tizetatug rezetecan

tizetatug rezetecan is a clinical-stage TROP-2–targeted antibody-drug conjugate developed by Shanghai Hengrui Pharmaceutical for the treatment of advanced solid tumors, including ovarian, breast, lung, salivary gland cancers and other malignant solid neoplasms.[1][3][5][9][12] It consists of a humanized IgG1κ monoclonal antibody against tumor-associated calcium signal transducer 2 (TROP-2/TACSTD2) conjugated via a tetrapeptide-based cleavable linker to the exatecan-derived DNA topoisomerase I inhibitor payload rezetecan (SHR9265), with an average drug–antibody ratio of about 4.[3][7][8][10][12] By binding TROP-2 on tumor cells, the ADC is internalized and releases the topoisomerase I inhibitor intracellularly, causing DNA damage, cell cycle arrest, and apoptosis, and has shown promising antitumor activity with a manageable safety profile across multiple phase 1–3 trials in heavily pretreated patients.[1][3][5][6][9][12]

Other names

tizetatug rezetecan