Drug intelligence / Profile preview

retigabine

Development stage
Phase 3
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Retigabine (also known as ezogabine in the US) is a unique anticonvulsant that was primarily used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. It has a distinctive mechanism of action compared to other antiepileptic drugs, working primarily as a potassium channel opener by activating voltage-gated potassium channels (Kv7.2-7.5, formerly KCNQ2-5) in the brain. This mechanism enables generation of the M-current, stabilizes the membrane potential, and controls neuronal excitability. Additionally, it may affect GABA neurotransmission by enhancing the GABA-A receptor. Developed by Valeant Pharmaceuticals and GlaxoSmithKline, it was approved in 2011 but discontinued globally in June 2017 due to serious side effects, including a black box warning related to risks of retinal abnormalities, potential vision loss, and blue discoloration of the skin, nail, mucous membrane, and eyes.

Brand names
TrobaltPotiga
Other names
ezogabine
02

Targets

GABRR (GABA-A receptor subunit rho)KCNQ4 (Potassium channel subfamily KQT member 4)

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