Esreboxetine
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| Other names | AXS-14; PNU-165442G |
| Routes of administration | Oral |
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| Formula | C19H23NO3 |
| Molar mass | 313.397 g·mol−1 |
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Esreboxetine (developmental code names AXS-14, PNU-165442G) is a selective norepinephrine reuptake inhibitor. It is the (S,S)-(+)-enantiomer of reboxetine and is even more selective as a norepinephrine reuptake inhibitor in comparison.[1][2]
Esreboxetine was developed by Pfizer for the treatment of neuropathic pain and fibromyalgia. It failed to show significant benefit over currently available medications and was discontinued.[1][3][4][5] A subsequent 2012 study (n=277) found esreboxetine gave significant reductions in pain and fatigue in fibromyalgia patients.[6]
References
- 1 2 Bingham M, Napier SJ (2009). Transporters as Targets for Drugs (Topics in Medicinal Chemistry). Berlin: Springer. ISBN 978-3-540-87911-4.
- ↑ Fish PV, Mackenny M, Bish G, Buxton T, Cave R, Drouard D, et al. (2009). "Enantioselective synthesis of (R)- and (S)-N-Boc-morpholine-2-carboxylic acids by enzyme-catalyzed kinetic resolution: application to the synthesis of reboxetine analogs". Tetrahedron Letters. 50 (4): 389–391. doi:10.1016/j.tetlet.2008.11.025.
- ↑ Rao SG (October 2009). "Current progress in the pharmacological therapy of fibromyalgia". Expert Opinion on Investigational Drugs. 18 (10): 1479–1493. doi:10.1517/13543780903203771. PMID 19732029. S2CID 12726987.
- ↑ "Search of esreboxetine". ClinicalTrials.gov.
- ↑ Kelly J (26 February 2009). "Pfizer Stops Work on Esreboxetine for FM". Musculoskeletal Report. New York, NY. Archived from the original on 29 February 2012.
- ↑ Arnold LM, Hirsch I, Sanders P, Ellis A, Hughes B (July 2012). "Safety and efficacy of esreboxetine in patients with fibromyalgia: a fourteen-week, randomized, double-blind, placebo-controlled, multicenter clinical trial". Arthritis and Rheumatism. 64 (7): 2387–2397. doi:10.1002/art.34390. PMID 22275142.