Table 2.
Main pharmacology and pharmacokinetic properties of the principal ALK inhibitors.
| Generation | Targets | ALK Ki (nM) [21] | |
|---|---|---|---|
| Crizotinib | First | ALK, c-Met, ROS1 | 1.6 |
| Ceritinib | Second | ALK, IGF-1R, InsR, ROS1 | 0.10 |
| Alectinib | Second | ALK, RET | 0.09 |
| Brigatinib | Second | ALK, EGFR | 0.10 |
| Lorlatinib | Third | ALK | 0.14 |
ALK: anaplastic lymphoma kinase, c-Met: Hepatocyte growth factor receptor, ROS1: ROS proto-oncogene 1, IGF-1R: insulin-like growth factor 1 receptor, InsR: insulin receptor, RET: rearranged during transfection, EGFR: epidermal growth factor receptor.