Table 1.

Overview of pharmacokinetic variables

	Healthy volunteers [34]				Healthy volunteers [30]	Healthy volunteers (liver) [40]	Healthy volunteers (renal) [40]	Healthy volunteers [36]	Pop-PK model for MF & PV patients [32]
Ruxolitinib dose	5 mg	10 mg	25 mg	50 mg	25 mg	25 mg	25 mg	25 mg	10 mg, 25 mg and 50 mg
Single or multiple dose	Single dose	Single dose	Single dose	Single dose	Single dose	Single dose	Single dose	Single dose	Multiple dose
No. of patients	12	6	6	6	6	32	8	9	414
Cmax (nM) [mg/L]	195 [0.060] (CV = 35.4%)	368 [0.11] (CV = 29.9%)	934 [0.28] (CV = 55.9%)	1700 [0.52] (CV = 29.2%)	1093 [0.33] (SD = 651 [0.20])	1350 [0.41] (CV = 46.2%)	1110 [0.34] (CV = 28.9%)	1100 [0.34] (SD = 332 [0.10])
Tmax (h)	2.0 (range 0.50–3.0)	1.8 (range 0.50–4.0)	2.0 (range 0.50–6.0)	1.0 (range 0.50–2.0)	0.63 (SD = 0.31)	0.5 (range 0.5–1.5)	1.0 (range 05–1.5)	0.9 (SD = 0.5)
T½ (h)	2.6 (CV = 40%)	3.4 (CV = 41%)	3.0 (CV = 22%)	2.7 (CV = 21%)	2.32 (SD = 0.37)	2.7 (CV = 25%)	3.7 (CV = 23%)	2.8 (SD = 0.7)
AUCinf (nM*h) [mg/L*h]	823 [0.25] (CV = 31.7 %)	1759 [0.54] (CV = 22.2%)	4110 [1.25] (CV = 34.1%)	6940 [2.11] (CV = 27.2%)	3200 [0.97] (SD = 1361 [0.41])	3520 [1.07] (CV = 42.4%)	4670 [1.42] (CV = 21.4%)	4350 [1.32] (SD = 1990 [0.61])
Vz/F, (L)	75.1 (CV = 48.2%)	90.8 (CV = 36.3%)	85.7 (CV = 23.7%)	90.5 (CV = 43.2%)		91.5 (CV = 29.4%)	103 (CV = 23.2%)		58.6 (RSE = 2.8%) (Vc/F)
CL/F (L/h)	19.8 (CV = 31.2%)	18.6 (CV = 20.4%)	19.9 (CV = 37.7%)	23.5 (CV = 59.2%)		23.2 (CV = 49.6%)	19.3 (CV = 20.5%)	22.8 (SD = 10.3)	Male: 22.1 (RSE = 3.4%) Female: 17.7 (RSE = 3.5%)

AUC_inf area under the curve to infinity, C_max maximum drug concentration, CL/F clearance, CV coefficient of variation, MF myelofibrosis, Pop-PK population pharmacokinetics, PV polycythemia vera, RSE relative standard error, SD standard deviation, T_max time to reach maximum concentration, T_½ elimination half-life, Vz/F terminal volume of distribution