Launaea taraxacifolia (Willd.) Amin ex C. Jeffrey is a herb found mostly in tropical Africa. The plant, commonly found in West Africa, is used in the management of many diseases including cardiovascular, respiratory, haematological, endocrine, and metabolic diseases in Ghana, Nigeria, Benin, Serra Leone, and Senegal. This piece provides comprehensive and updated information on the traditional uses, phytochemical constituents, and pharmacological and toxicological information available on Launaea taraxacifolia to support its medicinal uses and also unearth knowledge gaps for future studies. An electronic literature search using search engines, namely, Google Scholar, ScienceDirect, and PubMed, was carried out to obtain information on the plant. Both common and scientific names of the plant were used as keywords for the search process. This paper captured information on Launaea taraxacifolia from 1985 to 2018. The search revealed that the leaves of the plant possess nutritional/pharmacological effects on diseases such as diabetes mellitus, hypertension, cancer, malaria, bacterial infections, and arthritis. The leaf has been shown to be a rich source of phytoconstituents such as flavonoids, phenolic acids, tannins, alkaloids, glycosides, coumarins, triterpenoids, ascorbic acid, lycopene, and β-carotene. Also, isolated phytoconstituents as well as the safety profile of the plant have been documented. This review on Launaea taraxacifolia has provided a one-stop documentation of information in support of the several purported ethnopharmacological uses of the plant. It also reveals information gaps such as the need to research into its pharmacokinetics, interactions with drugs of importance, and its development into a plant-based drug in order to expand its clinical use.