Hyzetimibe

Hyzetimibe
Clinical data
Other names	HS-25
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name (3R,4S)-1-(4-Fluorophenyl)-3-((Z)-3-(4-fluorophenyl)-4-hydroxy-but-2-enyl)-4-(4-hydroxyphenyl)azetidin-2-one;
CAS Number	1266548-74-6 ;
PubChem CID	50923862 ;
ChemSpider	68007168 ;
UNII	NUM111M552 ;
ChEMBL	ChEMBL4297389 ;
Chemical and physical data
Formula	C25H21F2NO3
Molar mass	421.444 g·mol−1
	InChI InChI=InChI=1S/C25H21F2NO3/c26-19-6-1-16(2-7-19)18(15-29)5-14-23-24(17-3-12-22(30)13-4-17)28(25(23)31)21-10-8-20(27)9-11-21/h1-13,23-24,29-30H,14-15H2/b18-5+/t23-,24-/m1/s1; Key:HEHHPZYUXSFAPV-SMOXZEHUSA-N;

Last updated October 01, 2025

Hyzetimibe is a pharmaceutical drug that inhibits cholesterol absorption.^[1]^[2] It targets the NPC1-like intracellular cholesterol transporter 1.^[2]

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.^[3]

In China, it is used as a lipid-lowering agent and it has efficacy similar to ezetimibe.^[4]

References

↑ Ruan Z, Jiang B, Chen J, Zhang X, Lou H, Xiang M, et al. (October 2014). "Pharmacokinetics, pharmacodynamics, safety, and tolerability of hyzetimibe (HS-25) in healthy Chinese subjects". Journal of Clinical Pharmacology. 54 (10): 1144–1152. doi:10.1002/jcph.310. PMID 24752831.
1 2 Liao J, Yang L, Zhou L, Zhao H, Qi X, Cui Y, Ouyang D (2022). "The NPC1L1 Gene Exerts a Notable Impact on the Reduction of Low-Density Lipoprotein Cholesterol in Response to Hyzetimibe: A Factorial-Designed Clinical Trial". Frontiers in Pharmacology. 13 755469. doi: 10.3389/fphar.2022.755469 . PMC 8963242 . PMID 35359877.
↑ Pharmacokinetic Study of Oral 14C-Radiolabeled Hyzetimibe, A New Cholesterol Absorption Inhibitor
↑ Li JJ, Zhao SP, Zhao D, Lu GP, Peng DQ, Liu J, et al. (2023). "2023 Chinese guideline for lipid management". Frontiers in Pharmacology. 14 1190934. doi: 10.3389/fphar.2023.1190934 . PMC 10498001 . PMID 37711173.

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[1] Ruan Z, Jiang B, Chen J, Zhang X, Lou H, Xiang M, et al. (October 2014). "Pharmacokinetics, pharmacodynamics, safety, and tolerability of hyzetimibe (HS-25) in healthy Chinese subjects". Journal of Clinical Pharmacology. 54 (10): 1144–1152. doi:10.1002/jcph.310. PMID 24752831.

[Liao_2022-2] 1 2 Liao J, Yang L, Zhou L, Zhao H, Qi X, Cui Y, Ouyang D (2022). "The NPC1L1 Gene Exerts a Notable Impact on the Reduction of Low-Density Lipoprotein Cholesterol in Response to Hyzetimibe: A Factorial-Designed Clinical Trial". Frontiers in Pharmacology. 13 755469. doi: 10.3389/fphar.2022.755469 . PMC 8963242 . PMID 35359877.

[3] Pharmacokinetic Study of Oral 14C-Radiolabeled Hyzetimibe, A New Cholesterol Absorption Inhibitor

[4] Li JJ, Zhao SP, Zhao D, Lu GP, Peng DQ, Liu J, et al. (2023). "2023 Chinese guideline for lipid management". Frontiers in Pharmacology. 14 1190934. doi: 10.3389/fphar.2023.1190934 . PMC 10498001 . PMID 37711173.

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