Table 4.
Other parameters including parameters estimated from fitting the PBPK model to plasma 6-MP and intracellular concentrations of 6-MP, 6-TGN and 6-MMPR
| Parameter | Definition | Estimate(%SE) | Source |
|---|---|---|---|
| MW (g) | Molecular weight | 152.2 | – |
| fu | Plasma fraction unbound | 0.81 | 7,48 |
| ka (h–1) | Absorption rate constant | 0.33 (161) | –† |
| CLG,XO,ad (l h–1) | Intestinal clearance due to XO | 18.7 (20) | –† |
| CLL,XO,ad (l h–1) | Hepatic clearance due to XO | 38.4 (22) | –† |
| CLPLAS,ad (l h–1) | Plasma clearance | 31.3 (11) | –† |
| PSBC (l h–1) | RBC permeability-surface area product | 50 | –* |
| CLHGPRT (l h–1) | Intracellular HGPRT clearance | 6.3 (30) | –† |
| CLIMPD (l h–1) | Intracellular IMPD clearance | 0.004 (37) | –† |
| CLMMPR (l h–1) | Intracellular MMPR clearance | 0.002 (41) | –† |
| CLTGN (l h–1) | Intracellular TGN clearance | 0.009 ⋅ BSA1.16 | 36 |
| Km,TPMT (mg l–1) | Michaelis–Menten constant | 45.65 | 35 |
| CPPGL (mg g–1) | Cytosolic protein g–1 of liver | 81 | 26 |
*
Fixed.
†
Estimated.