DS-6157

DS-6157 is an investigational antibody-drug conjugate (ADC) developed for the treatment of gastrointestinal stromal tumors (GIST). It consists of a humanized monoclonal antibody targeting G protein-coupled receptor 20 (GPR20), which is selectively and abundantly expressed in GISTs. The antibody is conjugated via a novel tetrapeptide-based linker to a DNA topoisomerase I inhibitor payload, specifically an exatecan derivative known as DXd. Upon binding to GPR20 on tumor cells, DS-6157 is internalized, and the linker is cleaved by lysosomal enzymes within the cell, releasing the cytotoxic DXd payload that inhibits topoisomerase I and induces apoptosis. Clinical development was discontinued after Phase 1 due to insufficient efficacy[2][3][5][6].

Other names

anti-GPR20/DXd antibody-drug conjugate