Drug intelligence / Profile preview

zonampanel

Development stage
Phase 2
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Intravenous
01

Overview

Zonampanel is a small molecule quinoxalinedione derivative that acts as a selective and competitive antagonist of the α-amino‑3‑hydroxy‑5‑methylisoxazole‑4‑propionic acid (AMPA) receptor. It was developed as a neuroprotective agent for the treatment of acute ischemic stroke and cerebral ischemia. Zonampanel blocks glutamatergic neurotransmission at AMPA receptors to reduce excitotoxic neuronal damage during ischemic events. Clinical development was discontinued after phase 2 trials due to severe central nervous system side effects such as hallucinations and catatonia[1][8]. The drug is primarily excreted unchanged in urine via renal organic anion transporters[6][9].

Other names
zonampanel anhydrouszonampanel monohydrate(2,3-dioxo-7-(1H-imidazol-1-yl)-6-nitro-1,2,3,4-tetrahydro-1-quinoxalinyl)acetic acid monohydrate2-[7-(1H-imidazol-1-yl)-6-nitro-2,3-dioxo–1,2,3,4-tetrahydroquinoxalin–1–yl]acetic acidCHEMBL119625CHEMBL-119625CHEMBL 119625
02

Targets

AMPAR (AMPA receptor)

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