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This is a combination therapy consisting of osimertinib, a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), and sacituzumab tirumotecan (also known as sac-TMT or SKB264), a trophoblast cell-surface antigen 2 (TROP2)-directed antibody-drug conjugate (ADC). Osimertinib irreversibly binds to specific mutant forms of EGFR (T790M, L858R, and exon 19 deletions), inhibiting tumor cell growth. Sacituzumab tirumotecan consists of a humanized monoclonal antibody targeting TROP2, linked to a belotecan-derivative topoisomerase I inhibitor payload (KL610023) via a novel linker. This combination is being investigated by the Guangdong Association of Clinical Trials in a Phase II study for patients with EGFR-mutated advanced non-small cell lung cancer (NSCLC) who exhibit persistent circulating tumor DNA (ctDNA) after initial osimertinib treatment, as well as in Phase III trials for EGFR-mutant NSCLC.
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