Drug intelligence / Profile preview

XEN393

Development stage
Discontinued
Lead developer
Xenon Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

XEN393 is a **novel, selective small molecule inhibitor** that targets the voltage-gated sodium channels **NaV1.2 and NaV1.6**. It was developed to selectively block these channels, which are abundantly expressed in excitatory neurons and implicated in certain forms of epilepsy, while sparing NaV1.1 and NaV1.3, thereby reducing adverse effects associated with nonselective sodium channel blockade[1][3][4]. Preclinical studies demonstrated that XEN393 was highly potent (IC50 ≈ 0.005 µM for NaV1.2 and 0.01 µM for NaV1.6), prevented electrically induced seizures in both mice and rats, and had good brain tolerability, suggesting potential use as an antiseizure drug for specific epileptic syndromes such as EIEE11 (NaV1.2 gain-of-function)[1][4]. However, development for epilepsy and other nervous system diseases was **discontinued** before clinical trials commenced[3].

Brand names
XEN393XEN-393XEN 393
Other names
XEN393XEN-393XEN 393
02

Targets

SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN5A (Sodium channel protein type 5 subunit alpha)SCN8A (NaV1.6)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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