The leaves of Ficus carica Linn. (FC) have been widely used for medicine purposes since ancient times, and its decoction is consumed as tea. Many scientific papers have been published in the literature and the researchers across the world are still exploring the health benefits of FC leaves. In this review, we have collected the literature published since 2010 in the databases: Pubmed, Scopus, Web of Science, SciFinder, Google Scholar, Baidu Scholar and local classic herbal literature. The summary of the chemical constituents in FC leaves, biological activities, toxicity studies, and clinical studies carried out on FC leaves is provided in this review. In addition, the molecular mechanisms of the active constituents in FC leaves are also comprehended. FC leaves are reported to 126 constituents out of which the polyphenolic compounds are predominant. Many scientific studies have proven the antidiabetic, antioxidant, anti-inflammatory, anticancer, anticholinesterase, antimicrobial, hepatoprotective, and renoprotective activities. Many studies have carried out to provide the insights on molecular pathways involved in the biological activities of FC leaves. The toxicity studies have suggested that FC leaves exhibit toxicity only at very high doses. We believe this review serve as a comprehensive resource for those who are interested to understand the scientific evidence that support the medicinal values of FC leaves and also the research gaps to further improve the commercial value and health benefits of FC leaves.