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.
YES
DIRECT
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.
YES
DIRECT
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.
TROP-2–directed antibody–drug conjugate delivering SN-38 (topoisomerase I inhibitor).
Humanized anti-TROP2 monoclonal antibody linked to SN-38 (active metabolite of irinotecan). After binding TROP2 on tumor cells and internalization, the linker is cleaved to release SN-38, which inhibits topoisomerase I by stabilizing the Topo I–DNA complex, leading to DNA damage, replication arrest, and apoptosis (with potential bystander effect).
YES
DIRECT
ADC binds TROP-2 on target cells, is internalized, and releases SN-38, which inhibits topoisomerase I, causing DNA damage and apoptosis (with possible bystander effect).