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. 2016 Apr 18;59(10):5011–5021. doi: 10.1021/acs.jmedchem.6b00372

Table 4. Full Pharmacokinetic Parameters of Compound 27 Compared to Compound 2 at a Dose of 10 mg/kg.

compd (route) AUC0–lasta (μg·min/mL) AUC0–∞b (μg·min/mL) Cmaxc (μg/mL) Tmaxd (h) CLe (mL min–1 kg–1) Vdf (L/kg) t1/2g Fh (%)
27 (iv) 1540 1570     6.4 3.58 t1/2α = 3.6 min  
              t1/2β = 6.5 h  
27 (po) 552 582 2.7 0.5     t1/2α = 2.4 h 37
              t1/2β = 6.6 h  
2 (iv)i 1180 1460     6.9 0.30 t1/2α = 35.2 min  
              t1/2β ≥ 20 h  
2 (po)i 408 738 1.3 1     t1/2α = 1.9 h 50
              t1/2β > 20 h  
a

AUC0–last = area under the curve from 0 min to the last quantifiable time point.

b

AUC0–-∞ = area under the curve from 0 min extrapolated to infinity.

c

Cmax = maximum concentration.

d

Tmax = time at which maximum concentration is achieved.

e

CL = clearance.

f

Vd = volume of distribution.

g

t1/2α = half-life of distribution. t1/2β = half-life of elimination.

h

F = oral bioavailbility.

i

Data for compound 2 reproduced from Bouley et al. for comparison.