befotertinib + itraconazole

The combination of befotertinib and itraconazole is evaluated in drug-drug interaction (DDI) studies to characterize the pharmacokinetic effects of co-administering a strong CYP3A4 inhibitor with a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Befotertinib (developed by Betta Pharmaceuticals in collaboration with InventisBio) is an orally administered small molecule approved in China for the treatment of EGFR T790M mutation-positive non-small cell lung cancer (NSCLC). Itraconazole is a triazole antifungal agent that also acts as a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme, which is primarily responsible for the metabolism of befotertinib. Clinical trials, such as the Phase 1 sequential crossover study NCT07809815, assess how CYP3A4 inhibition by itraconazole alters the systemic exposure, clearance, and safety profile of befotertinib to guide clinical dosing recommendations.

Other names

D-0316 + itraconazolebefotertinib + itraconazolebefotertinib mesylate + itraconazole