Potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat.
APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).