Safinamide, also known as FCE-26743 and EMD-1195686, is a drug indicated for the treatment of Parkinson's disease with multiple methods of action. Potential additional uses might be restless legs syndrome (RLS) and epilepsy. Safinamide is a reversible and selective monoamine oxidase B inhibitor, reducing degradation of dopamine, and a glutamate release inhibitor. It also inhibits dopamine reuptake. Additionally, safinamide blocks sodium and calcium channels. Safinamide has been approved by the European Medicines Agency for the treatment of adult patients with idiopathic Parkinson’s disease as add-on therapy to a stable dose of Levodopa (L-dopa) alone or in combination with other PD drugs in patients with mid-to-late-stage fluctuating disease.
Park, Ki Duk; Yang, Xiao-Fang; Dustrude, Erik T.; Wang, Yuying; Ripsch, Matthew S.; White, Fletcher A.; Khanna, Rajesh; Kohn, Harold. Chimeric agents derived from the functionalized amino acid, lacosamide, and the α-aminoamide, safinamide: evaluation of their inhibitory actions on voltage-gated sodium channels, and antiseizure and antinociception activities and comparison with lacosamide and safinamide. Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy. (ACS Chemical Neuroscience Volume 6 Issue 2)
Murugan, Muthukrishnan; Mohammad, Mujahid. An improved enantioselective and regioselective process for preparation of anti-parkinson agent safinamide and its analogues. WO 2014178083. (Council of Scientific & Industrial Research, India)
Barbanti, Elena; Faravelli, Laura; Salvati, Patricia; Canevotti, Renato; Ponzini, Francesco. Process for the production of highly pure 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides as cytochrome P450 inhibitors and their pharmaceutical compositions and use in the treatment of diseases. WO 2009074478. (Newron Pharmaceuticals S.p.A., Italy)
Barbanti, Elena; Caccia, Carla; Salvati, Patricia; Velardi, Francesco; Ruffilli, Tiziano; Bogogna, Luigi. Process for the production of 2-[4-(3- and 2-fluorobenzyloxy) benzylamino]propanamides. US 20090156678. (Newron Pharmaceuticals S.p.A., Italy)
Barbanti, Elena; Caccia, Carla; Salvati, Patricia; Velardi, Francesco; Rufilli, Tiziano; Bogogna, Luigi. Process for the production of 2-[4-(3- and 2-fluorobenzyloxy)benzylamino]propanamides (safinamide and ralfinamide) of high purity by catalytic hydrogenation of Schiff base intermediates and their use for treating CNS disorders. WO 2007147491. (Newron Pharmaceuticals S.p.A., Italy)
Leonetti, Francesco; Capaldi, Carmelida; Pisani, Leonardo; Nicolotti, Orazio; Muncipinto, Giovanni; Stefanachi, Angela; Cellamare, Saverio; Caccia, Carla; Carotti, Angelo. Solid-Phase Synthesis and Insights into Structure-Activity Relationships of Safinamide Analogues as Potent and Selective Inhibitors of Type B Monoamine Oxidase. Journal of Medicinal Chemistry. Volume 50. Issue 20. Pages 4909-4916. 2007.
Reddi, Anjaneyulu; Mujahid, Mohammad; Sasikumar, Murugesan; Muthukrishnan, Murugan. A new enantioselective synthesis of the anti-Parkinson agent safinamide. Synthesis. Volume 46. Issue 13. Pages 1751-1756. 2014.
Xing, Ruijuan; Lu, Tao; Liu, Leina; Zhu, Mengchu; Du, Yumin. Synthesis of safinamide. Zhongguo Yiyao Gongye Zazhi. Volume 43. Issue 3. Pages 161-163. 2012.
Sun, Tingting. Preparation of safinamide mesylate. CN 107915657 A. (2018).
