Esreboxetine

Esreboxetine is a norepinephrine reuptake inhibitor (NRI) that was under development by Pfizer for the treatment of neuropathic pain and fibromyalgia but was discontinued during phase III clinical trials due to a lack of efficacy.

Chemistry

Esreboxetine is the (S,S)-stereoisomer of reboxetine. The chemical name of esreboxetine is (S,S)-2-((S)-alpha-(2-ethoxyphenoxy)benzyl)morpholine methanesulfonate.

Pharmacology

Esreboxetine acts as a highly selective norepinephrine reuptake inhibitor. It is approximately 1,000 times more selective for norepinephrine reuptake inhibition than for serotonin and is inactive at histamine, dopamine, alpha1-, alpha2-, and beta-adrenergic; muscarinic; serotonin1; serotonin2; and dopamine2 receptors.

Clinical trials

Esreboxetine was under development for the treatment of neuropathic pain and fibromyalgia but was discontinued during phase III clinical trials due to a lack of efficacy. The results of a phase II trial in peripheral neuropathy were published in 2007.

See also

• List of investigational analgesics

References

Esreboxetine Resources
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