Osimertinib showed preclinical evidence of concentrations in mouse brain tissue 5 - to 25-fold higher than in plasma, [16] and has shown greater penetration of the BBB in mouse models than gefitinib, rociletinib, or afatinib.
[21] In the recently presented FLAURA study, in which
osimertinib was used in untreated patients with advanced EGFR - mutant NSCLC, the HR for systemic disease control and CNS control similarly favored
osimertinib over erlotinib or gefitinib, supporting the preclinical data that
showed osimertinib's penetration across the BBB and providing support for using this agent in first - line management of EGFR - mutant patients with brain metastases.