Phillyrin (PHI) is one of the main active components in Forsythia suspensa (Thunb.) Vahl, belonging to the class of lignans, which has anti‐inflammatory, antioxidant, anti‐tumor, antiviral, antibacterial, weight loss and other pharmacological effects, involving a variety of potential signaling pathways, such as TLR, NF‐κB, PI3K/AKT, NRF2, PPAPs signaling pathways. The review search systematically and comprehensively CNKI, Wanfang, PubMed, Web of Science and other databases, screened nearly 100 relevant literature in the past five years, and summarized and evaluated the information of PHI extraction and purification, pharmacological activity, potential mechanism and structure‐activity relationship. And further discusses the pharmacological effects of PHI and potential molecular mechanisms. The results of the review confirm that PHI has the potential to be developed into a therapeutic anti‐inflammatory, anti‐tumor and other therapeutic agents, all of which provide a scientific basis and direct reference for the pharmacological research of PHI.