glucuronidation and metabolite clearance, potentially reducing liver burden. Hybutimibe has been approved in China for hypercholesterolemia and has completed phase III trials demonstrating efficacy in lowering LDL-C both as monotherapy and in combination with atorvastatin. It is well-tolerated with a safety profile comparable to existing therapies[1][5][6][10].

Brand names
hybutimibe
Other names
hyzetimibe
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)

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