Icacinaceae, an Angiospermic family comprising 35 genera and 212 accepted species, including trees, shrubs, and lianas with pantropical distribution, is one of the most outshining yet least explored plant families, which despite its vital role as a source of pharmaceuticals and nutraceuticals has received a meagre amount of attraction from the scientific community. Interstingly, Icacinaceae is considered a potential alternative resource for camptothecin and its derivatives, which are used in treating ovarian and metastatic colorectal cancer. However, the concept of this family has been revised many times, but further recognition is still needed. The prime objective of this review is to compile the available information on this family in order to popularize it in the scientific community and the general population and promote extensive exploration of these taxa. The phytochemical preparations or isolated compounds from the Icacinaceae family have been centrally amalgamated to draw diverse future prospects from this inclusive plant species. The ethnopharmacological activities and the associated endophytes and cell culture techniques are also depicted. Nevertheless, the methodical evaluation of the Icacinaceae family is the only means to preserve and corroborate the folkloristic remedial effects and provide scientific recognition of its potencies before they are lost under the blanket of modernization.