THERAPY DOSSIER · th-818e1a975e21

S-ketamine (optically pure); charybdotoxin as comparator channel blocker

Drug · Glutamate [NMDA] receptor negative allosteric modulator (NEGATIVE ALLOSTERIC MODULATOR); noncompetitive binding to NMDA glutamate receptors, NMDA subtype non-selective

Non-drug Suggest a correction

Evidence & regulatory context

Mechanism: Glutamate [NMDA] receptor negative allosteric modulator (NEGATIVE ALLOSTERIC MODULATOR); noncompetitive binding to NMDA glutamate receptors, NMDA subtype non-selective
Target: CHEMBL2094124
Injury models: Other
Reported indication: Not recorded
First approval: 2019
Development stage: Not recorded
ChEMBL record: Not recorded
ChEMBL max phase: 4 / 4 (development scale, not regulatory approval)
Synonyms: Esketamina; Esketamine; JNJ-54135419; (-)-ketamine; S-(-)-ketamine; S-ketamine; L-ketamine; Ketanest S; Spravato
Note: Not recorded

Clinical trials 9

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

NCT04548973 ↗PHASE4completed

Multicenter Study of the Efficacy and Safety of Esketamine for Analgesia

Fetal or Neonatal Effect of Damage to Placenta From Caesarean Section

Enrolment: 600 · Results not recorded

NCT04303325 ↗PHASE4unknown

Effect of Esketamine on Postoperative Depression, Gut Microbiota and BIS Data in Breast Cancer Surgery (ESPOD-BI)

Depression

Enrolment: 72 · Results not recorded

NCT05950646 ↗PHASE4completed

Mini-dose Dexmedetomidine-Esketamine Infusion on Sleep Quality in Older Patients Undergoing Knee or Hip Replacement

Old Age · Knee Replacement Surgery · Hip Replacement Surgery · Sleep Quality

Enrolment: 154 · Results not recorded

NCT02918318 ↗PHASE2completed

Fixed Doses of Intranasal Esketamine in Japanese Subjects With Treatment Resistant Depression

Depression

Enrolment: 202 · Results not recorded

NCT04745286 ↗EARLY_PHASE1unknown

Effects of Small-dose S-ketamine on Anesthesia-induced Atelectasis Under General Anesthesia

Atelectasis

Enrolment: 100 · Results not recorded

NCT04860661 ↗NAcompleted

Effect of Prophylactic Esketamine on Postpartum Depression in Cesarean Section

Postpartum Depression

Enrolment: 336 · Results not recorded

NCT05582135 ↗NAcompleted

Epidural Esketamine and Morphine for Postoperative Analgesia After Caesarean Delivery: A Pilot Study

Analgesia

Enrolment: 119 · Results not recorded

NCT06432322 ↗NAcompleted

Effects of Esketamine Challenge on Brain Glutamate Release, Resting State Connectivity and Neuroplasticity

Depression

Enrolment: 16 · Results not recorded

NCT06900205 ↗NAwithdrawn

Effects of Esketamine on Postoperative Delirium and Sleep Disturbance After Major Non-cardiac Surgery

Postoperative Delirium (POD) · Postoperative Sleep Disturbance

Enrolment: 0 · Results not recorded

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 22131399 ↗2011Reported benefit

Microglial Ca(2+)-activated K(+) channels are possible molecular targets for the analgesic effects of S-ketamine on neuropathic pain.

MouseOtherTransgenic mice (line not stated) and cultured microgliaMaleIntrathecal administration used for charybdotoxin; route for S-ketamine not stated in abstractDuring development of tactile allodynia after nerve injury

Model: Peripheral (spinal) nerve injury producing tactile allodynia and spinal microglial hyperactivation

S-ketamine preferentially suppressed nerve injury-induced tactile allodynia and spinal microglial hyperactivation and inhibited BK currents induced by nerve injury or NS1619. Intrathecal charybdotoxin inhibited allodynia, P2X4 receptor expression and brain-derived neurotrophic factor synthesis. NS1…

Extraction: extract · Supplied extraction confidence: 0.55. Machine-extracted fields require source verification.

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