Drug intelligence / Profile preview

tonabersat

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Tonabersat is a small molecule benzopyran derivative that acts as a selective modulator of gap junctions, particularly targeting connexin43 hemichannels. It inhibits the opening of these channels and reduces gap junction coupling, thereby blocking pathological processes such as cortical spreading depression associated with migraine aura and pain. Tonabersat has demonstrated efficacy in preclinical models for migraine prophylaxis, epilepsy (as an anticonvulsant), and neuroprotection against inflammatory damage in the central nervous system. The drug effectively crosses the blood-brain barrier and binds to a unique stereoselective site in astrocytes. Developed initially for migraine prevention, it has reached phase II clinical trials for migraine and phase I studies for epilepsy, with additional preclinical exploration as an adjuvant therapy in glioblastoma[1][2][4][6][8].

Brand names
Xiflam
Other names
tonabersate
02

Targets

GJA1 (Connexin43 Hemichannel)

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