A bibliographic investigation was carried out by gathering and analyzing the recognized books, including Chinese herbal classic, the Internet (Google Scholar, Baidu Scholar), and scientific databases (Pubmed, Scifinder, Scopus, CNKI, ACS, and Web of Science) for available information on Euphorbia hirta. Whole plants of E. hirta have been used in traditional Chinese medicine (TCM) due to its properties that can cure and detoxify fever, promote diuresis, stop itching, and induce prolactin. Traditional uses of E. hirta are also recorded in some other pan-tropical areas, where it has been used for over 10 types of diseases. A number of chemical constituents, including flavonoids, terpenoids and phenols, have been isolated and identified from E. hirta. Various biological evaluations have been reported for its importance. Modern pharmacological investigation demonstrated that its crude extracts and active compounds possesses wide pharmacological effects, such as antibacterial, anti-inflammatory, antioxidant, sedative and anti-allergy. The current study summarizes the updated information concerning the ethnopharmacology, phytochemistry, and pharmacology of E. hirta as well as its toxicology, and discusses the existing problem and future research direction of E. hirta.