Description
Application
TAK-475 has been used:
as a farnesyl-diphosphate farnesyltransferase 1 (FDFT1) inhibitor to study its effects on cell signaling in pancreatic ductal adenocarcinoma cells
as a squalene synthase (SQS) inhibitor to stabilize HMG-CoA reductase (HMGCR)-dCat-ELuc proteins
as an SQS inhibitor to study its effects on the migration of prostate cancer cells
Biochem/physiol Actions
Squalene synthase inhibitor
TAK-475 (Lapaquistat acetate) is a potent and selective squalene synthase inhibitor. TAK-475 effectively lowers low-density lipoprotein cholesterol in human. Clinical development of TAK-475 was discontinued due to hepatotoxicity seen in two patients receiving a high dose.