Safinamide

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Structural formula
Structural formula of safinamide
General
Surname Safinamide
other names

(S) -2- [4- (3-fluorobenzyloxy) benzylamino] propionamide ( IUPAC )

Molecular formula C 17 H 19 FN 2 O 2
External identifiers / databases
CAS number 133865-89-1
EC number 603-772-2
ECHA InfoCard 100.120.167
PubChem 131682
ChemSpider 116349
DrugBank DB06654
Wikidata Q2211523
properties
Molar mass 302.34 g mol −1
safety instructions
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Safinamid is the international non-proprietary name for an approved active ingredient for the treatment of Parkinson's disease . From a chemical point of view, it is an α-aminoamide derivative .

Working principle

Safinamide is a monoamine oxidase B inhibitor (see monoamine oxidase inhibitors ). The substance is said to act as a dopamine and glutamate modulator. Safinamide should enable both selective and reversible MAO-B inhibition, as well as blockade of dopamine reuptake. In clinical studies that the two key mechanisms for the control of dopamine concentration was shown brain glutamate and dopamine reuptake by inhibiting the MAO-B activity - - may be affected. In addition to reversibly inhibiting MAO-B, safinamide blocks the voltage-dependent sodium and calcium channels .

Safinamide is used as an adjunct therapy to levodopa in Parkinson's disease in mid- to late-stage patients with fluctuations.

Development history

Safinamide was originally invented by the Italian pharmaceutical company Farmitalia Carlo Erba . In 1993 Farmitalia was taken over by Pharmacia . Two years later, Upjohn and Pharmacia merged to become Pharmacia & Upjohn . In 1998 - the company was now called Pharmacia Corporation - a worldwide restructuring program of the company followed, in which the newly founded company Newron Pharmaceuticals obtained all rights to safinamide (then still known as PNU15774E). In 2006, Newron reached an agreement with Merck KGaA that the exclusive worldwide rights to develop, manufacture and market safinamide would go to Merck. These exclusive rights related to Parkinson's disease, Alzheimer's disease and other diseases. On October 21, 2011, Merck announced that it would return the exclusive rights to Newron in April 2012. The decision was justified with the prioritization of projects and a - compared to earlier assessments - lower market potential of safinamide.

Current situation of admission

The first application for approval to the FDA was rejected in early August 2014 due to formal errors in the approval application. The application was re-submitted to the FDA in late December 2016. In March 2017, approval was granted by the FDA. Safinamide was recommended for approval by the European Medicines Agency in December 2014 , which was granted by the European Commission in spring 2015. The drug is currently being marketed in Germany under the trade name Xadago . Authorization was also applied for to Swissmedic in April 2014 ; any authorization is still pending.

further reading

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ^ RG Fariello: Safinamide. In: Neurotherapeutics . Volume 4, No. 1, January 2007, pp. 110-116, doi: 10.1016 / j.nurt.2006.11.011 , PMID 17199024 (Review).
  3. ↑ a b c Promising data on the cognitive effects of safinamide in early-stage Parkinson's disease. (PDF; 187 kB) Merck Serono press release dated June 8, 2007
  4. ↑ C. Caccia, R. Maj, M. Calabresi, S. Maestroni, L. Faravelli, L. Curatolo, P. Salvati, RG Fariello: Safinamide: from molecular targets to a new anti-Parkinson drug. In: Neurology . Volume 67, No. 7 Suppl 2, October 2006, pp. S18-S23, PMID 17030736 (review).
  5. ↑ Paolo Pevarello, Alberto Bonsignori, Philippe Dostert, Franco Heidempergher, Vittorio Pinciroli, Maristella Colombo, Robert A. McArthur, Patricia Salvati, Claes Post, Ruggero G. Fariello, Mario Varasi: Synthesis and Anticonvulsant Activity of a New Class of 2- [ (Arylalkyl) amino] alkanamide derivatives . In: Journal of Medicinal Chemistry . tape 41 , no. 4 , 1998, pp. 579-590 , doi : 10.1021 / jm970599m .
  6. ↑ Safinamide: FCE 26743, NW 1015, PNU 151774, PNU 151774E. In: Drugs in R&D. Volume 5, No. 6, 2004, pp. 355-358, PMID 15563241 (review).
  7. ↑ Merck: Main results of the long-term study with safinamide as an adjunct therapy to levodopa in Parkinson's in advanced stages. Press release. In: lifepr.de. Merck, November 4, 2010, accessed November 25, 2017 .
  8. ↑ Merck KGaA returns safinamide rights to Newron. In: Berliner Morgenpost. October 21, 2011
  9. ^ Newron information about FDA Refusal to File Newron press release of July 29, 2014
  10. ↑ Newron information on the re-filing of the approval application for safinamides with the FDA Newron press release dated December 29, 2014
  11. ↑ Newron: Safinamide Receives FDA Approval for Parkinson's Disease | 03/21/17 | finanzen.ch . In: finanzen.ch . ( finanzen.ch [accessed on March 22, 2017]).
  12. ↑ Summary of the EPAR for the public - Xadago Summary of the Xadago approval from EMA