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Drug Research and Development Pipeline
Balsalazide Tablets
In July 2007, Salix Pharmaceuticals, Inc. submitted to the U.S. Food and Drug Administration (FDA) a New Drug Application (NDA) seeking approval to market
a tablet formulation of balsalazide disodium, with a 3.3g twice daily dosing regimen, for the treatment of mildly to moderately active ulcerative
colitis. Balsalazide 1.1g tablets are an advanced formulation of the azo–bonded 5–ASA prodrug, balsalazide disodium, specifically designed
for 99% delivery directly to the colon.
Budesonide
Salix has recently obtained a license from Dr. Falk Pharmaceuticals (Germany) to develop its family of budesonide products in the United States, which
includes a patent–protected gastro–resistant capsule and a rectal foam. Salix is currently evaluating the budesonide foam preparation for
the treatment of mild to moderately active forms of distal ulcerative colitis, specifically ulcerative colitis affecting the rectum and sigmoid colon.
Crofelemer
Salix recently has acquired rights to crofelemer from Napo Pharmaceuticals, Inc. Crofelemer currently is being investigated as an anti–secretory
anti–diarrheal agent for the treatment of chronic diarrhea in people living with HIV, or HIV–associated diarrhea. Crofelemer is a locally–acting,
minimally–absorbed product which is believed to possess dual mechanisms of action that may be effective in treating both acute infectious
diarrhea and chronic diarrhea.
Mesalamine Granules
Granulated mesalamine is an advanced formulation of 5–ASA with both a delayed and extended release system that delivers mesalamine directly to the
colon with minimal systemic exposure and once–daily dosing. In October 2008, Salix was granted approval for the maintenance of remission of
ulcerative colitis (trade name: APRISO).
Metoclopramide
In September 2007, Salix expanded its product portfolio through the acquisition of an orally disintegrating formulation of metoclopramide.
Wilmington Pharmaceuticals, the licensor, submitted to the US Food and Drug Administration (FDA) a New Drug Application seeking approval to market an orally
disintegrating tablet (ODT) formulation of metoclopramide for the treatment of short-term therapy (4 to 12 weeks) for adults with symptomatic, documented
gastroesophageal reflux who fail to respond to conventional therapy and for the relief of symptoms associated with acute and recurrent diabetic gastroparesis.
Upon approval from the FDA in September 2009, Salix received exclusive worldwide rights to this new ODT metoclopramide formulation (trade name: METOZOLV® ODT).
Rifaximin
Rifaximin, a nonsystemic (<0.4% of the drug absorbed into the bloodstream), gastrointestinal-selective, oral antibiotic,
represents Salix’s next effort to provide products that meet the needs of gastroenterologists and their patients.
On March 24, 2010, the US Food and Drug Administration (FDA) granted marketing approval for XIFAXAN®
(rifaximin) 550 mg tablets for reduction in risk of overt hepatic encephalopathy (HE) recurrence in patients 18 years of age or older.
Caused by chronic liver failure, HE is a serious disorder that can result in cognitive, psychiatric and motor impairments.
Salix also markets XIFAXAN® (rifaximin) 200 mg tablets, approved by the FDA on May 25, 2004 for the treatment of patients,
12 years of age or older, with travelers’ diarrhea (TD) caused by noninvasive strains of Escherichia coli.
Salix obtained the North American licensing rights to rifaximin from Alfa Wassermann SpA (Italy). The product has been marketed in Italy
(Normix® and Rifacol®) since 1988 and is now approved in over 30 countries.
Over 550 clinical papers, abstracts, and textbook chapters discussing the use of rifaximin for treatment of various GI disorders have been published to date.
Current areas of research and development for rifaximin include TD prophylaxis, Irritable Bowel Syndrome (IBS), Hepatic Encephalopathy and Clostridium difficile infection.
In June 2010, Salix submitted to the FDA an efficacy supplement for XIFAXAN® (rifaximin) 550 mg tablets for the
proposed indication of treatment of nonconstipation irritable bowel syndrome (Non–C IBS) and IBS–related bloating.
Additional Opportunities
New product opportunities are a key component of our future growth. Please check here for announcements of the latest additions to our product pipeline.
Important Safety Information about XIFAXAN 200 mg
XIFAXAN® (rifaximin) 200 mg Tablets are indicated for the treatment of patients (≥12 years of age) with travelers’ diarrhea caused by noninvasive strains of Escherichia coli. XIFAXAN should not be used in patients with diarrhea complicated by fever or blood in the stool or diarrhea due to pathogens other than E coli. XIFAXAN should be discontinued if diarrhea symptoms get worse or persist more than 24 to 48 hours and alternative antibiotic therapy should be considered. E coli has been shown to develop resistance to rifaximin in vitro. However, the clinical significance of such an effect has not been studied.
