Table 1. Blood-brain barrier (BBB) penetration capabilities of EGFR- and ALK-TKIs in human.
TKIs | Penetration (CSF/blood) |
---|---|
EGFR-TKIs | |
Gefitinib | 1.1% (43) |
Erlotinib | 2.8% (43) |
Afatinib | 1.7% (44) |
Osimertinib | |
160 mg | 16% (45) |
80 mg | 2.0% (46) |
ALK-TKIs | |
Crizotinib | 0.26% (47) |
Ceritinib | No human data [animal model: 15% (48)] |
Alectinib | No human data [animal model: 63–94% (49)] |
Brigatinib | No human nor animal data |
Lorlatinib | 75% (50) |
EGFR, epidermal growth factor receptor; ALK, anaplastic lymphoma kinase; TKI, tyrosine kinase inhibitor; CSF, cerebrospinal fluid.