TROP2-targeting MMAE Antibody-Drug Conjugate

TROP2-targeting MMAE Antibody-Drug Conjugates (ADCs) represent a class of highly potent antineoplastic agents designed to selectively deliver the cytotoxic payload Monomethyl auristatin E (MMAE) to cancer cells that overexpress Trophoblast cell surface antigen 2 (TROP2). TROP2 is a transmembrane glycoprotein frequently overexpressed in various solid tumors, including breast, gastric, ovarian, pancreatic, and lung cancers, and its overexpression is often associated with aggressive disease and poor prognosis. The ADC consists of an anti-TROP2 monoclonal antibody, a cleavable linker, and MMAE. Upon administration, the antibody component binds specifically to TROP2 on the surface of tumor cells. The ADC-antigen complex is then internalized into the cell via endocytosis. Within the lysosomal compartment, the linker is cleaved by lysosomal enzymes, releasing free MMAE into the cytoplasm. MMAE, a synthetic derivative of dolastatin 10, exerts its potent antimitotic effect by binding to tubulin and inhibiting its polymerization, thereby disrupting microtubule dynamics, leading to G2/M phase cell cycle arrest and ultimately inducing apoptosis in the targeted cancer cells. This targeted delivery mechanism aims to maximize efficacy against TROP2-expressing tumors while minimizing systemic toxicity associated with unconjugated MMAE.

Other names

MMAE-TROP2 ADCMMAE-TROP-2 ADCMMAE-TROP 2 ADC