It is excreted mainly in the form of metabolites, with only trace amounts of the parent compound identified.The medication has an elimination half-life of about 8 hours or of 6 to 10 hours. Its half-life is shorter than that of other orexin receptor antagonists such as suvorexant (12 hours) and lemborexant (~18–55 hours). The relatively short half-life of daridorexant may allow for reduced daytime sedation. The duration of action of daridorexant in terms of sedative effects is approximately 8 hours with a 50 mg dose. Chemistry
Daridorexant is a small-molecule compound. The chemical name of daridorexant is (S)-(2-(5-chloro-4-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone. Its molecular formula is C23H23N6O2Cl and its molecular weight is 450.93 g/mol (or 487.38 g/mol for the hydrochloride). Daridorexant hydrochloride is a white to light yellowish powder and is very slightly soluble in water. History
Daridorexant was patented in 2013 and was first described in the scientific literature in 2017. It was approved for medical use in the United States in January 2022 and became available in this country in May 2022. On 24 February 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Quviviq, intended for the treatment of insomnia. On 29 April 2022, daridorexant was authorized for use in the European Union. It was the first orexin receptor antagonist to become available for use in the European Union. (The earlier orexin receptor antagonists suvorexant and lemborexant are not available in the European Union.)
Daridorexant, sold under the brand name Quviviq, is an orexin antagonist medication which is used for the treatment of insomnia. Daridorexant is taken by mouth.Side effects of daridorexant include headache, somnolence, and fatigue. The medication is a dual orexin receptor antagonist (DORA). It acts as a selective dual antagonist of the orexin receptors OX1 and OX2. Daridorexant has a relatively short elimination half-life of 8 hours and a time to peak of about 1 to 2 hours. It is not a benzodiazepine or Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.Daridorexant was approved for medical use in the United States in January 2022 and became available in May 2022. It was approved in the European Union in April 2022, and is the first orexin receptor antagonist to become available in European Union. The medication is a schedule IV controlled substance in the United States and may have a modest potential for misuse. Medical uses
Daridorexant is indicated for the treatment of adults with insomnia characterized by difficulties with sleep onset and/or sleep maintenance. The medication has been found to significantly improve latency to persistent sleep (LPS), wake after sleep onset (WASO), and subjective total sleep time (TST) in regulatory clinical trials. At doses of 25 to 50 mg and in terms of treatment–placebo difference, it reduces LPS by 6 to 12 minutes, reduces WASO by 10 to 23 minutes, and increases subjective TST by 10 to 22 minutes.