Name: Safinamide
CAS#: 133865-89-1
Chemical Formula: C17H19FN2O2
Exact Mass: 302.1431
Molecular Weight: 302.3494
Elemental Analysis: C, 67.53; H, 6.33; F, 6.28; N, 9.27; O, 10.58
EOS Med Chem produce Safinamide, FCE 26743, 133865-89-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Safinamide, FCE 26743, 133865-89-1 Intermediates, EOS Med Chem have 8; Safinamide, FCE 26743, 133865-89-1 Impurity we have 10, all from GMP, FDA plant.
Now Safinamide, FCE 26743, 133865-89-1 DMF document is preparing.
Until 2016, Aug, Safinamide, FCE 26743, 133865-89-1 more than produced 25kg API, 120kg Intermediates
Description: 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.
Synonym: FCE-26743; FCE 26743; FCE26743; EMD-1195686; EMD 1195686; EMD1195686; Safinamide. Xadago
IUPAC/Chemical Name: (S)-2-((4-((3-fluorobenzyl)oxy)benzyl)amino)propanamide
SMILES Code: C[C@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
1: Stocchi F, Torti M. Adjuvant therapies for Parkinson's disease: critical evaluation of safinamide. Drug Des Devel Ther. 2016 Feb 5;10:609-18. doi: 10.2147/DDDT.S77749. eCollection 2016. Review. PubMed PMID: 26917951; PubMed Central PMCID: PMC4751980.
2: Cattaneo C, Sardina M, Bonizzoni E. Safinamide as Add-On Therapy to Levodopa in Mid- to Late-Stage Parkinson's Disease Fluctuating Patients: Post hoc Analysesof Studies 016 and SETTLE. J Parkinsons Dis. 2016;6(1):165-73. doi: 10.3233/JPD-150700. PubMed PMID: 26889632; PubMed Central PMCID: PMC4927927.
3: Perez-Lloret S, Rascol O. The safety and efficacy of safinamide mesylate for the treatment of Parkinson's disease. Expert Rev Neurother. 2016;16(3):245-58. doi: 10.1586/14737175.2016.1150783. Epub 2016 Feb 19. PubMed PMID: 26849427.
4: Rasheed MZ, Tabassum H, Parvez S. Mitochondrial permeability transition pore: a promising target for the treatment of Parkinson's disease. Protoplasma. 2016 Jan 29. [Epub ahead of print] PubMed PMID: 26825389.
5: Müller T. Safinamide for symptoms of Parkinson's disease. Drugs Today (Barc). 2015 Nov;51(11):653-9. doi: 10.1358/dot.2015.51.11.2414529. Review. PubMed PMID: 26744740.
6: Fabbri M, Rosa MM, Abreu D, Ferreira JJ. Clinical pharmacology review of safinamide for the treatment of Parkinson's disease. Neurodegener Dis Manag. 2015 Dec;5(6):481-96. doi: 10.2217/nmt.15.46. Epub 2015 Nov 20. PubMed PMID: 26587996.
7: Cattaneo C, Ferla RL, Bonizzoni E, Sardina M. Long-Term Effects of Safinamide on Dyskinesia in Mid- to Late-Stage Parkinson's Disease: A Post-Hoc Analysis. J Parkinsons Dis. 2015;5(3):475-81. doi: 10.3233/JPD-150569. PubMed PMID: 26406127; PubMed Central PMCID: PMC4923744.
8: Sadeghian M, Mullali G, Pocock JM, Piers T, Roach A, Smith KJ. Neuroprotection by safinamide in the 6-hydroxydopamine model of Parkinson's disease. Neuropathol Appl Neurobiol. 2016 Aug;42(5):423-35. doi: 10.1111/nan.12263. Epub 2015 Sep 25. PubMed PMID: 26300398.
9: Reichmann H. Modern treatment in Parkinson's disease, a personal approach. J Neural Transm (Vienna). 2016 Jan;123(1):73-80. doi: 10.1007/s00702-015-1441-1. Epub 2015 Aug 21. PubMed PMID: 26293352.
10: Rascol O, Perez-Lloret S, Ferreira JJ. New treatments for levodopa-induced motor complications. Mov Disord. 2015 Sep 15;30(11):1451-60. doi: 10.1002/mds.26362. Epub 2015 Aug 21. Review. PubMed PMID: 26293004.
11: Robakis D, Fahn S. Defining the Role of the Monoamine Oxidase-B Inhibitors for Parkinson's Disease. CNS Drugs. 2015 Jun;29(6):433-41. doi: 10.1007/s40263-015-0249-8. Review. PubMed PMID: 26164425.
12: Martinez-Martin P, Rodriguez-Blazquez C, Forjaz MJ, Kurtis MM. Impact of Pharmacotherapy on Quality of Life in Patients with Parkinson's Disease. CNS Drugs. 2015 May;29(5):397-413. doi: 10.1007/s40263-015-0247-x. Review. PubMed PMID: 25968563.
