Table 2. Tyrosine kinase inhibitors (TKIs) and ABCC10 modulators.
Compound | Concentrations | Effect on ABCC10 substrate drug | Effect on accumulation of [3H]-paclitaxel | Effect on efflux of [3H]-paclitaxel | Effect on ABCC10 protein expression |
Cepharanthine[24] | 2 µmol/L | + | ↑ | ↓ | ↔ |
Imatinib[28] | 1, 2.5, 5 µmol/L | + | ↑ | ↓ | ↔ |
Nilotinib[28] | 1, 2.5, 5 µmol/L | + | ↑ | ↓ | ↔ |
Lapatinib[33] | 0.625, 1.25, 2.5 µmol/L | + | ↑ | ↓ | ↔ |
Erlotinib[33] | 0.625, 1.25, 2.5 µmol/L | + | ↑ | ↓ | ↔ |
Sorafenib[19] | 5 µmol/L | + | N/A | N/A | N/A |
Sildenafil[41] | 1.25, 2.5, 5 µmol/L | + | ↑ | ↓ | ↔ |
Vardenafil[41] | 1.25, 2.5, 5 µmol/L | + | ↑ | ↓ | ↔ |
Tariquidar[61] | 0.1, 0.3 µmol/L | + | ↑ | ↓ | ↓ (>24 h treatment) |
Tandutinib[47] | 5, 10 µmol/L | + | ↑ | ↓ | ↔ |
(+): this compound shows reversal activity for the ABCC10 transporter; (-): this compound shows no reversal activity for the ABCC10 transporter; (↑): increase or up-regulate; (↓): decrease or down-regulate; (↔): no significant alterations; (N/A): not applicable.