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. 2019 Nov;8(Suppl 3):S298–S307. doi: 10.21037/tlcr.2019.05.15

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.