TABLE 1

Mean pharmacokinetic parameters of almorexant and its four primary metabolites in plasma and of total radioactivity in plasma and whole blood after a single 200-mg oral administration of ¹⁴C-almorexant in healthy male subjects

Data are expressed as median (range) for T_max and geometric mean (95% confidence interval) for C_max, t_1/2, and AUC_0–inf; n = 6.

	C_max	T_max	t_1/2	AUC_0–inf
	ng/ml^a	h	h	ng·h/ml^b
Almorexant	113 (74.8, 170)	0.8 (0.5–1.0)	17.8 (12.4, 25.7)	262 (206, 333)
ACT-078332 (M6)	99.4 (70.6, 140)	1.5 (1.0–2.0)	10.4 (9.04, 12.0)	1039 (743, 1452)
ACT-172515 (M5)	80.4 (59.1, 109)	0.9 (0.8–1.5)	26.3 (23.9, 28.9)	282 (223, 356)
ACT-127979 (M8)	61.4 (44.1, 85.4)	1.0 (0.8–1.0)	21.7 (14.2, 33.0)	386 (283, 526)
ACT-127980 (M3)^c	25.7 (17.2, 38.4)	0.8 (0.5–1.0)	22.1 (11.1, 43.8)	160 (102, 252)
Radioactivity in whole blood	678 (561, 819)	1.0 (1.0–2.0)	39.0 (34.1, 44.5)	26,321 (22,051, 31,420)
Radioactivity in plasma	1060 (871, 1291)	1.0 (1.0–4.0)	78.0 (66.2, 91.9)	51,547 (45,940, 57,839)

↵^a Unit for radioactivity in whole blood and plasma is ng-Eq/ml.
↵^b Unit for radioactivity in whole blood and plasma is ng-Eq·h/ml.
↵^c For one subject t_1/2 could not be reliably estimated, n = 5 for t_1/2 and AUC_0–inf.