LX4211 Achieves Positive Results in Type 2 Diabetes Patients with Renal Impairment

   LX4211 Achieves Positive Results in Type 2 Diabetes Patients with Renal
                                  Impairment

PR Newswire

THE WOODLANDS, Texas, Oct. 1, 2013

THE WOODLANDS, Texas, Oct. 1, 2013 /PRNewswire/ --Lexicon Pharmaceuticals,
Inc. (Nasdaq: LXRX) announced today that LX4211, a first-in-class, dual
inhibitor of sodium glucose transporters 1 and 2 (SGLT1 and SGLT2),
successfully met the primary endpoint of reducing post-prandial glucose, in a
study of patients with type 2 diabetes and moderate to severe renal
impairment. Reducing elevated post-prandial glucose, high blood sugar levels
after meals, is a key objective of diabetes therapy.

In a placebo-controlled, proof-of-concept study, LX4211 provided clinically
meaningful and statistically significant reductions (p<0.05) in post-prandial
glucose in diabetes patients with moderate to severe renal impairment (Stage 3
and 4 kidney disease). Importantly, these effects were maintained in a
sub-group with the most advanced renal impairment, pre-defined as those with
glomerular filtration rate (GFR) less than 45 ml/min/1.73 m^2. LX4211 also
produced significant elevations in GLP-1, a hormone involved in control of
glucose and appetite.

Renal impairment occurs in approximately 30% of patients with type 2 diabetes
and represents a major unmet medical need with limited treatment options.
LX4211's inhibition of SGLT1 in the gastrointestinal (GI) tract, reducing
glucose absorption and triggering GLP-1 secretion, offers the potential for
treating this medically challenging population with compromised kidney
function. In previous Phase 2 studies, LX4211 improved glycemic control in
patients with type 2 diabetes with normal renal function.

"Our hypothesis was that LX4211 would improve glycemic control even in
patients with the greatest degree of renal impairment due to its inhibition of
SGLT1 in the GI tract," said Pablo Lapuerta, M.D., Lexicon's chief medical
officer. "The post-prandial glucose reductions and GLP-1 elevations observed
in this study population support the rationale for demonstrating effective
HbA1c reduction in a larger, longer-term Phase 3 trial, and provide further
support for the clinical differentiation of LX4211 as a first-in-class dual
SGLT1 and SGLT2 inhibitor."

In this multicenter study, 30 patients with poorly controlled type 2 diabetes
and moderate to severe renal impairment were randomized to either placebo or a
400 mg dose of investigational drug LX4211 taken orally once per day before
breakfast. Patients' post-prandial glucose was measured after a standardized
meal both at baseline before treatment and after one week of therapy. In
addition to achieving the primary efficacy objective of post-prandial glucose
reduction, there were no serious adverse events observed in the study and no
discontinuations of LX4211 due to adverse events. Lexicon plans to present
full results of the study at scientific congresses in 2014.

About Lexicon

Lexicon is a biopharmaceutical company focused on discovering breakthrough
treatments for human disease. Lexicon currently has multiple programs in
clinical development for diabetes, irritable bowel syndrome, carcinoid
syndrome and other indications, 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. The 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. 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, 2012, 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.

Website: http://www.lexpharma.com
Contact: Alex Abuin, Ph.D., Vice President, Communications and Alliance
Management, 281/863-3213, aabuin@lexpharma.com