Lexicon Initiates Phase 2 Trial of Type 2 Diabetes Drug Candidate

THE WOODLANDS, Texas -- Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), has obtained favorable results from its recently completed Phase 1 studies of LX4211 and has initiated a Phase 2 clinical trial of the drug candidate in patients with type 2 diabetes mellitus.

LX4211 is an orally-delivered, small molecule drug candidate that inhibits the sodium glucose transporter 2 (SGLT2). LX4211 was developed at Lexicon as a potent inhibitor of the sodium glucose transporter 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. Compounds developed by Lexicon that inhibit SGLT2 may potentially treat diabetes by increasing urinary glucose excretion, thereby lowering blood glucose levels as well as caloric load.

"LX4211 offers an opportunity to treat diabetes by increasing urinary glucose excretion through a mechanism of action that is expected to avoid some of the disadvantages of existing diabetes drugs that result in storage of excess glucose," said Brian P. Zambrowicz, Ph.D., executive vice president and chief scientific officer at Lexicon. "By contrast, LX4211 through inhibition of SGLT2 has the potential to reduce caloric load and thereby enhance overall glucose homeostasis in patients with type 2 diabetes."

In the recently completed Phase 1 clinical trial in normal healthy volunteers, LX4211 was well tolerated at all dose levels and produced a dose-dependent increase in urinary glucose excretion. LX4211 also demonstrated a favorable pharmacokinetic profile supporting the potential for once daily dosing. Adverse events were generally mild and were distributed across all dose groups, including the placebo group.

Based on the Phase 1 clinical results, Lexicon has initiated a Phase 2 clinical trial to evaluate the safety and tolerability of two dose levels of LX4211 and its effect on diabetes biomarkers including: fasting blood glucose, urinary glucose excretion and response to oral glucose tolerance testing in patients with type 2 diabetes. The four-week, randomized, double-blind, placebo-controlled study will be conducted in the U.S. and is expected to enroll 36 patients with type 2 diabetes.

Source: Lexicon Pharmaceuticals, Inc.