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zonampanel + alteplase
- Development stage
- Discontinued
- Lead developer
- Astellas Pharma
- Modality
- Recombinant Proteins and Enzymes, Small Molecules
- Administration
- Intravenous
01
Overview
Zonampanel + alteplase is an investigational combination therapy that was studied for the treatment of acute ischemic stroke. The combination consists of **zonampanel** (also known as YM872), a quinoxalinedione derivative that acts as a competitive antagonist of the AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor, and **alteplase** (t-PA), a recombinant tissue plasminogen activator. The therapy was designed to provide a synergistic effect: alteplase serves as a thrombolytic agent to dissolve blood clots and restore cerebral blood flow, while zonampanel acts as a neuroprotective agent to prevent glutamate-mediated excitotoxicity and reduce brain damage. Clinical development, including the Phase 2 ARTIST+ trial, was terminated early by Astellas Pharma due to the observation of severe neuropsychiatric side effects associated with zonampanel, such as hallucinations, agitation, and catatonia.
- Brand names
- Activase
- Other names
- YM872 + alteplaseYM872 + t-PAARTIST+
02
Targets
FGG (Fibrinogen gamma chain)FGA (Fibrinogen alpha chain)AMPAR (AMPA receptor)PLG (Plasminogen)ABCC4 (Multidrug resistance-associated protein 4)
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