sacituzumab tirumotecan + fluorouracil + leucovorin

**Sacituzumab tirumotecan + fluorouracil + leucovorin** is an investigational combination regimen comprising an antibody-drug conjugate (ADC), *sacituzumab tirumotecan*, together with the chemotherapeutic agent *fluorouracil* (5-FU) and the folate analog *leucovorin*. Sacituzumab tirumotecan is composed of an anti-TROP2 monoclonal antibody conjugated via a cleavable linker to a belotecan-derived topoisomerase I inhibitor payload. The ADC delivers cytotoxic drug specifically to TROP2-expressing tumor cells, leading to DNA damage and cell death. Fluorouracil is a pyrimidine analog antimetabolite that inhibits thymidylate synthase, interfering with DNA synthesis. Leucovorin enhances the cytotoxic action of fluorouracil by stabilizing the binding of fluorouracil metabolite to thymidylate synthase. This regimen is under clinical investigation for advanced gastrointestinal cancers, including colorectal cancer, pancreatic ductal adenocarcinoma, and biliary tract cancer, as well as for gastric, gastroesophageal junction, and esophageal adenocarcinoma[1][3][5][7]. The combination aims to exploit targeted delivery of cytotoxic payloads with sacituzumab tirumotecan and potentiate the effect with standard cytotoxic chemotherapy.

Other names

sac-TMT + 5-FU + leucovorinMK-2870 + 5-fluorouracil + leucovorin