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ezogabine MR1
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ezogabine MR1 is an experimental modified-release formulation of ezogabine (also known as retigabine), a first-in-class potassium channel opener. Developed by GSK, this formulation was one of five prototypes (MR1-MR5) evaluated in Phase 1 clinical trials to optimize the pharmacokinetic profile of the drug, which originally required three-times-daily dosing in its immediate-release form. Ezogabine acts as a positive allosteric modulator of KCNQ2-5 (Kv7.2-7.5) voltage-gated potassium channels, stabilizing the neuronal membrane potential and reducing hyperexcitability. While the immediate-release version (Potiga/Trobalt) was approved for the treatment of partial-onset seizures, it was later withdrawn from the market due to safety concerns regarding skin and retinal pigmentation. Consequently, the development of the modified-release formulations, including MR1, was discontinued.
- Other names
- ezogabine modified release prototype 1retigabine modified release prototype 1
02
Targets
KCNQ5 (Potassium voltage-gated channel subfamily KQT member 5)KCNQ2 (Potassium voltage-gated channel subfamily KQT member 2)KCNQ3 (Potassium voltage-gated channel subfamily Q member 3)KCNQ4 (Potassium channel subfamily KQT member 4)
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