Abstract: Trastuzumab deruxtecan (DS-8201a) is a novel antibody-drug conjugate (ADC) of human epidermal growth factor receptor 2 (HER2) targeted antibody and DNA topoisomerase Ⅰ inhibitor (deruxtecan, DXd). DS-8201a has the characteristics of loading new cytotoxic drugs, high proportion of drug antibodies and high cell membrane permeability. Compared to traditional anti-HER2 drugs only aimed at patients with overexpression of HER2, DS-8201a can also play a role in tumors with high and low expressions of HER2. So far, phase Ⅰ to Ⅲ clinical trials have been carried out in a variety of solid tumors, such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer. Studies have shown results, including indications, toxicity and safety, determination of effective dose, comparison with existing first-line and posterior-line standard chemotherapy regimens, and efficacy comparison between monotherapy and combination therapy. It may provide a new therapeutic method for clinical treatment of tumors with overexpression or low expression of HER2, and pulmonary symptoms should be monitored during use. In this review, the drug structure characteristics, related clinical research progress and prospect of DS-8201a were summarized.

Key words: Human epidermal growth factor receptor 2, Antibody-drug conjugate, Breast cancer, Stomach cancer, Non-small cell lung cancer, Colorectal cancer