Squalene synthase inhibition: a novel target for the management of dyslipidemia

Curr Atheroscler Rep. 2007 Jan;9(1):78-80. doi: 10.1007/BF02693932.

Abstract

A new class of compounds, known as squalene synthase inhibitors, has recently reached phase III clinical trials and may provide another therapeutic option for clinicians to improve risk management of low-density lipoprotein cholesterol (LDL-C). The clinical need for another LDL-C-lowering therapy is evident by the inability to achieve an LDL-C target of less than 70 mg/dL in the majority of very high-risk patients on statin monotherapy. Human clinical trial data with TAK-475, a novel and potent inhibitor of squalene synthase, have not yet been published.

MeSH terms

  • Clinical Trials, Phase III as Topic
  • Drug Delivery Systems*
  • Dyslipidemias / drug therapy*
  • Dyslipidemias / enzymology*
  • Farnesyl-Diphosphate Farnesyltransferase / antagonists & inhibitors*
  • Farnesyl-Diphosphate Farnesyltransferase / metabolism*
  • Humans
  • Oxazepines / pharmacology
  • Piperidines / pharmacology

Substances

  • 1-((1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl)acetyl)piperidine-4-acetic acid
  • Oxazepines
  • Piperidines
  • Farnesyl-Diphosphate Farnesyltransferase