AZD3759 (Zorifertinib) is a potent, orally active, BBB-penetrating EGFR inhibitor (IC50=7.2 nM, L858R pEGFR).
AZD3759 fully penetrate the blood-brain barrier (BBB), with equal free concentrations in the blood, cerebrospinal fluid, and brain tissue; causes tumor regression in subcutaneous xenograft, leptomeningeal metastasis (LM), and brain metastasis (BM) lung cancer models and prevents the development of BM in nude mice.
