TROP2-targeted Antibody-Drug Conjugate

TROP2-targeted Antibody-Drug Conjugates (ADCs) represent a class of anticancer drugs designed to selectively deliver potent cytotoxic agents to tumor cells that overexpress Trophoblast cell surface antigen 2 (TROP2). TROP2 is a transmembrane glycoprotein involved in various cellular signaling pathways, including calcium signal transduction, MAPK, PI3K/AKT, ERK, and JNK, which contribute to cell proliferation, invasion, and metastasis. Its high expression in numerous solid tumors, such as breast, lung, urothelial, pancreatic, cervical, and gastric cancers, makes it an attractive therapeutic target. The mechanism of action involves a monoclonal antibody that specifically binds to TROP2 on the surface of cancer cells. Upon binding, the ADC is internalized, and a cleavable linker releases a cytotoxic payload, typically a topoisomerase I inhibitor or a microtubule inhibitor, directly into the tumor cell, leading to cell death. This targeted delivery aims to maximize efficacy while minimizing systemic toxicity to healthy tissues. Several TROP2 ADCs are currently approved or in various stages of clinical development by companies like Gilead Sciences, AstraZeneca, Daiichi Sankyo, and Merck.

Other names

TROP2-directed ADCTROP-2-directed ADCTROP 2-directed ADC