. 2014 Nov 20;78(6):1315–1333. doi: 10.1111/bcp.12418

Table 3.

Mean (SD) pharmacokinetic parameters of AMG 181 after a single intravenous (i.v.) or subcutaneous (s.c.) administration in healthy subjects, or subjects with ulcerative colitis (UC)

Regimen	t_max (days, h)	C_max (μg ml⁻¹)	C_max/Dose (μg ml⁻¹ mg⁻¹)	AUC(0,t) (μg ml⁻¹ day)	AUC(0,∞) (μg ml⁻¹ day)	AUC(0,∞)/Dose (μg ml⁻¹ day mg⁻¹)	t_1/2 (days)	V_z, V_z/F (l)	CL, CL/F (l day⁻¹)	V_ss (l)
0.7 mg s.c.	2.0	0.0225	0.0322	0.0433	NC	NC	NC	NC	NC	NC
(n = 3)	(2.0, 3.0)	(0.0180)	(0.0256)	(0.0644)	NC	NC	NC	NC	NC	NC
2.1 mg s.c.	3.5	0.126	0.0598	1.01	2.84^*	1.35^*	11.0^*	11.7^*	0.739^*	NC
(n = 4)	(2.0, 7.1)	(0.100)	(0.0476)	(0.95)	NC	NC	NC	NC	NC	NC
7 mg s.c.	4.0	0.245	0.0351	2.64	4.12^*	0.589^*	10.0^*	24.5^*	1.70^*	NC
(n = 5)	(2.0, 4.0)	(0.046)	(0.0066)	(1.25)	NC	NC	NC	NC	NC	NC
21 mg s.c.	7.1	2.51	0.119	63.5^†	67.2^†	3.20^†	20.6^†	9.53^†	0.326^†	NC
(n = 6)	(3.1, 10.0)	(0.51)	(0.024)	(13.6)	(15.0)	(0.71)	(9.0)	(3.92)	(0.078)	NC
70 mg s.c.	5.6	10.1	0.144	410^†	414^†	5.92^†	25.2^†	6.36^†	0.185^†	NC
(n = 6)	(3.0, 10.0)	(2.45)	(0.035)	(149)	(155)	(2.22)	(7.0)	(1.16)	(0.056)	NC
210 mg s.c.	10.0	29.8	0.142	1690^†	1720	8.21	37.3	6.76	0.132	NC
(n = 6)	(7.0, 14.0)	(6.2)	(0.030)	(520)	(487)	(2.32)	(7.43)	(1.08)	(0.046)	NC
70 mg i.v.	1.4	23.0	0.329	501	503	7.19	27.3	5.50	0.140	4.12
(n = 6)	(1.4, 1.6)	(3.5)	(0.050)	(34)	(34)	(0.48)	(3.5)	(0.63)	(0.010)	(0.43)
210 mg i.v.	1.0	72.1	0.343	1720^†	1730^†	8.25^†	34.5^†	6.17^†	0.124^†	5.08^†
(n = 6)	(1.0, 1.0)	(13.3)	(0.063)	(290)	(277)	(1.32)	(4.1)	(1.25)	(0.023)	(0.86)
420 mg i.v.	1.0	151	0.360	4380^†	4480	10.7	32.2	4.40	0.0965	3.83
(n = 6)	(1.0, 94.8)	(35.3)	(0.084)	(860)	(802)	(1.91)	(6.6)	(0.78)	(0.0189)	(0.66)
210 mg s.c.	4.0	30.1	0.143	1270	1270	6.07	24.0	7.31	0.228	NC
(UC; n = 3)	(3.9, 7.2)	(8.47)	(0.040)	(682)	(687)	(3.27)	(5.1)	(4.60)	(0.176)	NC

n = 1

^†

n = 5. Smaller ns indicated insufficient data for estimation due to BQL values or subjects withdrew consent early. All values are reported to three significant figures except for t_max, where values are reported to one decimal place. t_max: time to C_max, presented as median (min–max); units: days for s.c., h for i.v.. C_max: maximum observed AMG 181 concentration in serum; dose-normalized value: C_max/Dose. AUC(0,t): area under the concentration–time curve from time zero to the last observed concentration. AUC(0,∞): area under the concentration–time curve from time zero extrapolated to infinity; dose-normalized value: AUC(0,∞)/Dose. t_1/2: linear β-phase half-life. V_z and V_z/F: linear β-phase volume and apparent volume of distribution for i.v. and s.c., respectively; V_ss: volume of distribution at steady-state for i.v.. F: bioavailability after s.c. administration. CL and CL/F: clearance and apparent clearance for i.v. and s.c., respectively. NC, not calculated.