Safinamide: A Review in Parkinson’s Disease

• Published in: CNS drugs Vol. 31; no. 2; pp. 169 - 176
• Main Authors: Blair, Hannah A., Dhillon, Sohita
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.02.2017; Springer Nature B.V
• Subjects: Adis Drug Evaluation; Alanine - administration & dosage; Alanine - adverse effects; Alanine - analogs & derivatives; Alanine - pharmacology; Amine oxidase (flavin-containing); Antiparkinson Agents - administration & dosage; Antiparkinson Agents - adverse effects; Antiparkinson Agents - pharmacology; Benzylamines - administration & dosage; Benzylamines - adverse effects; Benzylamines - pharmacology; Bioavailability; Clinical trials; Dopamine; Dopamine receptors; Dose-Response Relationship, Drug; Drug dosages; Drug Therapy, Combination; Dyskinesia; Glutamatergic transmission; Humans; Levodopa; Levodopa - administration & dosage; Medicine; Medicine & Public Health; Metabolism; Metabolites; Monoamine Oxidase Inhibitors - administration & dosage; Monoamine Oxidase Inhibitors - adverse effects; Monoamine Oxidase Inhibitors - pharmacology; Motor task performance; Movement disorders; Neurodegenerative diseases; Neurology; Neurosciences; Parkinson Disease - drug therapy; Parkinson Disease - physiopathology; Parkinson's disease; Pharmacotherapy; Psychiatry; Psychopharmacology; Quality of Life; Rodents; Studies; Urine; Entacapone; Levodopa; Motor Fluctuation; Little Square Mean; Rasagiline
• DOI: 10.1007/s40263-017-0408-1
• ISSN: 1172-7047; 1179-1934

Safinamide (Xadago ® ) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. In the EU, safinamide is approved for the treatment of mid- to late-stage fluctuating Parkinson’s disease (PD) as add-on therapy to a stable dose of levodopa alone or in combination with other PD medications. Safinamide 50–100 mg/day administered as a fixed or flexible dose significantly increased daily ‘on’ time without dyskinesia (primary endpoint) in patients with mid- to late-stage PD with motor fluctuations in 24-week, placebo-controlled clinical trials. Other outcomes, including motor function, overall clinical status and health-related quality of life, were also generally improved with safinamide. Furthermore, in an 18-month extension of one study, although dyskinesia (primary endpoint) was not significantly improved with safinamide relative to placebo, treatment benefits in other outcomes were generally sustained over 24 months of treatment. Safinamide was generally well tolerated in clinical trials; dyskinesia was the most common adverse event. Although further studies are needed, including comparative and long-term studies, current evidence indicates that safinamide extends the treatment options available for use as add-on therapy to levodopa and other PD medications in patients with mid- to late-stage PD experiencing motor fluctuations.