Trastuzumab rezetecan — Investigational Agent
Antibody-Drug Conjugate · Phase 3 · Jiangsu HengRui Medicine
Mechanism of Action
Trastuzumab rezetecan is a HER2-directed antibody-drug conjugate composed of a trastuzumab-based humanized anti-HER2 monoclonal antibody linked via a cleavable tetrapeptide linker to a novel topoisomerase I inhibitor payload (SHR9265). Upon binding HER2 on tumor cells, the ADC is internalized and lysosomally processed, releasing the membrane-permeable payload that induces DNA damage and apoptosis. Its high drug-to-antibody ratio and bystander effect allow killing of adjacent HER2-low or heterogeneous tumor cells. This positions it for both HER2-positive and HER2-low breast cancer.
Investigational Indications
- HER2-positive metastatic breast cancer
- HER2-low breast cancer
- HER2-expressing gynecologic and solid tumors