Edible medicinal plants are important sources for the development of health beneficial products and drugs. Several species of the genus Spatholobus are considered as medicinal and food homologous plants in various Asian countries for the treatment of menstrual pain, anemia, paralysis, arthralgia, etc. Regarding this genus, mounting investigations on different aspects have been conducted; however, a comprehensive review about these findings is yet to be compiled. Herein, we reviewed the up-to-date information on the botanical description, distribution, ethnopharmacology, phytochemistry, pharmacology, and toxicology of the Spatholobus species for the first time to support their development potential. Thus far, 175 phytochemicals have been isolated, and flavonoids are the predominant constituents. Furthermore, 141 compounds show the ideal characteristic behavior of a drug-like molecule. Besides, the compounds and crude extracts of this genus have been demonstrated to exert a wide range of in vitro and in vivo bioactivities, such as antitumor activity, antioxidant activity, antiinflammatory activity, antiischemic activity, antimicrobial activity, and neuroprotective activity. Toxicity studies have revealed that Spatholobus species seem to have no apparent toxic effects. Even so, the need for in-depth studies to reveal the scientific connotation of the widely documented traditional actions, the structure-activity relationship of the bioactive compounds, and the systematic toxic reactions are warranted, and also to provide essential evidence for the beneficial use of Spatholobus plants and developing novel health care products and therapeutic drug from this genus.