Chemistry:Ralfinamide
From HandWiki
Short description: Investigational analgesic drug
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| Formula | C17H19FN2O2 |
| Molar mass | 302.349 g·mol−1 |
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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 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
- 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
References
- ↑ "Chapter 8: Therapies and Treatments". Pain: New Insights for the Healthcare Professional (2013 ed.). ScholarlyEditions. 22 July 2013. pp. 506–. ISBN 978-1-4816-6118-8. https://books.google.com/books?id=RViI916bD-IC&pg=PA506.
- ↑ 2.0 2.1 2.2 "Drug Discovery for Neuropathic Pain". Neuropathic Pain: Mechanisms, Diagnosis and Treatment. Oxford University Press. 21 June 2012. pp. 40–. ISBN 978-0-19-539470-2. https://books.google.com/books?id=1fF7pRxFzZUC&pg=PA40.
- ↑ 3.0 3.1 3.2 "Overview: Novel Targets for New Analgesics". The Essence of Analgesia and Analgesics. Cambridge University Press. 14 October 2010. pp. 436–. ISBN 978-1-139-49198-3. https://books.google.com/books?id=ZwPIjKg0XukC&pg=PA436.
- ↑ "Recent Advances in Voltage-Gated Sodium Chanel Blockers: Therapeutic Potential as Drug Targets in the CNS". Annual Reports in Medicinal Chemistry. Academic Press. 17 December 2008. pp. 55–. ISBN 978-0-08-092187-7. https://books.google.com/books?id=uVjF7DQswzkC&pg=PA55.
- ↑ 5.0 5.1 "Pharacological Modulation of Ion Channels for the Treatment of Chronic Pain". Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad. John Wiley & Sons. 26 January 2010. pp. 689–. ISBN 978-0-470-53894-4. https://books.google.com/books?id=GS_98F19H74C&pg=PA689.
- ↑ "344 Ralfinamide Acts Through Nmda Receptor Complex: A Central Role for Chronic Pain Treatment". European Journal of Pain 11 (S1): S152–S153. 2007. doi:10.1016/j.ejpain.2007.03.359. ISSN 1090-3801.
- ↑ "Pressor response to oral tyramine and monoamine oxidase inhibition during treatment with ralfinamide (NW-1029)". Neurotoxicity Research 23 (4): 315–326. May 2013. doi:10.1007/s12640-012-9344-5. PMID 22872464.
- ↑ Rang & Dale's Pharmacology: with STUDENT CONSULT Online Access. Elsevier Health Sciences. 14 April 2011. pp. 2476–. ISBN 978-0-7020-4504-2. https://books.google.com/books?id=s2R-ZYz_iBYC&pg=PT2476.
- ↑ "Sodium Channel Blockers for the Treatment of Chronic Pain". Structure, Function and Modulation of Neuronal Voltage-Gated Ion Channels. John Wiley & Sons. 9 December 2008. pp. 377–. ISBN 978-0-470-42989-1. https://books.google.com/books?id=0MKlV3tuoEMC&pg=PA377.
- ↑ "Newron reports SERENA trial top-line results for ralfinamide". Bloomberg. 6 May 2010. https://www.bloomberg.com/apps/news?pid=conewsstory&tkr=NP5:GR&sid=af0gKdEDHRDA.
- ↑ "Newron Announces Positive Results With Ralfinamide From Phase II Trial in Neuropathic Pain". PR Newswire. 26 October 2014. http://www.prnewswire.com/news-releases/newron-announces-positive-results-with-ralfinamide-from-phase-ii-trial-in-neuropathic-pain-74976442.html.
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