lucamtasutab

Lucamtasutab (formerly known as sacituzumab tirumotecan, SKB264, or MK-2870) is a TROP-2-directed antibody-drug conjugate (ADC) developed by Kelun-Biotech and licensed to Merck & Co. (MSD) for global development outside of Greater China. The molecule consists of a humanized monoclonal antibody targeting trophoblast cell-surface antigen 2 (TROP-2) conjugated to a novel topoisomerase I inhibitor payload (a belotecan derivative) via a pH-sensitive carbonate linker. TROP-2 is a transmembrane glycoprotein overexpressed in a variety of epithelial tumors, including non-small cell lung cancer (NSCLC), triple-negative breast cancer (TNBC), and gastric cancer. Upon binding to TROP-2, the ADC is internalized, and the payload is released within the acidic environment of the endosome/lysosome, where it inhibits DNA topoisomerase I, causing double-strand DNA breaks and subsequent cell death. Lucamtasutab is currently in Phase 3 clinical development for several indications, including NSCLC and TNBC, both as a monotherapy and in combination with other agents like pembrolizumab.

Other names

sacituzumab tirumotecan