Subcutaneous xenograft models were established for <i>in vivo</i> tumor-suppressive activity evaluation, and patient-derived organoid models validated its potential clinical efficacy.<h4>Results</h4>In preclinical models, SHR-A1921 specifically bound to Trop-2, followed by internalization into tumor cells and subsequent intracellular trafficking to lysosomes, where the release of SHR9265 occurred. The gene discussed is TACSTD2; the disease is neoplasm.