osimertinib + febuxostat

**Osimertinib + febuxostat** is an investigational oral co-administration regimen being studied in the Phase 2 OSIBBBOOST proof-of-concept trial for patients with **EGFR-mutated metastatic non-small cell lung cancer** without central nervous system metastases and without the ABCG2 34G>A polymorphism. Osimertinib is an irreversible, mutant-selective EGFR tyrosine kinase inhibitor with established antitumor activity in EGFR-mutated NSCLC. Febuxostat is repurposed in this regimen as a potent ABCG2 breast cancer resistance protein inhibitor to reduce transporter-mediated osimertinib efflux at the blood-brain barrier and increase osimertinib exposure in cerebrospinal fluid. The regimen is not a fixed-dose product; its clinical objective is pharmacokinetic enhancement of central nervous system osimertinib penetration.

Other names

febuxostat + osimertinib