Pharmacokinetic parameters of radioactivity, lemborexant, and its metabolites in plasma after a single oral administration of [14C]lemborexant to healthy male volunteers
Parameters except for tmax represent the mean ± S.D. of eight subjects. The tmax is expressed as median and range.
| Analyte | Cmax | tmax | AUC(0–inf) | t1/2 | CL/F | Vz/F | AUC(0–inf) Ratio |
|---|---|---|---|---|---|---|---|
| ng/mla | h | ng·h/mla | h | l/h | l | % of radioactivity | |
| Radioactivity | 61.7 ± 9.81 | 1.00 (1.00–3.00) | 1390 ± 450 | 43.6 ± 16.3 | 7.60 ± 2.12 | 440 ± 56.0 | — |
| Lemborexant | 29.5 ± 5.91 | 1.00 (1.00–3.00) | 317 ± 92.5 | 45.2 ± 15.5 | 32.8 ± 7.79 | 2120 ± 907 | 23.1 ± 2.3 |
| M4 | 5.18 ± 1.34 | 3.50 (2.00–4.00) | 96.2 ± 27.1 | 30.5 ± 11.3 | — | — | 7.0 ± 0.8 |
| M9 | 3.87 ± 0.533 | 2.00 (1.00–4.00) | 65.6 ± 14.7 | 27.7 ± 6.21 | — | — | 4.9 ± 0.6 |
| M10 | 3.32 ± 0.915 | 4.00 (3.00–8.00) | 167 ± 57.4 | 36.2 ± 9.39 | — | — | 12.1 ± 2.5 |
—, not applicable; CL/F, oral clearance; t1/2, terminal elimination half-life; tmax, time to reach maximum concentration; Vz/F, volume of distribution based on the terminal phase.
↵a Units for radioactivity are nanogram equivalent per milliliter and nanogram equivalent·hour per milliliter.