13: Deeks ED. Safinamide: first global approval. Drugs. 2015 Apr;75(6):705-11. doi: 10.1007/s40265-015-0389-7. Review. PubMed PMID: 25851099.
14: Chung JY, Lee JW, Ryu CH, Min HK, Yoon YJ, Lim MJ, Park CH. 1-[2-(4-Benzyloxyphenoxy)Ethyl]Imidazole inhibits monoamine oxidase B and protects against neuronal loss and behavioral impairment in rodent models of Parkinson's disease. J Neurosci Res. 2015 Aug;93(8):1267-78. doi: 10.1002/jnr.23577. Epub 2015 Feb 24. PubMed PMID: 25711470.
15: Cada DJ, Baker DE. Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049. PubMed PMID: 25673895; PubMed Central PMCID: PMC4319806.
16: Kakkar AK, Dahiya N. Management of Parkinson׳s disease: Current and future pharmacotherapy. Eur J Pharmacol. 2015 Mar 5;750:74-81. doi: 10.1016/j.ejphar.2015.01.030. Epub 2015 Jan 28. Review. PubMed PMID: 25637088.
17: Park KD, Yang XF, Dustrude ET, Wang Y, Ripsch MS, White FA, Khanna R, Kohn H. 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. ACS Chem Neurosci. 2015 Feb 18;6(2):316-30. doi: 10.1021/cn5002182. Epub 2014 Dec 9. PubMed PMID: 25418676; PubMed Central PMCID: PMC4372064.
18: Schaeffer E, Pilotto A, Berg D. Pharmacological strategies for the management of levodopa-induced dyskinesia in patients with Parkinson's disease. CNS Drugs. 2014 Dec;28(12):1155-84. doi: 10.1007/s40263-014-0205-z. Review. PubMed PMID: 25342080.
19: Vijverman AC, Fox SH. New treatments for the motor symptoms of Parkinson's disease. Expert Rev Clin Pharmacol. 2014 Nov;7(6):761-77. doi: 10.1586/17512433.2014.966812. Review. PubMed PMID: 25318835.
20: Kandadai RM, Jabeen SA, Kanikannan MA, Borgohain R. Safinamide for the treatment of Parkinson's disease. Expert Rev Clin Pharmacol. 2014 Nov;7(6):747-59. doi: 10.1586/17512433.2014.968555. Epub 2014 Oct 10. Review. PubMed PMID: 25300164.
CAS#: 133865-89-1
Chemical Formula: C17H19FN2O2
Exact Mass: 302.1431
Molecular Weight: 302.3494
Elemental Analysis: C, 67.53; H, 6.33; F, 6.28; N, 9.27; O, 10.58
EOS Med Chem produce Safinamide, FCE 26743, 133865-89-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Safinamide, FCE 26743, 133865-89-1 Intermediates, EOS Med Chem have 8; Safinamide, FCE 26743, 133865-89-1 Impurity we have 10, all from GMP, FDA plant.
Now Safinamide, FCE 26743, 133865-89-1 DMF document is preparing.
Until 2016, Aug, Safinamide, FCE 26743, 133865-89-1 more than produced 25kg API, 120kg Intermediates
Description: 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.
Synonym: FCE-26743; FCE 26743; FCE26743; EMD-1195686; EMD 1195686; EMD1195686; Safinamide. Xadago
IUPAC/Chemical Name: (S)-2-((4-((3-fluorobenzyl)oxy)benzyl)amino)propanamide
SMILES Code: C[C@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
1: Stocchi F, Torti M. Adjuvant therapies for Parkinson's disease: critical evaluation of safinamide. Drug Des Devel Ther. 2016 Feb 5;10:609-18. doi: 10.2147/DDDT.S77749. eCollection 2016. Review. PubMed PMID: 26917951; PubMed Central PMCID: PMC4751980.
2: Cattaneo C, Sardina M, Bonizzoni E. Safinamide as Add-On Therapy to Levodopa in Mid- to Late-Stage Parkinson's Disease Fluctuating Patients: Post hoc Analysesof Studies 016 and SETTLE. J Parkinsons Dis. 2016;6(1):165-73. doi: 10.3233/JPD-150700. PubMed PMID: 26889632; PubMed Central PMCID: PMC4927927.
3: Perez-Lloret S, Rascol O. The safety and efficacy of safinamide mesylate for the treatment of Parkinson's disease. Expert Rev Neurother. 2016;16(3):245-58. doi: 10.1586/14737175.2016.1150783. Epub 2016 Feb 19. PubMed PMID: 26849427.
4: Rasheed MZ, Tabassum H, Parvez S. Mitochondrial permeability transition pore: a promising target for the treatment of Parkinson's disease. Protoplasma. 2016 Jan 29. [Epub ahead of print] PubMed PMID: 26825389.
