As the first domestically originated cell cycle protein-dependent kinase 4/6 inhibitor, dalpiciclib has been approved by the State Drug Administration for the treatment of hormone receptor-positive/human epidermal growth factor receptor 2-negative advanced or metastatic breast cancer in combination with fulvestrant or aromatase inhibitors. This article focuses on the progress of dalpiciclib research in breast cancer, summarizing the drug's mechanism of action, phase I-III clinical trials, and drug safety issues.