Esreboxetine

Esreboxetine.svg

Esreboxetine is a selective norepinephrine reuptake inhibitor (NRI) that was being developed as a potential treatment for major depressive disorder (MDD) and attention deficit hyperactivity disorder (ADHD). It is the (S,S)-enantiomer of reboxetine, which is a racemic mixture used as an antidepressant.

Pharmacology

Esreboxetine works by inhibiting the reuptake of norepinephrine (NE) into the presynaptic neuron, thereby increasing the concentration of norepinephrine in the synaptic cleft. This action is believed to contribute to its antidepressant and cognitive-enhancing effects. Unlike some other antidepressants, esreboxetine has minimal effects on the reuptake of serotonin and dopamine.

Clinical Development

Esreboxetine was investigated in clinical trials for the treatment of major depressive disorder and attention deficit hyperactivity disorder. However, its development was discontinued due to insufficient efficacy in clinical trials compared to existing treatments.

Side Effects

The side effects of esreboxetine are similar to those of other norepinephrine reuptake inhibitors. Common side effects include:

• Insomnia
• Dry mouth
• Constipation
• Increased heart rate
• Hypertension

Comparison with Reboxetine

Esreboxetine is the (S,S)-enantiomer of reboxetine, which means it is a more selective form of the drug. Reboxetine is a racemic mixture containing both (R,R)- and (S,S)-enantiomers. The (S,S)-enantiomer is believed to be more pharmacologically active, which led to the development of esreboxetine as a potentially more effective treatment.

Discontinuation

Despite initial promise, esreboxetine was discontinued in clinical development. The decision was based on the results of clinical trials that did not demonstrate a significant advantage over existing treatments for major depressive disorder and attention deficit hyperactivity disorder.

See Also

• Norepinephrine reuptake inhibitor
• Reboxetine
• Major depressive disorder
• Attention deficit hyperactivity disorder

External Links

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