5: Müller T. Safinamide for symptoms of Parkinson's disease. Drugs Today (Barc). 2015 Nov;51(11):653-9. doi: 10.1358/dot.2015.51.11.2414529. Review. PubMed PMID: 26744740.
6: Fabbri M, Rosa MM, Abreu D, Ferreira JJ. Clinical pharmacology review of safinamide for the treatment of Parkinson's disease. Neurodegener Dis Manag. 2015 Dec;5(6):481-96. doi: 10.2217/nmt.15.46. Epub 2015 Nov 20. PubMed PMID: 26587996.
7: Cattaneo C, Ferla RL, Bonizzoni E, Sardina M. Long-Term Effects of Safinamide on Dyskinesia in Mid- to Late-Stage Parkinson's Disease: A Post-Hoc Analysis. J Parkinsons Dis. 2015;5(3):475-81. doi: 10.3233/JPD-150569. PubMed PMID: 26406127; PubMed Central PMCID: PMC4923744.
8: Sadeghian M, Mullali G, Pocock JM, Piers T, Roach A, Smith KJ. Neuroprotection by safinamide in the 6-hydroxydopamine model of Parkinson's disease. Neuropathol Appl Neurobiol. 2016 Aug;42(5):423-35. doi: 10.1111/nan.12263. Epub 2015 Sep 25. PubMed PMID: 26300398.
9: Reichmann H. Modern treatment in Parkinson's disease, a personal approach. J Neural Transm (Vienna). 2016 Jan;123(1):73-80. doi: 10.1007/s00702-015-1441-1. Epub 2015 Aug 21. PubMed PMID: 26293352.
10: Rascol O, Perez-Lloret S, Ferreira JJ. New treatments for levodopa-induced motor complications. Mov Disord. 2015 Sep 15;30(11):1451-60. doi: 10.1002/mds.26362. Epub 2015 Aug 21. Review. PubMed PMID: 26293004.
11: Robakis D, Fahn S. Defining the Role of the Monoamine Oxidase-B Inhibitors for Parkinson's Disease. CNS Drugs. 2015 Jun;29(6):433-41. doi: 10.1007/s40263-015-0249-8. Review. PubMed PMID: 26164425.
12: Martinez-Martin P, Rodriguez-Blazquez C, Forjaz MJ, Kurtis MM. Impact of Pharmacotherapy on Quality of Life in Patients with Parkinson's Disease. CNS Drugs. 2015 May;29(5):397-413. doi: 10.1007/s40263-015-0247-x. Review. PubMed PMID: 25968563.
13: Deeks ED. Safinamide: first global approval. Drugs. 2015 Apr;75(6):705-11. doi: 10.1007/s40265-015-0389-7. Review. PubMed PMID: 25851099.
14: Chung JY, Lee JW, Ryu CH, Min HK, Yoon YJ, Lim MJ, Park CH. 1-[2-(4-Benzyloxyphenoxy)Ethyl]Imidazole inhibits monoamine oxidase B and protects against neuronal loss and behavioral impairment in rodent models of Parkinson's disease. J Neurosci Res. 2015 Aug;93(8):1267-78. doi: 10.1002/jnr.23577. Epub 2015 Feb 24. PubMed PMID: 25711470.
15: Cada DJ, Baker DE. Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049. PubMed PMID: 25673895; PubMed Central PMCID: PMC4319806.
16: Kakkar AK, Dahiya N. Management of Parkinson׳s disease: Current and future pharmacotherapy. Eur J Pharmacol. 2015 Mar 5;750:74-81. doi: 10.1016/j.ejphar.2015.01.030. Epub 2015 Jan 28. Review. PubMed PMID: 25637088.
17: Park KD, Yang XF, Dustrude ET, Wang Y, Ripsch MS, White FA, Khanna R, Kohn H. 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. ACS Chem Neurosci. 2015 Feb 18;6(2):316-30. doi: 10.1021/cn5002182. Epub 2014 Dec 9. PubMed PMID: 25418676; PubMed Central PMCID: PMC4372064.
18: Schaeffer E, Pilotto A, Berg D. Pharmacological strategies for the management of levodopa-induced dyskinesia in patients with Parkinson's disease. CNS Drugs. 2014 Dec;28(12):1155-84. doi: 10.1007/s40263-014-0205-z. Review. PubMed PMID: 25342080.
19: Vijverman AC, Fox SH. New treatments for the motor symptoms of Parkinson's disease. Expert Rev Clin Pharmacol. 2014 Nov;7(6):761-77. doi: 10.1586/17512433.2014.966812. Review. PubMed PMID: 25318835.
20: Kandadai RM, Jabeen SA, Kanikannan MA, Borgohain R. Safinamide for the treatment of Parkinson's disease. Expert Rev Clin Pharmacol. 2014 Nov;7(6):747-59. doi: 10.1586/17512433.2014.968555. Epub 2014 Oct 10. Review. PubMed PMID: 25300164.
