Ryder T1, Walker GS, Goosen TC, Ruggeri RB, Conn EL, Rocke BN, Lapham K, Steppan CM, Hepworth D, Kalgutkar AS.
Chem Res Toxicol. 2012 Oct 15;25(10):2138-52. doi: 10.1021/tx300243v. Epub 2012 Sep 27.Inhibition of intestinal and hepatic microsomal triglyceride transfer protein (MTP) is a potential strategy for the treatment of dyslipidemia and related metabolic disorders. Inhibition of hepatic MTP, however, results in elevated liver transaminases and increased hepatic fat deposition consistent with hepatic steatosis. Diethyl 2-((2-(3-(dimethylcarbamoyl)-4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-ylcarboxamido)phenyl)acetoxy)methyl)-2-phenylmalonate (JTT-130) is an intestine-specific inhibitor of MTP and does not cause increases in transaminases in short-term clinical trials in patients with dyslipidemia. Read More