Table 2.

Pharmacokinetic parameters of difelikefalin [¹⁴C] equivalents in whole blood and plasma after a single IV bolus [¹⁴C]difelikefalin

Parameter	Healthy subjects
	Whole blood				Plasma
	n	Mean	SD	CV%	n	Mean	SD	CV%
tmax (h)	6	0.0867	0.0163	18.84	6	0.0867	0.0163	18.84
Cmax (ng-eq/mL)	6	13.6	1.40	10.30	6	24.8	2.29	9.25
AUClast (h*ng-eq/mL)	6	23.3	3.43	14.71	6	42.2	5.82	13.79
AUCinf (h*ng-eq/mL)	6	24.5	3.89	15.88	6	44.3	6.63	14.96
t1/2 (h)	6	2.56	0.668	26.05	6	2.60	0.680	26.14
CL (L/h)	6	8.54	1.63	19.05	6	4.70	0.810	17.25
Vz (L)	6	30.5	4.37	14.36	6	17.0	2.62	15.35
C0 (ng-eq/mL)	6	16.2	1.95	12.07	6	29.7	3.10	10.43

Parameter	Subjects on hemodialysis
	Whole blood				Plasma
	n	Mean	SD	CV%	n	Mean	SD	CV%
tmax (h)	6	0.0800	0.00	0.00	6	0.0800	0.00	0.00
Cmax (ng-eq/mL)	6	15.8	3.17	20.05	6	25.6	4.18	16.34
AUClast (h*ng-eq/mL)	6	208	39.1	18.77	6	338	49.7	14.70
AUCinf (h*ng-eq/mL)	6	290	67.6	23.31	6	474	122	25.61
t1/2 (h)	6	38.4	8.92	23.24	6	38.0	9.82	25.87
CL (L/h)	6	0.727	0.161	22.09	6	0.448	0.104	23.34
Vz (L)	6	39.3	7.88	20.06	6	23.4	1.45	6.22
C0 (ng-eq/mL)	6	18.9	3.88	20.51	6	30.9	5.46	17.65

AUC_inf area under the curve from time 0 h to infinity, AUC_last area under the curve from time 0 h to last quantifiable concentration, C₀ concentration at time-zero for IV dosing, CL total systemic clearance, C_max maximum concentration, CV% coefficient of variation, IV intravenous, t_max time to reach C_max, t_1/2 terminal elimination half-life, V_z volume of distribution in the terminal elimination phase