THERAPY DOSSIER · th-099ba4258ef4

Lomerizine hydrochloride, YM872 (zonampanel monohydrate) and oxidised ATP (oxATP), alone and in combination

Drug · Glutamate receptor ionotropic AMPA antagonist (competitive antagonist, direct interaction)

Evidence & regulatory context

Mechanism: Glutamate receptor ionotropic AMPA antagonist (competitive antagonist, direct interaction)
Target: CHEMBL2096670 (ionotropic glutamate receptor, AMPA)
Injury models: Other
Reported indication: Not recorded
First approval: Not recorded
Development stage: In trials, not approved
ChEMBL record: CHEMBL119625 ↗
ChEMBL max phase: 2 / 4 (development scale, not regulatory approval)
Synonyms: YM 872; YM-872; YM872; Zonampanel; Zonampanel monohydrate
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.

NCT00044057 ↗PHASE2completed

Neurologic Function and Disability in Acute Ischemic Stroke Given tPA Plus YM872 or tPA Plus Placebo

Acute Ischemic Stroke

Enrolment not recorded · Results not recorded

NCT00044070 ↗PHASE2completed

Effects of YM872 on Lesion Volume by Diffusion, Perfusion and FLAIR MRI in Acute Ischemic Stroke

Cerebrovascular Accident

Enrolment not recorded · Results not recorded

Preclinical evidence 1

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

PMID 28806920 ↗2017Mixed findings

Specific ion channels contribute to key elements of pathology during secondary degeneration following neurotrauma.

RatOtherPiebald Virol Glaxo (PVG)Femalen = Three cohorts: cohort 1 n = 30 (10 per group), cohort 2 n =…Lomerizine orally in butter; oxATP and YM872 by subcutaneously implanted mini-osmotic pump (Alzet Model 2002) with cannula targeting the injured dorsal optic nerveLomerizine 30 mg/kg; oxATP 1 mM and YM872 240 micromolar di…Treatment began on the day of surgery after full recovery from anaesthesia

Model: Partial transection of the dorsal right optic nerve approximately 1 mm behind the eye to a controlled depth of 200 micrometres using a diamond radial keratotomy knife, modelling secondary degeneration in ventral optic nerve

Partial optic nerve transection acutely increased Tau phosphorylation and acetylated tubulin and decreased NogoA in ventral nerve vulnerable to secondary degeneration. At day 3 all inhibitor combinations reduced phosphorylated Tau ratios, increased NogoA and shortened the paranodal gap. Only Lomeri…

Extraction: extract · Supplied extraction confidence: 0.92. Machine-extracted fields require source verification.

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