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Study 202 consisted of two steps: an open\u2010label, 20\u2009mg repeated\u2010dose in non\u2010elderly individuals (Step 1; <jats:italic>n<\/jats:italic>\u2009=\u200912) and a double\u2010blind, 20\u2009mg repeated\u2010dose in elderly individuals (Step 2; <jats:italic>n<\/jats:italic>\u2009=\u20098\/3 for vornorexant\/placebo). Vornorexant was rapidly absorbed and eliminated under fasting conditions, with a time to maximum plasma concentration of 0.500\u20133.00\u2009h (range) and elimination half\u2010life of 1.32\u20133.25\u2009h. The area under the plasma concentration\u2010time curve (AUC) of vornorexant increased proportionally with dose increments. Sleepiness\u2010related pharmacodynamic outcome changes (Karolinska sleepiness scale, digit symbol substitution test and psychomotor vigilance task) were generally increased with dose increments at 1 and 4\u2009h post\u2010dose, whereas no consistent dose\u2010related changes were detected the next morning. Food intake did not affect the maximum observed plasma concentration of vornorexant but increased the AUC<jats:sub>0\u2013inf<\/jats:sub>. Exposure in elderly individuals was generally comparable to that in non\u2010elderly individuals. Altogether, vornorexant may have a favourable profile for insomnia treatment, including rapid onset of action and minimal next\u2010day residual effects.<\/jats:p>","DOI":"10.1111\/bcpt.13930","type":"journal-article","created":{"date-parts":[[2023,8,11]],"date-time":"2023-08-11T05:51:46Z","timestamp":1691733106000},"page":"576-591","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":21,"title":["Pharmacokinetics, pharmacodynamics and safety profile of the dual orexin receptor antagonist vornorexant\/TS\u2010142 in healthy Japanese participants following single\/multiple dosing: Randomized, double\u2010blind, placebo\u2010controlled phase\u20101 studies"],"prefix":"10.1111","volume":"133","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5134-3554","authenticated-orcid":false,"given":"Daiji","family":"Kambe","sequence":"first","affiliation":[{"name":"Development Headquarters Taisho Pharmaceutical Co., Ltd.  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