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r-ketamine
- Development stage
- Phase 2
- Lead developer
- Perception Neuroscience
- Modality
- Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Intramuscular
01
Overview
r-Ketamine (arketamine) is the R-enantiomer of ketamine, a chiral cyclohexanone-derived compound. Unlike racemic ketamine or S-ketamine (esketamine), r-ketamine is under investigation for its rapid-acting and sustained antidepressant effects with fewer dissociative and psychotomimetic side effects. Its mechanism of action primarily involves antagonism of the N-methyl-D-aspartate receptor (NMDA receptor), but it also enhances neuroplasticity through increased glutamate release, AMPA receptor activation, BDNF-TrkB signaling, and downstream pathways such as MEK-ERK-CREB. Preclinical studies suggest additional anti-inflammatory properties and potential benefits in neurodegenerative disorders. Clinical trials have shown efficacy in treatment-resistant depression and bipolar depression; however, some recent studies have failed to meet primary endpoints despite promising post hoc results. Compared to S-ketamine or racemic ketamine, r-ketamine may offer longer-lasting antidepressant effects with lower risk of abuse or cognitive impairment[2][3][5][6][7].
- Other names
- arketamine(R)-(-)-ketamine
02
Targets
NMDAR (Glutamate receptor ionotropic, NMDA)
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