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

Table 1. Plasma 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 μg/mL 17.42 3.77 4.92 0.25 34.62 5.62 5.95 0.77
Tmax min   27.22 14.28 21.91   27.98 14.28 27.72
Vss mL 2.90       2.76      
V1_F mL 1.72 <0.01 <0.01 0.05 0.87 <0.01 <0.01 0.01
CL_F μL/min 199.16 0.11 0.16 2.01 146.90 0.07 0.13 0.52
V2_F mL 1.05 <0.01 <0.01 <0.01 2.04 <0.01 <0.01 <0.01
CLD2_F μL/min 84.57 <0.01 <0.01 <0.01 197.45 <0.01 <0.01 <0.01
K01 1/h   2.28 4.29 2.92   2.21 4.30 2.24
K10 1/h 6.94 2.13 4.11 2.56 10.17 2.08 4.10 2.09
K12 1/h 2.95 <0.001 <0.001 <0.001 13.67 <0.001 <0.001 <0.001
K21 1/h 4.85 2.14 2.00 2.58 5.82 2.08 2.00 2.09
K01_HL min   18.28 9.70 14.23   18.85 9.67 18.55
K10_HL min 5.99 19.47 10.10 16.22 4.09 19.93 10.13 19.85
Alpha 1/min 0.20 0.04 0.07 0.04 0.46 0.03 0.07 0.03
Beta 1/min 0.05 0.04 0.03 0.04 0.04 0.03 0.03 0.03
Alpha_HL min 3.49 19.53 10.11 16.32 1.51 20.00 10.14 19.92
Beta_HL min 14.73 19.42 20.75 16.02 19.33 19.92 20.75 19.87
MRT_last min 13.21 38.77 27.43 32.61 19.74 40.71 24.78 37.68
MRT_INF_obs min 18.03 47.94 36.15 33.97 37.00 64.30 26.30 54.41
MRT_INF_pred min 17.92 48.13 36.08 34.07 37.29 64.29 26.34 54.19
a

Cmax: peak plasma drug concentration; Tmax: time to reach peak plasma concentration following drug administration; Vss: apparent volume of distribution at a steady state; V1_F and V2_F: apparent volume of central and peripheral compartments in two compartmental models; CL_F and CLD2_F: apparent total body clearance of the drug from plasma and apparent total clearance of the drug from plasma 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.