THE WOODLANDS, Texas,
Oct. 12, 2012 /PRNewswire/
-- Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), a
biopharmaceutical company focused on discovering and developing
breakthrough treatments for human disease, announced today that it
has initiated a registrational, Phase 3 clinical trial of
telotristat etiprate, an investigational new drug candidate for the
treatment of carcinoid syndrome. Carcinoid syndrome is a
chronic condition caused by neuroendocrine tumors that usually
originate from the gastrointestinal tract. It is characterized by
severe diarrhea and flushing episodes with long-term consequences
including malnutrition, heart disease, and death. Carcinoid
syndrome has been linked to excess production of serotonin by
metastatic tumor cells.
Telotristat etiprate is an oral drug candidate designed to treat
carcinoid syndrome by reducing serotonin production in patients
with metastatic carcinoid tumors. Telotristat etiprate has Fast
Track status and Orphan Drug designation from the U.S. Food and
Drug Administration, and Orphan designation from the European
Medicines Agency.
"The registrational, Phase 3 study is designed to evaluate the
efficacy and safety of telotristat etiprate in patients with
carcinoid syndrome that is refractory to somatostatin therapy,"
said Pablo Lapuerta M.D., senior
vice president and chief medical officer at Lexicon.
"We are encouraged by the consistent clinical results
obtained to date in two Phase 2 trials that showed
telotristat etiprate significantly improved multiple dimensions of
carcinoid syndrome with a favorable safety profile."
The Phase 3 registrational trial is a 12-week, randomized,
double-blind, placebo-controlled study to evaluate the efficacy and
safety of telotristat etiprate as a new treatment for carcinoid
syndrome that is refractory to current therapy. Two dose
levels of telotristat etiprate, 250mg and 500mg three times daily
(TID), will be tested along with placebo. The study will
include approximately 105 patients with refractory carcinoid
syndrome on background somatostatin analog therapy, assigned
equally among the 3 treatment groups using a 1:1:1 randomization
plan. After the 12-week treatment period, patients will enter a 36
week open-label extension period where all patients will receive
telotristat etiprate 500mg TID.
About Telotristat Etiprate (LX1032)
Telotristat etiprate was discovered and developed at Lexicon to
reduce serotonin production by inhibiting tryptophan hydroxylase
(TPH), a key enzyme in the synthesis of serotonin.
Serotonin's breakdown product, 5-HIAA, is a biomarker used in the
diagnosis of the condition. In preclinical studies,
telotristat etiprate reduced 5-HIAA and peripheral serotonin in
several different species without affecting serotonin levels in the
brain. Telotristat etiprate is a member of a new class of
oral drugs invented by Lexicon, the serotonin synthesis inhibitors,
which are being developed in a spectrum of gastrointestinal
indications. Lexicon is also carrying out a Phase 2 trial of
telotristat etiprate in mild to moderate ulcerative colitis.
About Carcinoid Syndrome
Carcinoid syndrome is a chronic condition caused by metastatic
neuroendocrine tumors that usually originate from the
gastrointestinal tract. Patients with carcinoid syndrome
currently have limited therapeutic options, and the standard of
care includes chronic therapy with somatostatin analogs, which are
delivered by injection. With current therapy, carcinoid
syndrome symptoms return over time in most patients, hence the need
for new agents.
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, carcinoid
syndrome, irritable bowel 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 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 preclinical and clinical development of its
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, 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.