Ralfinamide Explained

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]}

It has a relatively complex pharmacology, acting as a mixed voltage-gated sodium channel blocker (including Na_v1.7), N-type calcium channel blocker, 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.^[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

• List of investigational analgesics
• Safinamide, different fluorine position
• Evenamide, structurally-related antipsychotic in development
• Lacosamide, used for partial-onset seizures and diabetic neuropathic pain
• Ziconotide, FDA approved peptide for chronic neuropathic pain

External links

• Ralfinamide - Newron Pharmaceuticals

Notes and References

1. Book: Action A . Chapter 8: Therapies and Treatments . Pain: New Insights for the Healthcare Professional . 2013 . https://books.google.com/books?id=RViI916bD-IC&pg=PA506 . 22 July 2013 . ScholarlyEditions . 978-1-4816-6118-8. 506–.
2. Book: Gilron I . Simpson DM, McArthur JC, Dworkin RH . Drug Discovery for Neuropathic Pain . https://books.google.com/books?id=1fF7pRxFzZUC&pg=PA40 . Neuropathic Pain: Mechanisms, Diagnosis and Treatment . 21 June 2012. Oxford University Press. 978-0-19-539470-2. 40–.
3. Book: Rodger IW, Lacouture PG . Overview: Novel Targets for New Analgesics . Sinatra RS, Jahr JS, Watkins-Pitchford JM . The Essence of Analgesia and Analgesics . https://books.google.com/books?id=ZwPIjKg0XukC&pg=PA436 . 14 October 2010. Cambridge University Press. 978-1-139-49198-3. 436–.
4. Book: Termin A, Martinborough E, Wilson D . Recent Advances in Voltage-Gated Sodium Chanel Blockers: Therapeutic Potential as Drug Targets in the CNS . Annual Reports in Medicinal Chemistry. https://books.google.com/books?id=uVjF7DQswzkC&pg=PA55. 17 December 2008. Academic Press. 978-0-08-092187-7. 55–.
5. Book: Liu Y, Qin N . Pharacological Modulation of Ion Channels for the Treatment of Chronic Pain . Lu C, Li AP . Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad. https://books.google.com/books?id=GS_98F19H74C&pg=PA689. 26 January 2010. John Wiley & Sons. 978-0-470-53894-4. 689–.
6. Colombo E, Curatolo L, Caccia C, Salvati P, Faravelli L . 344 Ralfinamide Acts Through Nmda Receptor Complex: A Central Role for Chronic Pain Treatment. European Journal of Pain. 11. S1. 2007. S152–S153. 1090-3801. 10.1016/j.ejpain.2007.03.359. 58186567.
7. Di Stefano AF, Radicioni MM, Rusca A . Pressor response to oral tyramine and monoamine oxidase inhibition during treatment with ralfinamide (NW-1029) . Neurotoxicity Research . 23 . 4 . 315–326 . May 2013 . 22872464 . 10.1007/s12640-012-9344-5 . 207442119 .
8. Book: Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson G . Rang & Dale's Pharmacology: with STUDENT CONSULT Online Access. 14 April 2011. Elsevier Health Sciences. 978-0-7020-4504-2. 2476–.
9. Book: Bowlby MR, Kaftan . Sodium Channel Blockers for the Treatment of Chronic Pain . Gribkoff VK, Kaczmarek LK . Structure, Function and Modulation of Neuronal Voltage-Gated Ion Channels. https://books.google.com/books?id=0MKlV3tuoEMC&pg=PA377. 9 December 2008. John Wiley & Sons. 978-0-470-42989-1. 377–.
10. Web site: Newron reports SERENA trial top-line results for ralfinamide . https://web.archive.org/web/20150924120655/https://www.bloomberg.com/apps/news?pid=conewsstory&tkr=NP5:GR&sid=af0gKdEDHRDA . 24 September 2015 . Bloomberg . 6 May 2010 .
11. Web site: Newron Announces Positive Results With Ralfinamide From Phase II Trial in Neuropathic Pain . https://web.archive.org/web/20150220072424/http://www.prnewswire.com/news-releases/newron-announces-positive-results-with-ralfinamide-from-phase-ii-trial-in-neuropathic-pain-74976442.html . 20 February 2015 . PR Newswire . 26 October 2014 .