Case study: Retrospective study of fasiglifam－ Is in vitro screening study a strong tool to avoid DILI risk?

Abstract

In vitro screening experiments such as hepatobiliary transporter inhibition, inhibition of mitochondrial function or reactive metabolite formation w/ and w/o covalent binding have been proposed to predict human drug-induced liver injury (DILI). Fasiglifam was an agonist of GPR40 under development for type 2 diabetes. Unfortunately, a development program was terminated late in phase III trials due to liver safety concerns. In this symposium, it would be introduced whether in vitro screening approaches of fasiglifam which were retrospectively conducted could predict DILI risk in a phase III.