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Daridorexant (CAS No. 1505484-82-1), also known by its international nonproprietary name and developed under identifiers such as ACT-541468 or nemorexant, is a novel orally active dual orexin receptor antagonist (DORA) designed for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. It represents an innovative pharmacological approach distinct from traditional hypnotics, targeting the central regulation of the sleep–wake cycle with high receptor selectivity.
Daridorexant functions by selectively antagonizing both orexin-1 (OX1R) and orexin-2 (OX2R) receptors, which are the primary receptors activated by endogenous orexin neuropeptides that promote wakefulness. By blocking orexin signaling, Daridorexant facilitates the physiological transition from wakefulness to sleep without directly modulating GABAergic pathways, offering a sleep-promoting mechanism with reduced risk of tolerance, dependence, and residual next-morning sedation compared with many GABA-A receptor modulators.
Originally approved for medical use under the brand Quviviq™, Daridorexant has received regulatory authorization in major markets including the United States, European Union, and other regions for the treatment of adult insomnia. Clinical studies have shown that Daridorexant improves key sleep parameters — including sleep latency, sleep maintenance, and subjective total sleep time — and has demonstrated benefits in daytime functioning at therapeutic doses.
Daridorexant (CAS No. 1505484-82-1), also known by its international nonproprietary name and developed under identifiers such as ACT-541468 or nemorexant, is a novel orally active dual orexin receptor antagonist (DORA) designed for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. It represents an innovative pharmacological approach distinct from traditional hypnotics, targeting the central regulation of the sleep–wake cycle with high receptor selectivity.
Daridorexant functions by selectively antagonizing both orexin-1 (OX1R) and orexin-2 (OX2R) receptors, which are the primary receptors activated by endogenous orexin neuropeptides that promote wakefulness. By blocking orexin signaling, Daridorexant facilitates the physiological transition from wakefulness to sleep without directly modulating GABAergic pathways, offering a sleep-promoting mechanism with reduced risk of tolerance, dependence, and residual next-morning sedation compared with many GABA-A receptor modulators.
Originally approved for medical use under the brand Quviviq™, Daridorexant has received regulatory authorization in major markets including the United States, European Union, and other regions for the treatment of adult insomnia. Clinical studies have shown that Daridorexant improves key sleep parameters — including sleep latency, sleep maintenance, and subjective total sleep time — and has demonstrated benefits in daytime functioning at therapeutic doses.
