Spathodea campanulata P. Beauv., belonging to the family Bignoniaceae, is a big erect tree with an ancient history of medicinal use in Africa. In the traditional system, it is mentioned for the treatment of malaria, diabetes, stomach ulcers, wounds, skin infections and viral diseases. The aim of the review is to make available the current information that exists on the traditional uses, phytochemistry, pharmacology, and toxicology of S. campanulata. Additionally, the potential uses of this plant to treat various diseases and to bring in a foundation for further research are emphasized. The present review is carried out by compiling literature from 1972 to 2021, concerning the morphology, traditional uses, phytochemistry, pharmacological activities, and toxicological aspects of S. campanulata. Literatures were collected from various online search engines, viz. Google Scholar, PubMed, Science Direct, Core, and Semantic Scholar. Diverse chemical compounds including iridoids, terpenoids, steroids, cinnamic acid derivatives, cerebrosides, flavonoids, and carotenoids have been isolated from this plant. Mostly in-vivo models have indicated several evidences of the use of this plant particularly to cure malaria. Few in-vivo studies have also proved the usefulness of this plant in inflammation, wound healing, diabetes, and convulsion. In some in-vitro studies, the anticancer, antibacterial, antiviral insecticidal, larvicidal, and anti-oxidant potential has been proved. Preclinical studies have demonstrated remarkable activity which supports the conventional use of the plant as an antimalarial, wound healing, antidiabetic, antimicrobial, and anti-inflammatory agent for years without any adverse effects. Based on the results obtained from a combination of in vivo and in vitro potency and toxicity studies reported, S. campanulata is a promising agent in the development of nutraceuticals against malaria and diabetes. Although few phytochemicals isolated (ursolic acid, tomentosolic acid, 20β-hydroxyursolic acid, verminoside, specioside, spathoside, kaempferol, and β-sitosterol-3-acetate) from the plant exhibited remarkable biological activity, it was only confined to preclinical study. The only clinical study documented is for curing malaria, but with crude extract only. With its current extensive traditional use, there is a need for additional studies of the isolated compounds, clinical trials, and product development to take full advantage of this widely distributed medicinal plant.