Phase 2 trial of LX4211 for the treatment of type 2 diabetes mellitus

Lexicon Pharmaceuticals announced positive results from its recently completed Phase 2 study of LX4211 in patients with type 2 diabetes mellitus. This study was a four-week, randomized, double-blind, placebo-controlled study in 36 patients with type 2 diabetes. Patients were randomized to receive either placebo (n=12) or LX4211, 150 mg (n=12) or 300 mg (n=12), once daily for 28 days. There was a marked decrease in fasting plasma glucose throughout the treatment period in both dose groups, with reductions at week four of 53.4 mg/dl and 65.9 mg/dl in the 150 mg and 300 mg dose groups, respectively, as compared to 15.1 mg/dl for placebo. These decreases in fasting plasma glucose relative to placebo were statistically significant for both LX4211 dose groups (p=0.001 and p<0.001, respectively). Notably, a substantial percentage (42%) of patients in the 300 mg dose group achieved fasting plasma glucose levels of <105 mg/dl at week four of dosing as compared to placebo (p=0.037).

After only four weeks of dosing, average percent hemoglobin A1c (HbA1c), a measure of blood glucose levels over time, was significantly reduced by 1.15 in the 150 mg dose group (p=0.036) and by 1.25 in the 300 mg dose group (p=0.017), as compared to 0.49 in the placebo group. HbA1c levels were reduced to less than or equal to 7% for half the patients in both dose groups; baseline levels were 8.22%, 8.50% and 8.20% for the 150 mg, 300 mg, and placebo groups, respectively. Patients in both dose groups also exhibited significantly improved glucose tolerance in response to oral glucose tolerance testing as compared to patients receiving placebo (p<0.001 for both dose groups), as measured by area under the curve (AUC). Consistent with the mechanism of action of LX4211, there was also a significant, dose-dependent increase in 24-hour urinary glucose excretion throughout the study period relative to placebo in both dose groups (p<0.001 at all time points measured).

LX4211 is a once-per-day, orally-delivered, small molecule drug candidate that inhibits the sodium-dependent glucose transporter 2 (SGLT2), lowering the accumulation of glucose in the body and reducing caloric load.

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