THE WOODLANDS, Texas,
June 29, 2012 /PRNewswire/ -- Lexicon
Pharmaceuticals, Inc. (Nasdaq: LXRX) announced today the
publication of results from two initial trials of LX4211 in
patients with type 2 diabetes in the online edition of the journal
Clinical Pharmacology & Therapeutics. The paper, containing
results from both trials, is entitled, "LX4211, a Dual SGLT1/SGLT2
Inhibitor, Improved Glycemic Control in Patients with Type 2
Diabetes in a Randomized, Placebo-controlled Trial," and will also
appear in an upcoming print edition of the journal. A link to the
online article can be accessed at
http://www.nature.com/clpt/journal/vaop/ncurrent/full/clpt201258a.html.
"This publication represents the first peer-reviewed description
of SGLT1 inhibition stimulating GLP-1 and PYY release in man," said
Dr. Brian Zambrowicz, Lexicon's executive vice president and chief
scientific officer. "Since LX4211 also inhibits SGLT2, the rapid
and significant glycemic control and metabolic benefits observed
may be attributed to effective dual inhibition of these two
targets."
In the 4-week Phase 2a study described in the paper, 36 patients
received once-daily oral administration of placebo or 150 mg or 300
mg of LX4211 (randomized 1:1:1) in an in-patient setting. Patients
receiving LX4211 exhibited rapid and significant improvements
relative to placebo in multiple measures of glycemic control,
including hemoglobin A1c (HbA1c), fasting plasma glucose, and oral
glucose tolerance. In addition, serum triglycerides were
significantly lower at the end of the four-week treatment period,
and trends of meaningful reductions in body weight and blood
pressure were observed. Importantly, LX4211 treatment demonstrated
a favorable safety profile and was well tolerated in the study.
Also described in the paper was a subsequent clinical study
conducted in a similar population of poorly-controlled patients
with type 2 diabetes that showed LX4211 treatment elevated GLP-1
and PYY, two gastrointestinal peptides known to be associated with
enhanced metabolic control. These elevations in GLP-1 levels after
LX4211 treatment were previously suggested by data from the Phase
2a study and, hence, the repeated observation confirmed that LX4211
can act as an oral, GLP-1 secretagogue.
Lexicon recently reported top-line results from a Phase 2b
double-blind study of LX4211 that extend favorable observations of
the early trials to an out-patient setting in a larger population
with a longer duration of therapy. The 12-week study was conducted
at more than 50 centers in the United
States in 299 patients with poorly-controlled diabetes
despite treatment with metformin, an established diabetes therapy.
Primary and secondary measures of efficacy from this study
demonstrated substantial, dose-dependent, statistically-significant
reductions in HbA1c, body weight and blood pressure. LX4211's dual
inhibition of SGLT1 and 2 was associated with an overall favorable
safety profile in the study and, notably, LX4211's inhibition of
SGLT1 was associated with a favorable gastrointestinal safety
profile similar to placebo.
About Lexicon
Lexicon is a biopharmaceutical company focused on
discovering breakthrough treatments for human disease. Lexicon
currently has five drug programs in mid-stage development for
diabetes, carcinoid syndrome, irritable bowel syndrome, rheumatoid
arthritis and glaucoma, all of which were discovered by Lexicon's
research team. Lexicon 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.
Safe Harbor Statement
This press release contains "forward-looking statements,"
including statements relating to Lexicon's clinical development
of LX4211, characterizations of the results of and projected timing
of clinical trials of LX4211, and the potential therapeutic and
commercial potential of LX4211. This press release also
contains forward-looking statements relating to Lexicon's growth
and future operating results, discovery and development of
products, strategic alliances and intellectual property, as well as
other matters that are not historical facts or information. All
forward-looking statements are based on management's current
assumptions and expectations and involve risks, uncertainties and
other important factors, specifically including those relating to
Lexicon's ability to successfully conduct clinical development of
LX4211 and preclinical and clinical development of its other
potential drug candidates, advance additional candidates into
preclinical and clinical development, obtain necessary regulatory
approvals, achieve its operational objectives, obtain patent
protection for its discoveries and establish strategic alliances,
as well as additional factors relating to manufacturing,
intellectual property rights, and the therapeutic or commercial
value of its drug candidates, that may cause Lexicon's actual
results to be materially different from any future results
expressed or implied by such forward-looking statements. Unless
specifically indicated otherwise, results reported as trends were
not statistically significant. Information identifying such
important factors is contained under "Risk Factors" in Lexicon's
annual report on Form 10-K for the year ended December 31, 2011, as filed with the Securities
and Exchange Commission. Lexicon undertakes no obligation to update
or revise any such forward-looking statements, whether as a result
of new information, future events or otherwise.
SOURCE Lexicon Pharmaceuticals, Inc.