Abstract
ERAS-801 is a highly CNS-penetrant small molecule (Kp, brain, mouse = 3.7 and Kp,uu, brain, mouse = 1.2) designed to reversibly inhibit EGFR alterations observed in GBM, including EGFR amplification and the EGFRvIII variant. It is currently being evaluated in recurrent GBM in the phase 1 clinical trial THUNDERBBOLT-1 (NCT05222802). ERAS-801 also shows in vitro activity against other EGFR alterations observed in NSCLC. Due to its high CNS penetration, an exploratory in vivo study was conducted to characterize ERAS-801’s activity in a CNS metastases model of EGFR mutant NSCLC.
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