Tonix Pharmaceuticals Holding Corp. (OTCBB: TNXP) (“TONIX” or the
“Company”), a specialty pharmaceutical company developing non-addictive
treatments for chronic pain syndromes, today reports that its new
sublingual (under-the-tongue) formulation of its fibromyalgia (FM) drug
TNX-102 reduces the production of a problematic metabolite, according to
data from a recently-completed clinical trial.
Buy Aceon (Perindopril Erbumine) pills online without prescription
“The study shows that bedtime TNX-102 SL should offer a substantial
improvement over off-label oral tablets in the treatment of
fibromyalgia”
TNX-102 is the Company’s low dose form of cyclobenzaprine.
Cyclobenzaprine is a drug originally approved by the Food and Drug
Administration for short term treatment of acute muscle spasm several
decades ago and it is currently one of the most widely prescribed
off-label medications for FM. TONIX has shown that low dose
cyclobenzaprine given before bedtime is effective to reduce the pain
suffered by FM patients and to improve the quality of sleep. Yet when
given as an oral pill on a chronic daily regimen, cyclobenzaprine can
lose its effectiveness over time.
Tonix’s research sheds light on a potential cause of this problem. Tonix
has discovered that a significant amount of cyclobenzaprine from oral
tablets is converted into a metabolite called norcyclobenzaprine, which
builds up in the body with daily dosing. Although norcyclobenzaprine had
been described previously in cases of overdose, Tonix has found that the
levels of norcyclobenzaprine are significant even at low doses and that
norcyclobenzaprine is a psychoactive substance. Norcyclobenzaprine has a
similar effect on the brain as cyclobenzaprine, so the accumulation of
the metabolite over time is expected to interfere with the beneficial
effects of bedtime cyclobenzaprine. Norcyclobenzaprine makes it
impossible to use currently available cyclobenzaprine tablets in a
chronic bedtime dosing regimen to achieve beneficial effects on the
sleeping brain and still have the drug largely cleared by the next
morning.
TONIX’s new sublingual formulation of cyclobenzaprine (TNX-102 SL) can
significantly reduce this problem, according to the Company’s
pharmacokinetic study. The study showed that levels of the
norcyclobenzaprine metabolite can be reduced by using a sublingual
formulation compared to oral cyclobenzaprine tablets. As a result,
TNX-102 SL is a significant advance over oral tablets and is suitable
for long-term treatment.
“The study shows that bedtime TNX-102 SL should offer a substantial
improvement over off-label oral tablets in the treatment of
fibromyalgia,” said Seth Lederman, M.D., Chief Executive Officer of
TONIX. “That’s why we believe our drug has the potential to be a
game-changing medication in relieving pain and other symptoms of
fibromyalgia, even though the oral tablet version of cyclobenzaprine is
already available.”
“Delivering the drug under the tongue gets it into the bloodstream
faster, and changes the way the drug is metabolized,” Lederman
explained. “As a result, the production of the psychoactive, persistent
metabolite, norcyclobenzaprine, is decreased. We look forward to
commencing a pivotal trial of TNX-102 SL in fibromyalgia in the first
quarter of 2013. We believe the drug will help people afflicted with
fibromyalgia get the relief they need, by improving sleep quality.”
The new results reported by TONIX today come from a study designed to
confirm in humans the results obtained in animals which demonstrate that
the Company’s TNX-102 SL (2.4 mg) tablet provides faster delivery and
more efficient absorption of cyclobenzaprine as compared to the
currently available oral (5 mg or 10 mg) pills that deliver
cyclobenzaprine to the stomach. In those studies, TONIX discovered that
cyclobenzaprine given in a novel sublingual formulation is absorbed with
a profile comparable to intravenous cyclobenzaprine. Cyclobenzaprine is
the active ingredient in two prescription muscle relaxants that have
been approved by the U.S. Food and Drug Administration and are marketed
by other companies.
About Fibromyalgia
FM is a common and complex central nervous system condition
characterized by chronic diffuse musculoskeletal pain, increased pain
sensitivity at multiple tender points, fatigue, abnormal pain
processing, and disturbed sleep, and often features psychological
stress. Despite the fact that most FM patients suffer from poor sleep,
there are no medications indicated for FM that work by improving sleep.
Research has shown that the restorative sleep of FM patients is
disrupted by alarm signals called CAP A2 and A3. In a Phase 2a trial,
TONIX demonstrated that bedtime administration of very low dose
cyclobenzaprine improves core FM symptoms including pain, tenderness,
fatigue, and depression, and also demonstrated that improvements in key
symptoms correlate with increased nights of restorative sleep. These
results were published in the December 2011 issue of the
Journal of
Rheumatology.
About TNX-102
TNX-102 is a bedtime medicine containing very low dose cyclobenzaprine
(2.4 mg). In a randomized, double-blind, placebo-controlled eight-week
Phase 2 study in FM patients, TONIX demonstrated that treatment with
TNX-102 led to significant improvements in pain and other core symptoms.
TONIX is optimizing TNX-102 for faster and more efficient absorption
relative to currently marketed cyclobenzaprine products. TONIX believes
its TNX-102 SL formulation will provide more targeted sleep quality
effects with less likelihood of side effects than commercially available
cyclobenzaprine preparations. Previous studies of the mechanism by which
cyclobenzaprine works have discovered that it acts selectively on
serotonin receptor type 2a (5HT2a) and alpha-2 adrenergic receptors.
Serotonin is thought to play a major role in the central inhibition of
pain.
About TONIX
TONIX is developing innovative prescription medications for challenging
disorders of the central nervous system. The Company targets conditions
characterized by significant unmet medical need, inadequate existing
treatment options, and high dissatisfaction among both patients and
physicians. TONIX’s core technology improves the quality of sleep in
patients with chronic pain syndromes. TONIX’s lead products are designed
to be fundamental advances in sleep hygiene and pain management and to
be safer and more effective than currently available treatments. TONIX’s
products are the result of a program to harvest advances in science and
medicine to search for potential therapeutic solutions among known
pharmaceutical agents. TONIX is developing new formulations that have
been optimized for new therapeutic uses. Its most advanced product
candidates, TNX-102 for FM and TNX-105 for post- traumatic stress
disorder, are novel dosage formulations of cyclobenzaprine, the active
ingredient in two U.S. FDA-approved muscle relaxants.
Certain statements in this press release are forward-looking within
the meaning of the Private Securities Litigation Reform Act of 1995.
These statements may be identified by the use of forward-looking words
such as "anticipate," "believe," "forecast," "estimated" and "intend,"
among others. These forward-looking statements are based on TONIX’s
current expectations and actual results could differ materially. There
are a number of factors that could cause actual events to differ
materially from those indicated by such forward-looking statements.
These factors include, but are not limited to, substantial competition;
our ability to continue as a going concern; our need for additional
financing; uncertainties of patent protection and litigation;
uncertainties of government or third party payer reimbursement; limited
sales and marketing efforts and dependence upon third parties; and risks
related to failure to obtain FDA clearances or approvals and
noncompliance with FDA regulations. As with any pharmaceutical under
development, there are significant risks in the development, regulatory
approval and commercialization of new products. TONIX does not undertake
an obligation to update or revise any forward-looking statement.
Investors should read the risk factors set forth in the Annual Report on
Form 10-K filed with the SEC on March 30, 2012 and future periodic
reports filed with the Securities and Exchange Commission. All of the
Company's forward-looking statements are expressly qualified by all such
risk factors and other cautionary statements. The information set forth
herein speaks only as of the date hereof.
