Drug intelligence / Profile preview

darigabat

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

Overview

Darigabat is a novel small molecule that acts as a selective positive allosteric modulator (PAM) of the GABA A receptor. It specifically targets the α2, α3, and α5 subunit-containing GABA A receptors while sparing the α1 subunit. This selectivity is designed to provide anxiolytic and antiseizure effects with reduced risk of sedation, cognitive impairment, tolerance development, and abuse potential compared to non-selective benzodiazepines. Darigabat is under clinical development for conditions including epilepsy (notably focal onset seizures and photosensitive epilepsy), panic disorder, and other anxiety disorders. The drug was originally developed by Pfizer and is currently being developed by Cerevel Therapeutics (a subsidiary of AbbVie). Clinical trials have shown it to be generally well-tolerated with side effects such as dizziness, fatigue, headache, mild somnolence, bradyphrenia (slowness of thought), modest memory impairment, mild cognitive impairment, balance impairment, and feeling abnormal[1][3][4][6][7][8].

Other names
darigabat
02

Targets

GABA_A receptor α1βγ2 (Gamma-aminobutyric acid type A receptor alpha-1 beta gamma-2 (α1βγ2 GABAA receptor))GABA-A receptor α3β2γ2 subtypeα5-GABAAR (Gamma-aminobutyric acid type A receptor alpha5beta2gamma2 subtype (GABAA receptor alpha5beta2gamma2 subtype))GABA-A receptor α2βγ2 subtype

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