HER2-directed antibody–drug conjugate with a topoisomerase I inhibitor payload (DXd).
HER2-targeted monoclonal antibody linked via a cleavable linker to the topoisomerase I inhibitor deruxtecan (DXd). After HER2 binding and internalization, DXd is released to inhibit Top1–DNA complexes, blocking DNA replication and causing cell-cycle arrest and apoptosis; also mediates ADCC and a bystander killing effect.
HER2-binding ADC is internalized and releases the topoisomerase I inhibitor deruxtecan, causing DNA damage/replication block, cell-cycle arrest and apoptosis; it also mediates ADCC and a bystander killing effect.
Humanized monoclonal antibody targeting HER2 (ERBB2); binds the extracellular domain to block receptor signaling and dimerization, reduces receptor shedding, and induces antibody-dependent cell-mediated cytotoxicity against HER2-overexpressing tumor cells.
Trastuzumab binds HER2 on target cells and recruits FcγR-expressing immune cells to mediate ADCC (and some CDC), killing HER2+ cells; it also blocks HER2 signaling, promoting apoptosis.
ATP-competitive, selective TRK (TRKA/B/C; NTRK1/2/3) tyrosine kinase inhibitor that blocks neurotrophin-TRK signaling and downstream pathways (e.g., MAPK/ERK, PI3K/AKT), leading to growth inhibition and apoptosis, particularly in tumors harboring NTRK gene fusions.
ATP-competitive inhibition of TRKA blocks neurotrophin-TRK signaling (e.g., MAPK/ERK, PI3K/AKT), leading to growth arrest and apoptosis in NTRK-driven cells.