Kasuga et al. preclinically evaluate TAS3351, a fourth generation EGFR-TKI, using biochemical, structural, and pharmacological assays. TAS3351 overcomes T790M and C797S mutations, which are two major resistant mutations that occur in EGFR and often cause resistance to existing EGFR-TKIs, and exhibits significant brain penetrability.
- Hidefumi Kasuga
- Yuki Kataoka
- Shinji Mizuarai