sacituzumab tirumotecan

Sacituzumab tirumotecan is a recombinant humanized IgG1 anti-TROP2 monoclonal antibody-drug conjugate (ADC) designed to target and deliver a cytotoxic payload specifically to TROP2-expressing tumor cells. The ADC consists of an antibody targeting trophoblast cell surface antigen 2 (TROP2), which is highly expressed in various epithelial-derived tumors, conjugated via a proprietary pyrimidine-thiol linker to a belotecan-derivative topoisomerase I inhibitor as the cytotoxic payload. The drug-to-antibody ratio (DAR) is approximately 7.4. Upon binding to TROP2 on cancer cells, the ADC is internalized and releases its topoisomerase I inhibitor payload through both extracellular pH-sensitive cleavage and intracellular enzymatic cleavage, resulting in DNA damage and apoptosis of targeted tumor cells as well as neighboring bystander effect due to membrane-permeable payload release. Sacituzumab tirumotecan has demonstrated significant clinical benefit in heavily pretreated advanced triple-negative breast cancer (TNBC) and non-small cell lung cancer (NSCLC), particularly those with EGFR mutations who have progressed after tyrosine kinase inhibitors and platinum-based chemotherapy[1][3][9].

Brand names

SKB264SKB-264SKB 264

Other names

Sacituzumab TirumotecanSac-TMTMK-2870MK2870MK 2870