Definition

An antibody-drug conjugate (ADC) composed of a monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) conjugated to an as of yet undisclosed topoisomerase inhibitor (TopoI), with potential antineoplastic activity. Upon administration of the anti-TROP-2/TopoI ADC MHB036C, the anti-TROP-2 antibody targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and cleavage, TopoI is released, and inhibits DNA topoisomerase activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of TROP-2-expressing tumor cells. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.