osimertinib + datopotamab deruxtecan

This combination consists of **osimertinib**, a third-generation small molecule **epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor**, and **datopotamab deruxtecan**, an **antibody-drug conjugate (ADC)** targeting TROP2 (trophoblast cell surface antigen 2). Osimertinib blocks EGFR signaling, a major driver of cell proliferation in EGFR-mutant non-small cell lung cancer (NSCLC), while datopotamab deruxtecan delivers a cytotoxic **topoisomerase I inhibitor payload** via a TROP2-directed monoclonal antibody, selectively targeting and killing TROP2-expressing cancer cells. The combination is under evaluation primarily for advanced or metastatic EGFR-mutant NSCLC, with rationale based on preclinical evidence that osimertinib upregulates TROP2, augmenting ADC targeting and efficacy. Both drugs are independently approved for other indications, but the combination is investigational[1][3][5][6][7].

Other names

osimertinib + Dato-DXdosimertinib + DS-1062a