TABLE 1

Pharmacokinetics for INCB018424 and total radioactivity in plasma from individual subjects administered an oral dose of [¹⁴C]INCB018424

Six healthy male human subjects were administered a single oral 25-mg (90 μCi) dose of [¹⁴C]INCB018424. Plasma was collected predose and at several time points between 0.25 and 36 h postdose. INCB018424 concentrations were determined using a validated LC-MS/MS method. Total radioactivity was determined by LSC. Standard noncompartmental pharmacokinetic methods were used to analyze the INCB018424 and total radioactivity plasma concentration data.

	Subject						Mean ± S.D.
	001	002	003	004	005	006	Mean ± S.D.
INCB018424
C_max (nM)	811	796	609	2387	1062	892	1093 ± 651
T_max (h)	0.25	0.50	1.0	0.50	0.50	1.0	0.63 ± 0.31
AUC_0–_t (nM · h)	2397	2200	2856	5894	2924	2866	3189 ± 1357
AUC_0–∞ (nM · h)	2401	2206	2866	5911	2937	2877	3200 ± 1361
t_1/2 (h)	2.45	2.74	2.73	1.92	2.10	1.96	2.32 ± 0.37
Radioactivity
C_max (nM)	1063	918	910	2874	1145	1217	1355 ± 754
T_max (h)	0.50	0.50	1.0	0.50	0.50	2.0	0.83 ± 0.61
AUC_0–_t (nM · h)	5761	5598	5680	10576	5789	6045	6575 ± 1966
AUC_0–∞ (nM · h)	5813	5660	5737	10629	5855	6091	6631 ± 1964
t_1/2 (h)	4.83	5.29	6.08	5.89	7.02	5.73	5.81 ± 0.75
AUC_{0–∞ INCB018424}/AUC_{0–∞ radioactivity}	0.41	0.39	0.50	0.56	0.50	0.47	0.47 ± 0.06