Table 1.
Michaelis-Menten kinetic parameters (Vmax and Km) and catalytic efficiency (Vmax/Km) estimated for tested TKIs for OATP-1B1 and/or OATP-1B3 transporter proteins.
| TKIs | OATP-1B1 | OATP-1B3 | ||||
|---|---|---|---|---|---|---|
|
|
|
|||||
| Km | Vmax | Vmax/Km | Km | Vmax | Vmax/Km | |
| Canertinib | – | – | – | 12.18±3.32 | 15.34±1.59 | 1.25 |
| Nilotinib | 10.14±1.91 | 6.95±0.47 | 0.68 | 7.84±1.43 | 6.75±0.42 | 0.86 |
| Vandetanib | 2.72±0.25 | 75.95±1.99 | 27.92 | 4.37±0.79 | 194.64±10.58 | 44.31 |
| Erlotinib | – | – | – | – | – | – |
| Pazopanib | – | – | – | – | – | – |
Units: Vmax, nmol/mg protein per minute; Km, μM; Vmax/Km, mL/mg protein per minute.