Esreboxetine

In this article, we will explore in depth the topic of Esreboxetine, a fundamental aspect that crosses various areas of daily life. We will delve into its origins, its evolution over the years and its relevance today. Through a detailed and exhaustive analysis, we will examine the different approaches and perspectives that exist around Esreboxetine, as well as its implications in the social, cultural, economic and political spheres. Likewise, we will stop to examine how Esreboxetine has impacted the way we perceive the world around us, and how it has shaped our interactions and relationships with other individuals. Throughout these pages, we propose to delve into all the aspects of Esreboxetine, with the aim of shedding light on a topic of great relevance in contemporary times.

Esreboxetine
Clinical data
Other namesAXS-14; PNU-165442G
Routes of
administration		Oral
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • (2S)-2-morpholine
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H23NO3
Molar mass313.397 g·mol−1
3D model (JSmol)
  • CCOC1=CC=CC=C1O(2CNCCO2)C3=CC=CC=C3
  • InChI=1S/C19H23NO3/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18/h3-11,18-20H,2,12-14H2,1H3/t18-,19-/m0/s1 ☒N
  • Key:CBQGYUDMJHNJBX-OALUTQOASA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Esreboxetine (developmental code names AXS-14, PNU-165442G) is a selective norepinephrine reuptake inhibitor which was under development by Pfizer for the treatment of neuropathic pain and fibromyalgia but failed to show significant benefit over currently available medications and was discontinued.[1][2][3][4] It is the (S,S)-(+)-enantiomer of reboxetine and is even more selective as a norepinephrine reuptake inhibitor in comparison.[1][5]

However, recently it has been found that esreboxetine could be effective in fibromyalgia patients.[6]

References

  1. ^ a b Bingham M, Napier SJ (2009). Transporters as Targets for Drugs (Topics in Medicinal Chemistry). Berlin: Springer. ISBN 978-3-540-87911-4.
  2. ^ 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.
  3. ^ "Search of esreboxetine". ClinicalTrials.gov.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.


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