Ralfinamide

Ralfinamide (INN) (code names NW-1029, FCE-26742A, PNU-0154339E)[1] is a multimodal drug which is under investigation by Newron Pharmaceuticals for the treatment of neuropathic pain and other pain conditions such as post-operative dental pain.[2][3][4][5]

Ralfinamide
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.120.272
Chemical and physical data
FormulaC17H19FN2O2
Molar mass302.349 g·mol−1
3D model (JSmol)

It has a relatively complex pharmacology, acting as a mixed voltage-gated sodium channel blocker (including Nav1.7),[2][3] N-type calcium channel blocker,[2][3] noncompetitive NMDA receptor antagonist,[6] and monoamine oxidase B inhibitor.[7][8]

It has thus far progressed as far as phase IIb/phase III clinical trials.[5][9] In 2010 it failed a phase II trial for lower back pain.[10] Encouraging Phase II results have been announced for neuropathic pain.[11]

See also

References

  1. Pain: New Insights for the Healthcare Professional: 2013 Edition. ScholarlyEditions. 22 July 2013. pp. 506–. ISBN 978-1-4816-6118-8.
  2. David M. Simpson; Justin C. McArthur; Robert H. Dworkin (21 June 2012). Neuropathic Pain: Mechanisms, Diagnosis and Treatment. Oxford University Press. pp. 40–. ISBN 978-0-19-539470-2.
  3. Raymond S. Sinatra; Jonathan S. Jahr; J. Michael Watkins-Pitchford (14 October 2010). The Essence of Analgesia and Analgesics. Cambridge University Press. pp. 436–. ISBN 978-1-139-49198-3.
  4. Annual Reports in Medicinal Chemistry. Academic Press. 17 December 2008. pp. 55–. ISBN 978-0-08-092187-7.
  5. Chuang Lu; Albert P. Li (26 January 2010). Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad. John Wiley & Sons. pp. 689–. ISBN 978-0-470-53894-4.
  6. Colombo, E.; Curatolo, L.; Caccia, C.; Salvati, P.; Faravelli, L. (2007). "344 Ralfinamide Acts Through Nmda Receptor Complex: A Central Role for Chronic Pain Treatment". European Journal of Pain. 11 (S1): S152–S153. doi:10.1016/j.ejpain.2007.03.359. ISSN 1090-3801.
  7. Di Stefano AF, Radicioni MM, Rusca A (May 2013). "Pressor response to oral tyramine and monoamine oxidase inhibition during treatment with ralfinamide (NW-1029)". Neurotox Res. 23 (4): 315–26. doi:10.1007/s12640-012-9344-5. PMID 22872464.
  8. Humphrey P. Rang; Maureen M. Dale; James M. Ritter; Rod J. Flower; Graeme Henderson (14 April 2011). Rang & Dale's Pharmacology: with STUDENT CONSULT Online Access. Elsevier Health Sciences. pp. 2476–. ISBN 978-0-7020-4504-2.
  9. Valentin K. Gribkoff; Leonard K. Kaczmarek (9 December 2008). Structure, Function and Modulation of Neuronal Voltage-Gated Ion Channels. John Wiley & Sons. pp. 377–. ISBN 978-0-470-42989-1.
  10. Newron reports SERENA trial top-line results for ralfinamide
  11. Newron Announces Positive Results With Ralfinamide From Phase II Trial in Neuropathic Pain


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.