Table 5 PMX53 and PMX205 pharmacokinetic parameters.

From: Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice

Parameter

PMX53

PMX205

Plasma

Brain

Spinal cord

Plasma

Brain

Spinal cord

Cmax (μg/ml or ng/g)

11.9

47.7

102.07

29.03

107.81

213.1

t1/2 (hr)

0.52

3.79

3.40

0.17

2.69

1.78

AUC 0-t (min*μg/ml or g)

204.6

3.18

6.69

347.90

4.18

7.95

AUC 0-inf_obs (min*μg/ml or g)

229.6

13.21

24.67

348.86

12.18

17.42

MRT 0-inf_obs (hr)

0.30

5.46

4.86

0.15

3.75

2.49

Vz_obs (ml or g)

8.26

745.1

358.60

1.32

572.84

265.65

Cl_obs (ml/min or g/min)

0.18

2.27

1.21

0.086

2.46

1.722

Vss_obs (ml or g)

3.28

743.9

354.73

0.79

553.84

257.98

  1. Pharmacokinetic parameters of PMX53 and PMX205 after single intravenous administration of 1 mg/kg of complement C5a receptor 1 antagonist to wild-type mice.
  2. Values represent calculated parameter values using mean of n = 4 concentration values. C max, max concentration of antagonist; t ½, elimination half-life; AUC 0-t, area under the concentration-time curve from time zero to time t i.e. 90 min; AUC 0-infinity, area under the concentration-time curve from time zero to infinity; MRT, mean residence time; Vz, volume of distribution at terminal phase; Cl, clearance; Vss, volume of distribution at steady state.
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