Phytolacca acinosa Roxb. is a valuable multipurpose medicinal herb used in traditional Chinese and other Asian folklore medicine systems to treat numerous diseases like eye disorders, body aches, swelling, edema, and sores. However, no comprehensive review has yet synthesized the diverse scientific studies on P. acinosa. To address this gap, this study compiles a global review by gathering scattered information on the taxonomy, ethnomedicine, pharmacology, phytochemistry, in vitro propagation, and toxicology of P. acinosa and explore the avenues for future research. The data about P. acinosa was gathered through internet search using relevant keywords in online databases like Google Scholar, Scopus, Web of Science, PubMed, Science Direct, CNKI, ResearchGate, and Wiley Online Library. Moreover, books offering comprehensive reviews of relevant literature were consulted for reference. The formulae and chemical structures of compounds were validated through the PubChem database and ChemDraw Ultra 11.0 was used to draw these structures. This review highlights the extensive ethnomedicinal properties of P. acinosa, which has been used in traditional medicine for centuries. Phytochemical analyses have identified a wide range of secondary metabolites, including phenolics, tannins, flavonoids, saponins, flavones, triterpenoids, polysaccharides, and glycosides. The literature review shows that P. acinosa has significant pharmacological effects, such as antimicrobial, anti-tumor, antioxidant, antiviral, anti-inflammatory, toxicological, and molluscicidal properties. Pharmacological investigations have partially validated its traditional and indigenous uses. However, despite its high therapeutic potential, several studies have reported the toxic effects on living organisms. This review underscores the need for more ethnopharmacological and toxicological investigations to ensure the safe medicinal use of P. acinosa. Furthermore, the review highlights the significant potential of P. acinosa for future drug discovery and development, positioning it as a promising plant for further commercial exploitation in the pharmaceutical industry.