trastuzumab-PEG6-DM1

Trastuzumab-PEG6-DM1 is an antibody-drug conjugate (ADC) consisting of the anti-HER2 monoclonal antibody trastuzumab conjugated to the cytotoxic agent DM1 (a maytansine derivative) via a PEG6 (polyethylene glycol with 6 units) linker. It targets the human epidermal growth factor receptor 2 (HER2), which is overexpressed in various cancers, most notably breast cancer. The ADC is designed to deliver the microtubule-inhibiting payload DM1 directly to HER2-positive cells, where it is internalized and released to induce cell cycle arrest and apoptosis. Preclinical research indicates that this specific formulation, featuring a PEG6 linker and an average drug-to-antibody ratio (DAR) of approximately 3, may be effective against trastuzumab-resistant and T-DM1-resistant breast cancer. It has also been utilized as a platform for developing radiolabeled versions for immunoPET imaging and targeted radiotherapy.