trastuzumab-based antibody-drug conjugates

Trastuzumab-based antibody-drug conjugates (ADCs) are a class of targeted cancer therapeutics consisting of the anti-HER2 humanized monoclonal antibody trastuzumab (or its derivatives) covalently linked to a cytotoxic payload. By binding to the extracellular domain of Receptor tyrosine-protein kinase erbB-2 (HER2/ERBB2), these ADCs undergo receptor-mediated endocytosis, delivering the cytotoxic payload directly into HER2-overexpressing tumor cells. This targeted delivery minimizes systemic toxicity while maximizing tumor cell death. Key approved examples include trastuzumab emtansine (T-DM1), which delivers a microtubule-inhibiting maytansinoid payload, and trastuzumab deruxtecan (T-DXd), which delivers a topoisomerase I inhibitor payload. Depending on the linker and payload properties, some of these ADCs can also exert a bystander effect, killing neighboring low-HER2-expressing tumor cells.

Other names

HER2-targeting antibody-drug conjugatesHER-2-targeting antibody-drug conjugatesHER 2-targeting antibody-drug conjugatestrastuzumab ADCstrastuzumab-based ADCs