Drug intelligence / Profile preview

midafotel

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

**Midafotel (SDZ EAA 494)** is a potent, competitive antagonist of the **N-methyl-D-aspartate (NMDA) receptor**. The drug displays strong selectivity and affinity for the NMDA receptor, with minimal activity on other neurotransmitter systems[1][7][8][10]. It was developed by **Sandoz** for the treatment of disorders such as epilepsy and for potential neuroprotective effects in conditions like cerebral ischemia and brain trauma[1][4][8]. Its primary mechanism involves blocking excitatory neurotransmission mediated by glutamate at the NMDA receptor, which is implicated in synaptic plasticity, memory formation, and neurotoxicity under pathological conditions. Despite promising pharmacology and efficacy in animal models (notably anticonvulsant and anti-ischemic effects), clinical trials in patients with refractory epilepsy were unsuccessful due to significant CNS-related adverse effects (e.g., sedation, ataxia, poor concentration, amnesia, depression, dysarthria)[4][1]. The development of midafotel was discontinued after lack of efficacy and risk-benefit concerns in clinical testing[4][8].

Other names
D-CPPeneSDZ EAA-494Midafotel
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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