In clinical trials, XIFAXAN was generally well tolerated. The most common side effects (vs placebo) were flatulence 11.3% (vs 19.7%), headache 9.7% (vs 9.2%), abdominal pain 7.2% (vs 10.1%), rectal tenesmus 7.2% (vs 8.8%), defecation urgency 5.9% (vs 9.2%), and nausea 5.3% (vs 8.3%).
For complete Prescribing Information, please click here.
APRISO™ is a locally-acting aminosalicylate indicated for the maintenance of remission of ulcerative colitis in patients 18 years and older.
APRISO is contraindicated in patients with hypersensitivity to salicylates, aminosalicylates, or to any of the components of APRISO capsules.
The recommended dose of APRISO is four 0.375 g capsules once daily in the morning (1.5 g/day) with or without food. Because dissolution of the coating of APRISO
granules depends on pH, APRISO should not be coadministered with antacids. Patients with phenylketonuria should be aware that APRISO contains aspartame,
equivalent to 0.56 mg of phenylalanine. In two well-controlled clinical trials, the most common treatment-related adverse events occurring in at least 3%
of adult patients taking 1.5 g/day of APRISO were headache (11% vs. 8% for placebo), diarrhea (8% vs. 7% for placebo), upper abdominal pain (5% vs 3% for placebo),
nausea (4% vs 3% for placebo), nasopharyngitis (4% vs 3% for placebo), influenza and influenza-like illness (4% vs 4% for placebo) and sinusitis (3% vs 3% for placebo).
For complete Prescribing Information, please click here.
Important Safety Information about METOZOLV ODT
Treatment with metoclopramide can cause tardive dyskinesia, a serious movement disorder that is often irreversible.
The risk of developing tardive dyskinesia increases with the duration of treatment and the total cumulative dose.
Metoclopramide therapy should be discontinued in patients who develop signs or symptoms of tardive dyskinesia.
There is no known treatment for tardive dyskinesia. In some patients, symptoms may lessen or resolve after metoclopramide treatment is stopped.
Treatment with metoclopramide for longer than 12 weeks should be avoided in all but rare cases where therapeutic benefit is thought to outweigh the risk of developing tardive dyskinesia.
METOZOLV® ODT
(metoclopramide HCl) is indicated as short-term (4 to 12 weeks) therapy for adults with symptomatic, documented gastroesophageal
reflux disease (GERD) who fail to respond to conventional therapy and for the relief of symptoms associated with acute and
recurrent diabetic gastroparesis (diabetic gastric stasis) in adults. Therapy should not exceed 12 weeks in duration. Take on
an empty stomach up to four times daily, at least 30 minutes before eating and at bedtime.
METOZOLV ODT is contraindicated in patients with intestinal obstruction, hemorrhage, or perforation; pheochromocytoma;
known sensitivity or intolerance to metoclopramide; epilepsy; or are receiving concomitant medications with extrapyramidal reactions.
Extrapyramidal symptoms (EPS), manifested primarily as acute dystonic reactions, occur in approximately 1 in 500 patients treated with the
usual adult dosages of 30 to 40 mg/day of metoclopramide. These usually are seen during the first 24 to 48 hours of treatment with metoclopramide,
occur more frequently in pediatric patients and adult patients less than 30 years of age and are even more frequent at higher doses.
Drug-induced Parkinsonism can occur during metoclopramide therapy, more commonly within the first 6 months after beginning treatment,
but also after longer periods. Patients with a history of Parkinson’s disease should be given metoclopramide cautiously, if at all,
since such patients can experience exacerbation of Parkinsonian symptoms when taking metoclopramide.
There have been rare reports of an uncommon but potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) associated
with metoclopramide. Clinical manifestations of NMS include hyperthermia, muscle rigidity, altered consciousness, and evidence of autonomic instability.
The management of NMS should include immediate discontinuation of metoclopramide and other drugs not essential to concurrent therapy.
Depression associated with metoclopramide use has occurred in patients with and without a history of depression.
For those patients with a prior history of depression, metoclopramide should only be given if the expected benefits outweigh the potential risks.
In one study in hypertensive patients, intravenously administered metoclopramide was shown to release catecholamines; hence, caution should be exercised
when metoclopramide is used in patients with hypertension. Any rapid rise in blood pressure associated with METOZOLV ODT use should result in immediate
cessation of metoclopramide use in those patients.
Since metoclopramide produces a transient increase in plasma aldosterone, patients with cirrhosis or congestive heart failure may be at risk of developing
fluid retention and volume overload. If these side effects occur at any time in any patients during metoclopramide therapy, the drug should be discontinued.
Adverse reactions, especially those involving the nervous system, may occur after stopping the use of METOZOLV ODT.
In clinical studies, the most frequently reported adverse events (≥2% occurrence) were headache, nausea, fatigue, somnolence, and vomiting.
Full Prescribing Information for METOZOLV ODT, including BOXED WARNING.