Leea macrophylla Roxb. ex hornis a perennial shrub that belongs to the Leeaceae family. The plant has widely been used as a traditional medicine for long time. It is rich in phytochemical constituents such as alkaloids, steroids, glycosides, saponins, carbohydrates, proteins and tannins. Moreover, it has significant therapeutic effects and various preclinical studies have been conducted on the plant to elucidate its pharmacological response which includes antidiabetic, hepatoprotective, antioxidant, antimicrobial, anti-inflammatory, antiurolithiatic and anti-nociceptive, cytotoxic, antithrombotic, neuroprotective, wound healing and cardiotonic activity . The scientific validation is essential for the acceptance of medicinal plants as therapeutic agents against several disorders. Hence, the traditional uses, phytochemical constituents, medicinal significance and pharmacological effects of the plant are discussed in this review.