Drug intelligence / Profile preview

esketamine

Development stage
Approved
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Intranasal, Intravenous, Intramuscular
01

Overview

Esketamine is the S-enantiomer of ketamine and acts as a non-selective, non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, an ionotropic glutamate receptor. It is approved as a nasal spray for adults with treatment-resistant depression (TRD) and for major depressive disorder (MDD) with acute suicidal ideation or behavior. Esketamine produces rapid antidepressant effects by blocking NMDA receptors on GABAergic interneurons, leading to increased glutamate release and enhanced synaptogenesis in brain regions involved in mood regulation. This mechanism also stimulates neurotrophic factor signaling and restores dopaminergic neurotransmission related to motivation and reward. Esketamine was developed by Janssen Pharmaceuticals and is marketed under the brand name Spravato for depression; it is also known as Ketanest when used as an anesthetic in some countries[1][2][5][6][8].

Brand names
SpravatoKetanest
Other names
S-ketamine(S)-ketamine
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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