Gmelina arborea Roxb. has been widely used in traditional medicine and is considered a vital component of Brihatpanchamoolya. It is also commonly used in modern medicine due to its rich content of phytochemicals. The primary constituents include lignans, flavonoids, tannins, glycosides and other bioactive compounds. Notably, the roots of Gmelina arborea contain glycosides, particularly flavone glycosides such as apigenin-7-rutinoside, luteolin-7glucuronide, sitosterol, quercetin and apigenin. The leaves are rich in iridoid glycosides, flavonoids and sterols. The stem contains several lignans, including gmelanone, iso-arboreal, paulownin and gmelinol. Additionally, the flower contains verbascoside, a compound belonging to the class of iridoid glycosides. This species has diverse pharmaceutical applications, including antiinflammatory properties. It also exhibits a wide range of beneficial effects, such as antioxidant, hepatoprotective, anticancer, neuroprotective, anti-tumour, cardioprotective, anticonvulsant and antihyperlipidemic activities. This study aims to bridge the gap between traditional knowledge and modern research by examining the pharmacological and phytochemical properties of G. arborea. A comprehensive review was conducted using well-known academic databases, including PubMed, Google Scholar and Science Direct. The findings were summarized and documented using bibliographic information, which may pay the way for future researcher in this area.