Metabolex, Inc., a biopharmaceutical company focused on the discovery and development of proprietary new medicines for the treatment of metabolic diseases, announced positive results from two multiple ascending dose Phase 1 clinical trials of MBX-2982.
MBX-2982 is a potent, selective, orally active agonist of G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion. It is a potential first-in-class treatment for type 2 diabetes that may offer improved glucose homeostasis over existing therapies.
Metabolex has recently completed two additional Phase 1 studies of MBX-2982 in subjects with pre-diabetes. In both studies, subjects with either impaired fasting glucose or impaired glucose tolerance were enrolled. The first study investigated the effect of four consecutive once daily doses (100 or 300 mg) of MBX-2982 on the pharmacokinetics of the drug as well as its effect on glucose excursions following a mixed meal. In addition, the effect of MBX-2982 on insulin secretion during a graded glucose infusion was examined. MBX-2982 was rapidly absorbed and its exposure at both doses approximately doubled on day four compared to day one, consistent with a terminal half-life of ~18 hr and supporting once daily dosing. The glucose excursions (area under the curve) following a mixed meal were reduced relative to baseline by 26% and 37%, respectively, for the 100 and 300 mg cohorts. During the graded glucose infusions, the exposure to glucose was reduced relative to baseline by 11% and 18% for the 100 and 300 mg cohorts, respectively. This was attributable to increases in insulin secretion. These results were all statistically significant.