Small molecule
PubChem CID 182137
Esketamine
Spravato
- Mechanism of action
- Non-competitive NMDA receptor antagonist
- In plain language
- Blocks a brain receptor called NMDA that's involved in mood and nerve-cell communication, though doctors don't fully know why blocking it relieves depression.
- How it works
- Esketamine, the S-enantiomer of racemic ketamine, is a non-selective, non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, an ionotropic glutamate receptor. Its major circulating metabolite, noresketamine, acts at the same receptor but with lower affinity. Per the FDA label, the mechanism by which NMDA receptor antagonism produces esketamine's antidepressant effect has not been established — the clinical benefit is observed, but the causal chain from receptor binding to mood improvement, better characterized for older antidepressant classes, remains an open question here.
- Therapeutic applications
- Indicated for treatment-resistant depression (TRD) in adults, as monotherapy or in conjunction with an oral antidepressant, and for depressive symptoms in adults with major depressive disorder (MDD) accompanied by acute suicidal ideation or behavior, used in conjunction with an oral antidepressant. The FDA label notes that esketamine's effectiveness in preventing suicide or reducing suicidal ideation itself has not been demonstrated.
- Class
- Small molecule
- Therapeutic area
- CNS / Psychiatric
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