THE WOODLANDS, Texas,
June 25, 2012 /PRNewswire/ -- Lexicon
Pharmaceuticals, Inc. (Nasdaq: LXRX), announced today that LX4211,
an investigational, oral, dual inhibitor of sodium glucose
transporters 1 and 2 (SGLT1 and SGLT2), showed substantial,
dose-dependent, statistically-significant reductions in hemoglobin
A1c (HbA1c) in a Phase 2b trial in patients diagnosed with
poorly-controlled type 2 diabetes who were concurrently treated
with metformin, an established diabetes therapy. LX4211 treatment
also produced significant reductions in body weight and blood
pressure. Importantly, LX4211 treatment had a favorable safety
profile and was well tolerated in the study.
LX4211, a unique dual inhibitor, reduces the amount of glucose
that enters the bloodstream from the gastrointestinal (GI) tract by
inhibiting SGLT1, the major transporter responsible for glucose
absorption, and enhances glucose excretion in the urine by
inhibiting SGLT2, the major transporter responsible for glucose
reabsorption by the kidney. Lexicon has previously demonstrated
that SGLT1 inhibition by LX4211 increases GLP-1 and PYY, GI
hormones associated with glycemic control and appetite.
"New diabetes therapies will need to help patients safely
control blood sugar and address other metabolic parameters that
play a role in this pervasive disease," said Dr. Arthur Sands, president and chief executive
officer of Lexicon. "The positive results obtained when LX4211 is
combined with metformin suggest it has the potential to make a
meaningful contribution to diabetes care."
In this 12-week dose-ranging study conducted in over 50 centers
in the United States, 299 patients
with poorly controlled type 2 diabetes on metformin therapy were
randomized to receive either LX4211 or placebo. The primary
endpoint of the study was the change in HbA1C, a measure of
glycemic control, from baseline to week 12. LX4211 was administered
at doses of 75 mg QD, 200 mg QD, 200 mg BID and 400 mg QD. Top-line
results showed that patients in the LX4211 treatment arms had mean
HbA1C reductions from baseline of 0.43, 0.52, 0.79 and 0.95
percent, respectively (p