1179-P: Pharmacokinetics, Pharmacodynamics, and Safety of HD-6277, a Selective Agonist of G-Protein-Coupled Receptor 40, in Healthy Subjects as a First-in-Human Study

HD-6277 is a potent and selective G-protein-coupled receptor 40 agonist for the treatment of type 2 diabetes mellitus. Previous studies with HD-6277 showed enhanced glucose-stimulated insulin secretion and improved glycemic control in type 2 diabetic rodent models. To evaluate the potential benefits of HD-6277 on safety, tolerability, pharmacokinetics and pharmacodynamics, HD-6277 was investigated with six and four sequential cohorts in single and multiple ascending doses in healthy subjects as randomized, double-blind, placebo-controlled study, respectively. HD-6277 was well absorbed over all doses under fasting conditions and systemic exposure was increased in dose-dependent manner both in single and multiple ascending dose study. There was no severe or serious adverse events showing generally mild and transient profile, which suggested no safety concerns with the doses administered. Therefore, this study showed HD-6277 was safe and well tolerated in healthy subjects. Its exploratory efficacy on type 2 diabetes mellitus patients is currently under evaluation.