Drug intelligence / Profile preview

selfotel

Development stage
Discontinued
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Selfotel** is a small molecule drug that acts as a **competitive antagonist of the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor**[1][3][6][7]. Chemically, it is a racemic mixture with the name (+/−)-cis-4-(phosphonomethyl)2-piperidine carboxylic acid, a rigid analog of 2-amino-5-phosphonopentanoic acid (AP5)[1]. Selfotel directly inhibits postsynaptic NMDA glutamate receptors, unlike noncompetitive NMDA antagonists such as ketamine and phencyclidine, and thus does not display dopaminergic side effects[1]. It was primarily developed as a neuroprotectant for **stroke, brain injuries, and cognition disorders**, but clinical development was discontinued due to limited efficacy and evidence of neurotoxicity, particularly increased mortality in severe stroke and head injury patients[2][3][5]. Preclinical and clinical studies showed neuroprotection in CNS injury models and attenuation of glutamate increases after trauma, but also dose-dependent CNS side effects (agitation, hallucinations, delirium)[1][4][6].

Other names
CGS 19755CGS19755CGS-19755sefotelselfotel
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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