TABLE 1

Selected pharmacokinetic parameters of darolutamide, its diastereomers, and keto-darolutamide after a single dose of ¹⁴C-darolutamide (300 mg) as oral solution

Data are presented as geometric means (geometric CV%) (N = 6).

Plasma PK Parameter	Total ¹⁴C Radioactivity	Parent Darolutamide	(S,R)-Darolutamide	(S,S)-Darolutamide	Keto-Darolutamide
AUC_0–inf (h.μg/mL)	159 (0.02)^a	45.6 (0.02)	7.11 (0.03)	38.3 (0.02)	93.7 (0.02)
C_max (μg/mL)	16.5 (0.02)^a	3.82 (0.02)	1.81 (0.02)	2.49 (0.02)	11.7 (0.02)
T_max (h)^b	1.5 (1.0–2.0)	1.5 (1.0–3.0)	1.0 (0.5–1.5)	3.0 (1.5–4.0)	1.5 (1.0–1.5)
t_1/2 (h)	11.5 (24.5)	10.6 (22.6)	6.58 (20.7)	10.7 (20.5)	10.7 (31.4)
Analyte-to-parent ratio^c	NC	0.185 (14.7)^d	0.156 (12.4)	0.841 (2.2)	2.06 (11.1)

NC, not calculated; PK, pharmacokinetic; T_max, time when maximum plasma concentration is observed.
↵^a Units are μg eq of ¹⁴C-darolutamide.
↵^b Median (range).
↵^c Based on individual AUC_0–inf.
↵^d Diastereomer ratio, calculated as (S,R)-darolutamide/(S,S)-darolutamide.