Squalene synthase inhibition: a novel target for the management of dyslipidemia.
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.
Davidson
Michael H
MH
Radiant Research, 515 N. State Street, Suite 2700, Chicago, IL 60610, USA. michaeldavidson@radiantresearch.com
D017326:Clinical Trials, Phase III as Topic; D016503:Drug Delivery Systems; D050171:Dyslipidemias / Q000188:drug therapy* / Q000201:enzymology*; D013186:Farnesyl-Diphosphate Farnesyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D006801:Humans; D010077:Oxazepines / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology
C466644:1-((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; D010077:Oxazepines; D010880:Piperidines; D013186:Farnesyl-Diphosphate Farnesyltransferase