On July 19, 2022, AstraZeneca announced that its HER2-targeted ADC drug Enhertu, developed in collaboration with Daiichi Sankyo, had been approved in the European Union as a monotherapy for patients with HER2-positive metastatic breast cancer who have received one or more prior anti-HER2-based regimens. This approval expands Enhertu's indication in Europe to include early-stage HER2-positive metastatic breast cancer.
Enhertu is a specially designed HER2-targeting antibody-drug conjugate (ADC) that links the humanized monoclonal antibody trastuzumab to a highly active topoisomerase I inhibitor derivative (DXd) via a 4-peptide linker. The two bind very strongly and are very stable in plasma. When HER2-positive breast cancer cells take up DS-8201, they release DXd after intracellular lysosomal enzymatic cleavage, which precisely kills tumor cells, thereby improving efficacy and reducing the occurrence of adverse reactions.
