Phase 1 study of MBX-2982 for the treatment of type 2 diabetes

Metabolex announced positive results from two Phase 1 clinical trials of MBX-2982 for the treatment of type 2 diabetes. Both studies enrolled patients with pre-diabetes. Study 1 investigated the pharmacokinetics of four consecutive once daily doses of MBX-2982 (100mg or 300mg) as well as its effect on glucose excursions following a mixed meal. Additionally, the effect of MBX-2982 on insulin secretion during a graded glucose infusion was examined.

Study 1 results showed that MBX-2982 was rapidly absorbed, its exposure doubling on day 4 compared to day 1, consistent with a terminal half-life of about 18 hours, thus supporting once daily dosing. Glucose excursions following a mixed meal were reduced by 26% and 37%, respectively, for the 100mg and 300mg cohorts. During the graded glucose infusions, exposure to glucose was reduced by 11% and 18% for the 100mg and 300mg cohorts, respectively. Results were all statistically significant.

Study 2 was a five-day, placebo-controlled, multiple ascending dose study with an alternate formulation of MBX-2982 at doses of 25mg, 100mg, 300mg, and 600mg. The effect of each dose on the glucose excursions following a mixed meal and an oral glucose challenge was evaluated. All four doses of MBX-2982 produced statistically significant decreases in the glucose excursion following a mixed meal, ranging from 34–51%. Similar decreases were also observed following the glucose challenge.

MBX-2982 is a potent, selective, orally active agonist of G protein-coupled receptor 119 (GPR119), a receptor expressed in pancreatic islets and the gastrointestinal tract that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion and release of incretin hormones such as GLP-1, and thus may preserve beta cell health.

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