THERAPY DOSSIER · th-bce16dec26c0

LY293558 combined with caramiphen, given with atropine and HI-6

Drug · LY293558 (tezampanel) is an AMPA/kainate ionotropic glutamate receptor antagonist (combination also includes caramiphen, atropine and HI-6).

Not approved Suggest a correction

Evidence & regulatory context

Mechanism: LY293558 (tezampanel) is an AMPA/kainate ionotropic glutamate receptor antagonist (combination also includes caramiphen, atropine and HI-6).
Target: AMPA receptor (CHEMBL2096670); kainate receptor (CHEMBL2109241)
Injury models: Chemical/toxin
Reported indication: Not recorded
First approval: Not recorded
Development stage: In trials, not approved
ChEMBL record: CHEMBL14935 ↗
ChEMBL max phase: 2 / 4 (development scale, not regulatory approval)
Synonyms: LY293558; Tezampanel; NGX424
Note: Not recorded

Clinical trials 2

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

NCT00567086 ↗PHASE2completed

Single subcutaneous dose of tezampanel (LY293558) in patients with acute migraine

Migraine

Enrolment: 306 · Results not recorded

NCT06538558 ↗PHASE1recruiting

Tezampanel for opioid withdrawal syndrome in opioid use disorder

Opioid Use Disorder

Enrolment: 40 · Results not recorded

Preclinical evidence 1

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

PMID 29713995 ↗2018Reported benefit

Full Protection Against Soman-Induced Seizures and Brain Damage by LY293558 and Caramiphen Combination Treatment in Adult Rats.

RatChemical/toxinSprague-DawleyMaleInjection (route not stated in abstract)LY293558 15 mg/kg; caramiphen 50 mg/kg20 min after soman exposure

Model: Acute soman exposure at 1.2 x LD50 inducing status epilepticus and brain damage

LY293558 plus caramiphen terminated status epilepticus faster than LY293558 alone, prevented seizure return over 72 h of monitoring and spontaneous recurrent seizures at day 7, produced no detectable neurodegeneration, and body weight loss and recovery matched unexposed controls.

Extraction: extract · Supplied extraction confidence: 0.8. Machine-extracted fields require source verification.

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