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. 2007 Aug;3(4):513–525.

Table 5.

Mean pharmacokinetic parameters for selected peptide deformylase inhibitors in mice and rats

Reference/species Compound Regimen Cmax (mg/L) Tmax (min.) AUC (mg/L•h) CL (mL/min/kg) t 1/2 (h) Vss(L/Kg) F (%)
[Azoulay-Dupuiset al 2004]/mice BB-83698 80 mg/kg SC × 1 dose 14.3a 60 57.4a,c 2.5a
61.9b 60 229.4b,c 2.6b
[Ramanathan-Girish et al 2004]/ mice BB-83698 10 mg/kg IV × 1 dose 6.3 3.8 44.4 1.0 2.0
50 mg/kg IV × 1 dose 44.6 55.1 15.1 2.6 2.6
[Craig 2001]/ neutropenic mice BB-83698 20 and 80 mg/kg SC and PO × 1 dose each 1.6–1.7 50
[Gross et al 2004]/ mice BB-81384 10 mg/kg IV × 1 dose 15.1 6.5d 25 2.2 1.6
10 mg/kg oral × 1 dose 1.6 3.6d 3.1 55
50 mg/kg oral × 1 dose 21.3 28.6d 3.7 88
[Clements et al 2001]/rats BB-3497 100 mg/kg oral × 1 dose 24.0 34e
[Chen et al 2004a]/ mice VRC 3375 100 mg/kg IV × 1 dose 0.25
100 mg/kg SC × 1 dose 66 20 0.25
100 mg/kg PO × 1 dose 43 10 0.25 64
[Hackbarth et al 2002]/mice VRC 4232 13 mg/kg IV × 1 dose 5580 1.1
13 mg/kg oral × 1 dose 167 3.2
VRC 4307 3.7 mg/kg IV × 1 dose 1720 0.1
3.7 mg/kg oral × 1 dose 1.5 15 0.1
[Teo et al 2006]/ mice PDF-611 1 mg/kg IV × 1 dose 604f 254g 65.8 0.5 3.0
5 mg/kg oral × 1 dose 194f 15 566g 3.7 45

Abbreviations:Cmax = peak plasma concentration, Tmax = time to Cmax, AUC = area under the plasma concentration-versus-time curve, CL = total body clearance, t 1/2 = terminal disposition half-life, Vss = volume of distribution at steady-state, F = oral bioavailability.

a

serum.

b

lung.

c

Over 10 hrs. post-dose.

d

Over 5 hrs. post-dose.

e

Over 24 hrs. post-dose.

f

ng/mL.

g

ng/mL•h.