THE WOODLANDS, Texas,
Aug. 16, 2012 /PRNewswire/ -- Lexicon
Pharmaceuticals, Inc. (Nasdaq: LXRX), a biopharmaceutical company
focused on discovering breakthrough treatments for human disease,
today reported preliminary results from Phase 1 studies of LX2931
and LX7101.
The Phase 1 study of LX2931, an inhibitor of
sphingosine-1-phosphate lyase, was a dose-ranging study to explore
higher doses of LX2931 in patients with rheumatoid arthritis. The
study involved 10 patients with rheumatoid arthritis, eight of whom
were randomized to LX2931 and two to placebo. The primary
endpoint in the study was an evaluation of the safety and
tolerability of escalating doses of LX2931 compared with placebo
over 12 weeks in subjects with active rheumatoid arthritis.
Secondary endpoints included pharmacokinetic and disease activity
measures.
Patients in the study received increasing doses over the course
of the study, beginning at 50 mg QD and escalating to 500 mg
QD. LX2931 was well-tolerated at all doses evaluated, with no
serious adverse events and no withdrawals due to adverse events.
Seven of eight patients on LX2931 achieved drug trough levels
greater than 60 ng/ml, a pharmacokinetic measure which a post-hoc
analysis of data from a prior Phase 2 study of LX2931 had suggested
was associated with better responses in American College of
Rheumatology (ACR) measures in the study. Six of the eight
LX2931-treated patients experienced a drop from baseline in the
DAS28 score of greater than or equal to 1.2, as did both placebo
patients. ACR20 and ACR50 responses were achieved at varying
frequencies in both LX2931-treated and placebo patients, but two of
eight patients dosed with LX2931 achieved an ACR70 response during
the course of the study, compared to none on placebo.
The Phase 1 study of LX7101, an inhibitor of LIM domain kinase 2
(LIMK2), was a first-in-man study evaluating two doses of LX7101 in
glaucoma patients. The study involved 63 patients with
glaucoma randomized among two doses of LX7101 (0.125% solution and
0.25% solution, each given as an eye drop) or vehicle. The
primary endpoint in the study was an evaluation of the safety and
tolerability of LX7101 compared with vehicle over two weeks.
Secondary endpoints included measures of intraocular pressure
(IOP), taken at multiple time points on day -1, day 1, day 7 and
day 14.
Patients in the study received a single daily dose of LX7101 or
placebo during the first week of the study and two daily doses
during the second week. LX7101 was well-tolerated at all
doses evaluated, with no serious adverse events and no withdrawals
due to adverse events. Mean IOP changes from baseline at day 14 for
each LX7101 dose arm compared to vehicle at eight hours post-dose
were 3.18 mmHg for 0.125% and 2.32 mmHg for 0.25%, compared to 0.40
mmHg for vehicle (p=0.007 for 0.125% and p=0.028 for 0.25%).
Reductions from baseline at day 14 in the diurnal mean IOP,
representing mean changes across all daily time points, were 3.37
mmHg for 0.125% and 3.52 mmHg for 0.25%, compared to 2.17 mmHg for
vehicle (also statistically significant).
"We believe the results of these studies offer a potential path
for evaluating the efficacy of higher doses of LX2931 and
demonstrate the potential utility of LX7101's novel mechanism of
action," said Dr. Arthur T. Sands, president and chief executive
officer of Lexicon. "We will be evaluating the results of
these studies internally and with prospective partners in
determining next steps for these programs."
About Lexicon
Lexicon is a biopharmaceutical company focused on
discovering breakthrough treatments for human disease.
Lexicon currently has four drug programs in mid-stage development
for diabetes, irritable bowel syndrome, carcinoid syndrome and
rheumatoid arthritis, 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 LX2931 and LX7101, characterizations of the results of and
projected timing of clinical trials of such compounds, and the
potential therapeutic and commercial potential of such
compounds. 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 LX2931 and LX7101
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.