Skip to main content
. 2020 Jan 30;5(5):2345–2354. doi: 10.1021/acsomega.9b03735

Table 3. Spinal Cord Pharmacokinetic Parameters of Complement C5a Receptor 1 Antagonistsa.

    PMX53 PMX205
parameters units i.v. s.c. i.p. p.o. i.v. s.c. i.p. p.o.
Cmax ng/g 129.82 96.56 71.26 75.88 449.84 225.14 219.65 214.33
Tmax min   23.15 11.86 14.89   45.90 17.48 63.47
Vss μg/(ng/g) 0.33       0.27      
V1_F μg/(ng/g) 0.23 0.12 0.35 0.32 0.07 0.05 0.06 0.05
CL_F ng/(min ng/g) 1.52 3.68 5.15 2.33 1.63 1.00 0.99 0.81
V2_F μg/(ng/g) 0.10 0.26 <0.01 0.16 0.20 0.05 0.14 <0.001
CLD2_F ng/(min ng/g) 30.58 1.36 0.01 2.71 21.89 0.07 2.59 <0.001
K01 1/hr   2.70 15.39 11.20   1.34 4.45 0.99
K10 1/hr 0.40 1.87 0.87 0.44 1.46 1.25 1.05 0.90
K12 1/hr 7.94 0.69 <0.01 0.51 19.69 0.08 2.75 <0.01
K21 1/hr 18.30 0.32 0.19 1.00 6.59 0.32 1.08 0.33
K01_HL min   15.39 2.70 3.71   30.93 9.36 42.04
K10_HL min 105.04 22.22 47.70 94.33 28.39 34.79 39.53 46.04
Alpha 1/hr 26.36 2.66 0.87 1.69 27.40 1.28 4.64 0.90
Beta 1/hr 0.27 0.22 0.19 0.26 0.35 0.32 0.24 0.33
Alpha_HL hr 0.03 0.26 0.79 0.41 0.03 0.55 0.15 0.77
Beta_HL hr 2.52 3.09 3.71 2.66 1.97 2.16 2.84 2.08
MRT_last hr 0.69 0.64 0.62 0.68 0.62 0.81 0.65 0.80
MRT_INF_obs hr 4.86 1.49 1.16 1.89 2.45 2.71 1.34 1.06
MRT_INF_pred hr 4.86 1.46 1.13 1.88 2.45 2.69 1.31 1.07
a

Cmax: peak drug concentration; Tmax: time to reach peak concentration following drug administration; Vss: apparent volume of distribution at a steady state; V1_F and V2_F: apparent volume of central and peripheral compartment in two compartmental models; CL_F and CLD2_F: apparent total body clearance of the drug and apparent total clearance of the drug after administration; K01: absorption rate constant; K10: elimination rate constant; K12 and K21: distribution and redistribution rate constant; K01_HL and K10_HL: distribution half-life and elimination half-life; Alpha and Beta: hybrid first-order rate constants expressing initial and terminal slopes of distribution and elimination phases; Alpha_HL and Beta_HL: initial or disposition half-life and terminal elimination half-life; MRT_last, MRT_INF_obs, and MRT_INF-pred: mean residence time at the last time point, infinity observed, and infinity predicted using two-compartmental analysis.