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Selegiline orally disintegrating tablet in the treatment of Parkinsons disease

Anthony Clarke and Joseph Jankovic

Mono- and adjunctive therapy with the oral monoamine oxidase B inhibitor selegiline has been used to treat motor complications resulting from long-term treatment of Parkinson’s disease. However, oral selegiline undergoes extensive first-pass metabolism resulting in low bioavailability and production of amphetamine and other metabolites, as well as compromised efficacy and tolerability. An orally disintegrating tablet of selegiline utilizing Zydis^® technology undergoes markedly reduced presystemic metabolism, thus providing higher plasma concentrations and lower levels of amphetamine metabolites. As an adjunct to levodopa, selegiline orally disintegrating tablet has been found to significantly reduce ‘off’ time, increase ‘on’ time, and improve motor function in Parkinson’s disease patients experiencing ‘wearing off’ episodes. This article provides an overview of the Zydis technology, the rationale for its application in delivering selegiline, and results from clinical trials of selegiline orally disintegrating tablet in patients with Parkinson’s disease.