Sacituzumab tirumotecan — Investigational Agent
Antibody-Drug Conjugate · Phase 3 · Merck / Kelun-Biotech
Mechanism of Action
Sacituzumab tirumotecan is a TROP2-directed antibody-drug conjugate. It consists of a humanized monoclonal antibody targeting the tumor-associated calcium signal transducer 2 (TROP2) conjugated to a novel topoisomerase I inhibitor payload (KL610023) via a stable, pH-sensitive linker. Upon binding to TROP2-expressing tumor cells, the ADC is internalized, and the payload is released within the acidic environment of the endosome and lysosome. The released payload induces DNA damage and apoptosis, and its membrane-permeable nature allows for a bystander effect on neighboring tumor cells.
Investigational Indications
- Triple-negative breast cancer (TNBC)
- HR+/HER2- breast cancer
- Non-small cell lung cancer (NSCLC)
- Endometrial carcinoma
- Gastric cancer