Pharmacological properties and clinical efficacy of rasagiline mesylate (Azilect^®)

Abstract

Parkinson’s disease is a neurodegenerative disorder that manifests as motor deficits, tremors, rigidity, and postural instability. The most prominent pathological feature of this disease is reduced striatal dopamine concentration due to the loss of nigrodopaminergic neurons. Symptomatic dopamine replacement therapy is the standard management approach for Parkinson’s disease. Treatment with monoamine oxidase B (MAO-B) inhibitors also improves Parkinson’s disease symptoms by inhibiting the striatal dopamine metabolism and increasing the intracerebral dopamine concentration. Rasagiline is a potent and specific MAO-B inhibitor and is currently approved as an antiparkinsonian drug in more than 50 countries, including the United States and European countries. Clinical trials conducted in Japan to evaluate the efficacy of rasagiline monotherapy in patients with early-stage Parkinson’s disease using the Movement Disorder Society-Unified Parkinson’s Disease Rating Scale Part II (patient motor experience of daily living) and Part III (clinician motor examination) have demonstrated the antiparkinsonian action of rasagiline. Furthermore, in patients with advanced Parkinson’s disease receiving levodopa, concomitant rasagiline administration reduced the duration of “wearing–off”. Based on these favorable results, rasagiline mesilate (Azilect^® tablets) was approved for manufacture and sales in Japan in March 2018. Here, we provide a comprehensive overview of the pharmacological properties and clinical effects of rasagiline based on the results of domestic trials, with the aim of increasing the understanding of rasagiline use in Japan.