trastuzumab-DLP1

Trastuzumab-DLP1 is an experimental antibody-drug conjugate (ADC) that targets the Human Epidermal Growth Factor Receptor 2 (HER2). It consists of the monoclonal antibody trastuzumab site-specifically conjugated to a novel dual-linker payload known as DLP1, with a drug-to-antibody ratio (DAR) of 4. The DLP1 payload is unique in that it combines two distinct mechanisms of action: a topoisomerase I inhibitor and a microtubule inhibitor. This dual-payload approach is designed to enhance cytotoxic potency and mitigate the development of resistance often seen with single-payload ADCs. In preclinical studies, trastuzumab-DLP1 demonstrated significant antitumor activity against various HER2-expressing cancer models, including breast, gastric, and colorectal cancers, and served as a key comparator for the biparatopic ADC TJ106.