Fallopia convolvulus (L.) Á. Löve, a widely distributed species of the Polygonaceae family, has long been valued in traditional medicine for its diverse therapeutic applications. This review investigates its phytochemical composition, traditional uses, and pharmacological potential, placing the plant in the broader context of natural product research. Bioactive compounds such as flavonoids, anthraquinones, steroids, and phenolic acids, which exhibit antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, are compiled and analyzed. Modern techniques have identified novel compounds like falloconvolin A and B, as well as compounds with estrogenic and neuroprotective properties. To support this analysis, information was sourced from ethnobotanical, phytochemical, pharmacological, and clinical studies, utilizing databases like PubMed, Science Direct, and ResearchGate. This comprehensive analysis underscores the importance of further research to elucidate the mechanisms of action of its bioactive constituents and to explore its potential for pharmaceutical innovation. Fallopia convolvulus represents a promising, sustainable resource for developing novel therapeutic agents, bridging traditional medicine with modern science.