Table 2.
Impact of investigated treatments on the plasma and tissue kinetics of [11C]erlotinib in NHPs.
| Condition | Monkey | AUCplasmaa (SUV.min) |
AUCbrain (SUV.min) |
AUCmuscle (SUV.min) |
AUCRbrain/muscle (unitless) |
AUCRbrain/plasma (unitless) |
kuptake,brain (mL/min/g) |
VT,brain (mL/cm3) |
|---|---|---|---|---|---|---|---|---|
| Baseline | M1 | 46.8 | 7.4 | 36.1 | 0.20 | 0.16 | 0.012 | 0.17 |
| M2 | 57.1 | 11.4 | 47.3 | 0.24 | 0.20 | 0.013 | 0.24 | |
| Erlotinib/tariquidar (10 mg/kg/h; 4 mg/kg/h) |
M1 | 69.4 | 28.8 | 61.4 | 0.47 | 0.41 | 0.032 | 0.58 |
| M2 | 55.2 | 63.8 | 67.3 | 0.95 | 1.16 | 0.035 | 1.21 | |
| Erlotinib (10 mg/kg/h) |
M1 | 47.7 | 10.9 | 41.5 | 0.26 | 0.23 | 0.016 | 0.28 |
| Tariquidar (4 mg/kg/h) |
M2 | 30.3 | 7.9 | 30.5 | 0.26 | 0.26 | 0.015 | 0.47 |
aCorrected for radiolabeled metabolites of [11C]erlotinib.