zorifertinib + osimertinib

zorifertinib + osimertinib is a combination therapy comprising two epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). Zorifertinib (AZD3759) is a small molecule inhibitor specifically engineered for 100% blood-brain barrier penetration, as it is not a substrate for P-gp or BCRP efflux pumps, making it highly effective against central nervous system (CNS) metastases. Osimertinib is a third-generation, irreversible EGFR-TKI that targets both EGFR-sensitizing mutations and the T790M resistance mutation. This combination is primarily being evaluated for the treatment of patients with advanced EGFR-mutated non-small cell lung cancer (NSCLC) who have developed leptomeningeal metastases (LM) and have progressed following prior treatment with osimertinib monotherapy. The combination aims to leverage the superior CNS penetration of zorifertinib alongside the systemic efficacy of osimertinib to overcome intracranial resistance.

Other names

Zorifertinib and Osimertinib Combination Therapy