Ralfinamide
Not to be confused with Rufinamide.
 | |
| Systematic (IUPAC) name | |
|---|---|
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N2-{4-[(2-Fluorobenzyl)oxy]benzyl}-L-alaninamide | |
| Identifiers | |
| CAS Number | 133865-88-0 |
| ATC code | None |
| PubChem | CID 5745207 |
| ChemSpider | 4676525 |
| Chemical data | |
| Formula | C17H19FN2O2 |
| Molar mass | 302.343 g/mol |
| |
| |
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
- 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
- ↑ Pain: New Insights for the Healthcare Professional: 2013 Edition. ScholarlyEditions. 22 July 2013. pp. 506–. ISBN 978-1-4816-6118-8.
- 1 2 3 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.
- 1 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.
- ↑ Annual Reports in Medicinal Chemistry. Academic Press. 17 December 2008. pp. 55–. ISBN 978-0-08-092187-7.
- 1 2 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.
- ↑ 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.
- ↑ 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.
- ↑ 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 0-7020-4504-7.
- ↑ 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.
- ↑ Newron reports SERENA trial top-line results for ralfinamide
- ↑ Newron Announces Positive Results With Ralfinamide From Phase II Trial in Neuropathic Pain
External links
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