THE WOODLANDS, Texas, Jan. 20 /PRNewswire-FirstCall/ -- Lexicon Pharmaceuticals, Inc. , a biopharmaceutical company focused on discovering breakthrough treatments for human disease, obtained positive results from a recently completed Phase 2 study of LX4211 in patients with type 2 diabetes mellitus. 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. LX4211, dosed as a single agent, provided improvements in glycemic control, demonstrating statistically significant benefits in the primary and multiple secondary efficacy endpoints.
The recently completed 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. Patients were sequestered, provided a controlled diet and monitored closely throughout the study period.
Importantly, 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).
"The magnitude and rapid response in glycemic control, combined with the triglyceride reduction, may distinguish LX4211 from other agents in this class," said Dr. Brian Zambrowicz, chief scientific officer of Lexicon. "We now believe that the action of LX4211 cannot be entirely explained by glucose excretion in the urine alone, but may also relate to secondary events that both further enhance glycemic control and provide the other metabolic improvements we have witnessed in this study."
"We believe the latest encouraging results with LX4211 demonstrate the potential for a therapeutic benefit for patients with type 2 diabetes," said Dr. Arthur T. Sands, president and CEO of Lexicon. "With positive results within the last few months from Phase 2 clinical trials of two candidates, we are proceeding with confidence that our drug discovery platform has produced investigational new drugs with great promise for patients."
About the LX4211 Mechanism of Action
LX4211 was developed at Lexicon as a potent inhibitor of the sodium glucose cotransporter 2 (SGLT2), a transporter responsible for the majority of glucose reabsorption by the kidneys. Lexicon found that mouse knockouts engineered to lack the SGLT2 gene are healthy and require less insulin to manage a glucose challenge. LX4211 may potentially treat diabetes by improving glycemic control as well as providing other metabolic benefits.
About Lexicon
Lexicon is a biopharmaceutical company focused on discovering breakthrough treatments for human disease. Lexicon currently has five drug candidates in development for autoimmune disease, carcinoid syndrome, diabetes, glaucoma and irritable bowel syndrome, all of which were discovered by the company's research team. The company has used its proprietary gene knockout technology to identify more than 100 promising drug targets. Lexicon has focused drug discovery efforts on these biologically-validated targets to create its extensive pipeline of clinical and preclinical programs. For additional information about Lexicon and its programs, please visit www.lexpharma.com.
Lexicon Pharmaceuticals, Inc.
