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XenoPort
announced today the inclusion of gabapentin
enacarbil, the active ingredient in Horizant(R) (gabapentin enacarbil)
Extended-Release Tablets, as a first-line therapy in new treatment
guidelines created by the Task Force of the International Restless Legs
Syndrome Study Group (IRLSSG). The manuscript, published in the current
issue of Sleep Medicine, provides information for physicians determining
treatment choices for restless legs syndrome/Willis-Ekbom Disease (RLS/WED)
based on the long-term benefits and risks of each major class of
medications. Horizant is the only non-dopamine agonist and the only
alpha-2-delta ligand approved by the U.S. Food and Drug Administration (FDA)
for the treatment of moderate-to-severe primary restless legs syndrome in
adults.
"The last few years have seen tremendous advances in our knowledge of both
the etiology of RLS/WED and its effective treatment," stated Diego
Garcia-Borreguero, M.D., Chair, International Restless Legs Study Group and
Director, Sleep Research Institute, Madrid, Spain. "These guidelines are an
important tool for guiding physicians in the choice for pharmacotherapy of
patients requiring long-term treatment of RLS/WED symptoms."
The guidelines state that either dopamine-receptor agonists or the
alpha-2-delta ligands, which include gabapentin enacarbil, are the
first-line treatment for patients with RLS/WED, and that the choice of the
initial treatment should be based on the individual clinical features of
RLS/WED in a given patient. The guidelines indicate that alpha-2-delta
ligands should be considered for initial treatment in patients with severe
sleep disturbance (disproportionate to other RLS/WED symptoms), comorbid
insomnia or anxiety, RLS/WED-related or comorbid pain, or a history of an
impulse control disorder (ICD) or anxiety. In addition, the guidelines
recommend that patients with clinically significant daytime symptoms should
be treated with a long-acting agent. The published guidelines are available
at www.IRLSSG.org.
"We are happy to see that Horizant, the only non-dopamine agonist and the
only alpha-2-delta ligand approved by the FDA, is being recognized as an
important treatment option for patients with RLS/WED," stated Ronald W.
Barrett, Ph.D., chief executive officer of XenoPort, Inc. "There is growing
recognition that the dopamine agonists are not appropriate or sufficient for
long-term treatment of all RLS/WED patients. We are proud to contribute an
alternative first-line treatment to the RLS/WED community."
About Restless Legs Syndrome
RLS/WED is a neurological condition that causes an irresistible urge to move
the legs. This urge is usually caused or accompanied by unpleasant
sensations of burning, creeping, tugging or tingling inside the patients'
legs, ranging in severity from uncomfortable to painful. These RLS-related
symptoms typically begin or worsen during periods of rest or inactivity,
particularly when lying down or sitting, and may be temporarily relieved by
movement such as walking or massaging the legs. Symptoms often worsen at
night, and disturbed sleep is a common result of RLS. Left untreated,
moderate-to-severe primary restless legs syndrome may cause exhaustion,
daytime fatigue, inability to concentrate and impaired memory.
About Horizant (gabapentin enacarbil)
Gabapentin enacarbil is a patented molecule that was discovered and
developed by XenoPort. It utilizes XenoPort's Transported Prodrug technology
that was designed to take advantage of high-capacity transport mechanisms in
the gastrointestinal tract to offer efficient absorption and extended
exposure of gabapentin. (Horizant is not interchangeable with other
gabapentin products).
IMPORTANT SAFETY INFORMATION
Effects on Driving
Horizant may cause significant driving impairment. Patients should not drive
until they have enough experience on Horizant to know if it impairs their
driving. Patients' ability to assess their driving competence and degree of
somnolence caused by Horizant can be imperfect.
Somnolence/Sedation and Dizziness
Horizant causes somnolence/sedation and dizziness. Patients should not drive
or operate other complex machinery until they have enough experience on
Horizant to know if it impairs their ability to perform these tasks.
Lack of Interchangeability With Gabapentin
Horizant is not interchangeable with other gabapentin products because of
differing pharmacokinetic profiles. The same dose of Horizant results in
different plasma concentrations of gabapentin relative to other gabapentin
products. The safety and effectiveness of Horizant in patients with epilepsy
have not been studied.
