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Hyzetimibe

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Chemical compound Pharmaceutical compound
Hyzetimibe
Clinical data
Other namesHS-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
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC25H21F2NO3
Molar mass421.444 g·mol
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

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.

References

  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.
  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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