Darigabat (CVL-865, PF-06372865): A Comprehensive Profile of an Investigational GABAA Receptor Modulator

1. Introduction to Darigabat

1.1. Overview and Background

Darigabat is an investigational small molecule pharmaceutical agent currently undergoing clinical evaluation for its potential therapeutic applications in a range of neurological and psychiatric conditions.[1] It is classified as a GABAergic medication, operating specifically as a positive allosteric modulator (PAM) of the gamma-aminobutyric acid type A (GABAA) receptor.[1] The development of Darigabat is centered on the hypothesis that it can deliver the established therapeutic benefits of GABAergic modulation, such as anxiolytic and anticonvulsant actions, while offering an improved side-effect profile. A key objective is the minimization of sedation, a common limiting side effect of older, non-selective GABAergic compounds like benzodiazepines. This anticipated improvement is attributed to Darigabat's selective interaction with specific subtypes of the GABAA receptor.[2]

1.2. Chemical Identity and Synonyms

The officially recognized generic name for this investigational compound is Darigabat.[1] Throughout its research and development phases, Darigabat has been identified by several internal developmental code names. The most prominent of these are CVL-865, utilized by Cerevel Therapeutics, and PF-06372865 (sometimes cited as PF-6372865), used during its initial development by Pfizer.[1] The International Nonproprietary Name (INN) "darigabat" was formally adopted for the compound previously designated CVL-865.[6]

1.3. Therapeutic Class