trastuzumab deruxtecan + fluorouracil + leucovorin

Trastuzumab deruxtecan is an antibody-drug conjugate composed of a humanized anti-HER2 monoclonal antibody (trastuzumab) linked to a topoisomerase I inhibitor payload (deruxtecan) via a cleavable peptide-based linker. It targets HER2-expressing tumor cells and delivers the cytotoxic agent directly into these cells after internalization, leading to DNA damage and apoptotic cell death. The drug exhibits a strong bystander effect due to the membrane permeability of its payload[1][3][5][6]. Trastuzumab deruxtecan is primarily indicated for HER2-positive cancers such as breast cancer, gastric cancer, non-small cell lung cancer, and has shown activity in colorectal cancer with HER2 overexpression[5][6][7]. Fluorouracil (5-FU) is an antimetabolite chemotherapy that inhibits thymidylate synthase and disrupts DNA synthesis. Leucovorin enhances the binding of 5-FU to thymidylate synthase, increasing its efficacy. This combination regimen may be used in clinical trials or off-label settings for advanced or metastatic cancers with HER2 expression.

Other names

fam-trastuzumab deruxtecan-nxkiDS-8201aDS8201aDS 8201a