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. 2022 Nov 13;114(2):654–664. doi: 10.1111/cas.15617

FIGURE 5.

FIGURE 5

Brain penetrability and antitumor activity of TAS2940 in NCI‐N87‐luc (human epidermal growth factor receptor type 2 [HER2] amp) and NCI‐H1975_EGFR ex20insSVD‐luc intracranial brain metastasis models. (A) The unbound concentration in the brain to the unbound concentration in plasma ratio (K p,uu,brain) values of lapatinib, neratinib, tucatinib, poziotinib, TAS2940, and osimertinib (n = 3). (B) Total flux (p/s) values in the NCI‐N87‐luc intracranial model. (C) Bioluminescence images obtained on day 22. (D) Total flux (p/s) values in the NCI‐N87‐luc intracranial model with different dosing schedules of TAS2940. (E) Target inhibition of TAS2940 assessed by phospho‐HER2 and growth fraction assessed by Ki‐67 in the NCI‐N87‐luc model. (F) Antitumor activity and survival benefit of TAS2940 in the NCI‐H1975_EGFR ex20ins SVD‐luc intracranial nude mouse model. Data are presented as the mean ± SE (n = 8 in B,C; n = 6 in D). EGFR, human epidermal growth factor receptor.