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Positive Results for a New First in Class Diabetes Drug
Posted: Wednesday, October 21, 2009
MBX-2982 could be a potential first-in-class treatment for Type 2 diabetes that may offer improved glucose homeostasis over existing therapies.
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.
Metabolex, the manufacturer has recently completed two 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.
The second study in a pre-diabetic population was a five-day placebo-controlled multiple ascending dose study with an alternate formulation of MBX-2982 at doses of 25, 100, 300 and 600 mg. Once daily dosing provided markedly enhanced exposures and improved dose proportionality, giving sustained levels of MBX-2982 predicted to be maximally effective. The effect of each dose on the glucose excursions following a mixed meal and an oral glucose challenge was investigated. All four doses of MBX-2982 produced statistically significant decreases in the glucose excursion following a mixed meal ranging from 34% to 51%. Similar decreases were also observed following the glucose challenge.
In both studies, MBX-2982 was safe and generally well tolerated with no serious adverse events, adverse event trends or dose-limiting toxicities. These results provide continued clinical validation of the potential therapeutic benefits of MBX-2982 in the treatment of Type 2 diabetes.
Harold Van Wart, Ph.D., Chief Executive Officer of Metabolex stated that, "These studies show that we are ready to advance MBX-2982 into a Phase 2a study in patients with Type 2 diabetes with a wide range of doses."
MBX-2982 is an agonist of GPR119, a GPCR that is expressed in pancreatic islets and the gastrointestinal tract. Pre-clinical studies conducted by Metabolex and others show that GPR119 agonists can stimulate glucose-dependent insulin secretion and release of incretin hormones such as GLP-1, and thus may preserve beta cell health. This novel dual mechanism may provide a unique therapeutic benefit in the treatment of Type 2 diabetes.
Source: Diabetes In Control: News Release: Metabolex
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