Table 1.
Inhibitory activity of cabozantinib in comparison with other tyrosine kinase inhibitors
| Target | Cabozantinib IC50 (nM)21 | Vandetanib IC50 (nM)32 | Motesanib IC50 (nM)33 | Sunitinib IC50 (nM)34 | Axitinib IC50 (nM)35 |
|---|---|---|---|---|---|
| VEGFR-2 | 0.035 | 40 | 3 | 9 | 0.2 |
| c-Met | 1.3–14.6 | – | – | 4000 | – |
| RET | 5.2 | 100 | 59–2500 | 50 | – |
| c-Kit | 4.6 | >20000 | 8 | 1 | 1.7 |
| Flt3 | 11.3 | – | – | 30–250 | <1000 |
| AXL | 7 | – | – | – | – |
| Tie2 | 14.3 | 2500 | – | – | – |
Notes: Where a range is cited, this indicates that IC50 varies according to receptor mutation status. Where a hyphen is shown, no IC50 was reported for that receptor tyrosine kinase.
Abbreviations: VEGFR-2, Vascular endothelial growth factor receptor 2; IC50, concentration at which 50% of maximal inhibition occurs; nM, nanomolar.