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Lapaquistat


Lapaquistat
Systematic (IUPAC) name
1-[[(3R,5S)-1-(3-hydroxy-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
Identifiers
CAS number	189059-71-0
ATC code	?
PubChem	?
Chemical data
Formula	C₃₁H₃₉Cl N₂O₈
Mol. mass	603.103 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Lapaquistat (TAK-475) is a cholesterol-lowering drug currently in phase 3 clinical trials. Unlike statins which inhibit HMG-CoA reductase, lapaquistat metabolits inhibit squalene synthase which is further downstream in the synthesis of cholesterol. It is hoped that side effects can be reduced by not disturbing the mevalonate pathway which is important for other biochemical molecules besides cholesterol.

References

Davidson MH (Jan 2007). "Squalene synthase inhibition: a novel target for the management of dyslipidemia". Curr Atheroscler Rep 9 (1): 78-80. PMID 17169251.

Category: Hypolipidemic agents