Suicidal Behavior and Ideation
Horizant is a prodrug of gabapentin, an antiepileptic drug (AED). AEDs
increase the risk of suicidal thoughts or behavior in patients taking these
drugs for any indication. As a prodrug of gabapentin, Horizant also
increases this risk. Patients treated with any AED for any indication should
be monitored for new or worsening depression, suicidal thoughts or behavior,
and/or any unusual changes in mood or behavior. Anyone considering
prescribing Horizant must balance the risk of suicidal thoughts or behavior
with the risk of untreated illness.
Patients, caregivers, and families should be informed that Horizant
increases the risk of suicidal thoughts and behavior and should be advised
of the need to be alert for new or worsening signs of and symptoms of
depression, any unusual changes in mood or behavior, or the emergence of
suicidal thoughts, behavior, or thoughts of self-harm. Behaviors of concern
should be reported immediately to healthcare providers.
Drug Reaction With Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan
Hypersensitivity
Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), also known as
multiorgan hypersensitivity, has been reported in patients taking
antiepileptic drugs, including gabapentin. Horizant is a prodrug of
gabapentin. Some of these events have been fatal or life-threatening. DRESS
typically, although not exclusively, presents with fever, rash, and/or
lymphadenopathy, in association with other organ system involvement, such as
hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis
sometimes resembling an acute viral infection. Eosinophilia is often
present. Because this disorder is variable in its expression, other organ
systems not noted here may be involved.
It is important to note that early manifestations of hypersensitivity, such
as fever or lymphadenopathy, may be present even though rash is not evident.
If such signs or symptoms are present, the patient should be evaluated
immediately. Horizant should be discontinued if an alternative etiology for
the signs or symptoms cannot be established.
Discontinuation of Horizant
When discontinuing Horizant, patients with RLS receiving 600 mg or less once
daily can discontinue the drug without tapering. If the recommended dose is
exceeded, the dose should be reduced to 600 mg daily for 1 week prior to
discontinuation to minimize the potential of withdrawal seizure.
Tumorigenic Potential
In an oral carcinogenicity study, gabapentin enacarbil increased the
incidence of pancreatic acinar cell adenoma and carcinoma in male and female
rats. The clinical significance of this finding is unknown.
ADVERSE REACTIONS
The most common adverse reactions for patients with RLS receiving Horizant
600 mg, 1,200 mg, and placebo, respectively, were somnolence/sedation (20%,
27%, and 6%), dizziness (13%, 22%, and 4%), headache (12%, 15%, and 11%),
nausea (6%, 7%, and 5%), and fatigue (6%, 7%, and 4%). A daily dose of 1,200
mg provided no additional benefit compared with the 600-mg dose, but caused
an increase in adverse reactions.
DRUG INTERACTIONS
Gabapentin enacarbil is released faster from Horizant Extended-Release
tablets in the presence of alcohol. Consumption of alcohol is not
recommended when taking Horizant. Horizant taken in conjunction with
morphine causes increased somnolence/sedation, dizziness, and nausea.
USE IN SPECIAL POPULATIONS
Pregnancy and Lactation
Based on animal data, Horizant may cause fetal harm. There are no adequate
and well-controlled studies of Horizant in pregnant women. Horizant should
be used during pregnancy only if potential benefit justifies potential risk
to fetus. Horizant is converted to gabapentin, which is secreted into human
milk. Discontinue nursing or discontinue Horizant, taking into account the
importance of Horizant to the mother, due to potential for adverse reactions
in nursing infants.
Renal Impairment
In patients with RLS who have compromised renal function, Horizant should be
dosed based upon creatinine clearance (CrCl): 30 to 59 mL/min, start with
300 mg per day and increase to 600 mg as needed; 15 to 29 mL/min, use 300 mg
per day; <15 mL/min, use 300 mg every other day. Horizant is not recommended
for use in patients receiving hemodialysis.
About XenoPort
XenoPort, Inc. is a biopharmaceutical company focused on developing and
commercializing a portfolio of internally discovered product candidates for
the potential treatment of neurological disorders. We are currently
commercializing Horizant, our first approved product, and developing our
novel fumaric acid ester product candidate, XP23829, as a potential
treatment for relapsing-remitting multiple sclerosis and/or psoriasis.
Horizant is being marketed by XenoPort in the United States. Regnite(R)
(gabapentin enacarbil) Extended-Release Tablets is being marketed in Japan
by Astellas Pharma Inc. XenoPort's pipeline of product candidates also
includes potential treatments for patients with spasticity related to spinal
cord injury and Parkinson's disease.
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