Valeant Pharmaceuticals International, a global, science-based specialty pharmaceutical company, announced that the US Food and Drug Administration (FDA) approved Zelapar (selegiline HCl) Orally Disintegrating tablets, a once-daily adjunct therapy for Parkinson's disease patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy.
Zelapar, a monoamine oxidase-B (MAO-B) inhibitor, is the first Parkinson's disease treatment to use a novel oral delivery system called Zydis Technology, which allows the tablets to dissolve within seconds in the mouth and deliver more active drug at a lower dose.
"With more than 1.5 million Americans with Parkinson's disease, and 60,000 new cases diagnosed each year, having new treatment options available to help manage the symptoms associated with the disease are critical," said Valeant president and chief executive officer, Timothy C. Tyson. "The approval of Zelapar means that patients now have an additional alternative that can help them significantly reduce their daily 'off' time during waking hours. Zelapar is the second therapy Valeant has brought to market to help in the treatment of Parkinson's disease, and we remain committed to the Parkinson's disease community and to providing therapies that fill the tremendous unmet medical need."
The use of Zelapar as adjunctive therapy to levodopa/carbidopa has been shown to reduce "off" time, on average, by 2.2 hours per day. Levodopa/carbidopa is commonly used early in the treatment of Parkinson's disease, but as the disease progresses it becomes increasingly difficult to adequately control symptoms with this medication. Parkinson's disease patients may endure many hours of "off" time each day in which their symptoms return as a result of levodopa/carbidopa wearing off.
"Patients with Parkinson's disease still experience many hours a day during which their treatment wears off," said Cheryl H. Waters, M.D., F.R.C.P. (C), Albert B. and Judith L. Glickman professor, Department of Neurology, Columbia University Medical Center. "The unique formulation of Zelapar allows the orally disintegrating tablet to dissolve within seconds. By delivering more active drug at a lower dose, Zelapar significantly reduces "off" time, giving valuable hours back to the patient."
The effectiveness of Zelapar as an adjunct to levodopa/carbidopa in the treatment of Parkinson's disease in patients who exhibit deterioration in the quality of their response to this therapy was established in a 12-week multi-centre, double-blind, randomized, placebo-controlled, parallel-group study. Patients received either 1.25 mg of the drug or placebo each day for the first six weeks and then 2.5 mg of the drug or placebo once-daily for the following six weeks. Zelapar was shown to significantly reduce "off" time after one week of treatment. At the end of 12 weeks, Zelapar treated patients had, on average, 2.2 hours per day less "off" time compared to baseline, and placebo-treated patients had 0.6 hours per day less "off" time. The observed reduction in "off" time between the two treatment groups compared to baseline was statistically significant (p less than 0.001).
The most common adverse events reported by patients treated with Zelapar were comparable to placebo and included nausea (11%), dizziness (11%), pain (8%), headache (7%), insomnia (7%), rhinitis (7%), dyskinesia (6%), skin disorders (6%), stomatitis (5%), back pain (5%) and dyspepsia (5%).
MAO inhibitors have been used as an adjunct therapy in Parkinson's disease since the first clinical trials of levodopa therapy in the early 1960s. Selegiline, the active ingredient in Zelapar, is an MAO-B inhibitor that prevents the breakdown of dopamine, the key neurotransmitter in the brain controlling movement. Using an innovative transbuccal drug delivery system called Zydis Technology, Zelapar Orally Disintegrating Tablets dissolve within seconds in the mouth and deliver more active drug at a lower dose.
Zelapar is the first Parkinson's disease treatment to use Zydis, and due to its fast-disintegrating technology, Zelapar significantly bypasses the gut and first-pass hepatic metabolism. It is primarily absorbed into the systemic circulation through the oral mucosa, thereby potentially enhancing the therapeutic effect and reducing side effects.