As an outstanding two-dimensional material, black phosphorene, has attracted significant attention in the biomedicine field due to its large surface area, strong optical absorption, distinct bioactivity, excellent biocompatibility, and high biodegradability. In this review, the preparation and properties of black phosphorene are summarized first. Thereafter, black phosphorene-based multifunctional platforms employed for the diagnosis and treatment of diseases, including cancer, bone injuries, brain diseases, progressive oxidative diseases, and kidney injury, are reviewed in detail. This review provides a better understanding of the exciting properties of black phosphorene, such as its high drug-loading efficiency, photothermal conversion capability, high 1 O2 generation efficiency, and high electrical conductivity, as well as how these properties can be exploited in biomedicine. Finally, the research perspectives of black phosphorene are discussed.