Background: Pseudoprotodioscin (PPD) is a prominent active steroidal saponin isolated from plants of the genus Dioscorea. Investigations have shown that PPD exhibits considerable biological activity and has great clinical potential. Methods: Dioscorea plants and pseudoprotodioscin were used as search terms for study retrieval. Studies involving PPD were collected from a wide range of databases, including China National Knowledge Infrastructure, PubMed, Web of Science, and Elsevier, as well as relevant scientific websites. Results: PPD possesses multiple bioactive properties, such as anticancer, anti-inflammatory, hepatoprotective, and cardioprotective effects. Pharmacokinetic studies in rats indicated that PPD undergoes rapid excretion and has low bioavailability (5.7%), which need to develop a more effective drug delivery system to modify, such as lipid-based nanoparticles. Additionally, Chinese patent medicines containing PPD have shown promising clinical applications in related diseases. Conclusions: This review highlights the therapeutic potential of PPD and its related Chinese patent medicines, providing a foundation for future research and clinical development. Further studies are required to optimize the pharmacokinetic profile of PPD and explore its full pharmacological potential and underlying mechanisms.