trophoblast cell surface antigen-2 antibody-drug conjugate

Trophoblast cell surface antigen-2 (TROP-2) antibody-drug conjugates (ADCs) are a class of targeted cancer therapeutics designed to deliver potent cytotoxic payloads specifically to cells expressing the TROP-2 protein. TROP-2 is a transmembrane glycoprotein overexpressed in various epithelial tumors, including non-small cell lung cancer (NSCLC), breast cancer, and urothelial carcinoma, while having limited expression in normal tissues. These ADCs typically consist of a humanized monoclonal antibody targeting TROP-2, a chemical linker (often cleavable), and a cytotoxic agent (payload), most commonly a topoisomerase I inhibitor such as SN-38 or deruxtecan. Upon binding to TROP-2 on the tumor cell surface, the ADC is internalized via endocytosis, and the payload is released intracellularly, leading to DNA damage and cell death. Key agents in this class include sacituzumab govitecan (approved for breast and urothelial cancers), datopotamab deruxtecan, and sacituzumab tirumotecan (both in late-stage development for NSCLC).

Other names

TROP-2 ADCTROP2 ADCTROP 2 ADCTrop-2-directed antibody-drug conjugateTrop2-directed antibody-drug conjugateTrop 2-directed antibody-drug conjugateTrophoblast cell-surface antigen 2-directed antibody-drug conjugate