Colebrookea oppositifolia Sm. is a valuable traditional therapeutic plant belonging to the family Lamiaceae. It is a dense and wool-like shrub that is mostly found in subtropical regions of some countries of Asia, such as China and India. It has been widely used for the mitigation of nervous system disorders like epilepsy. The active constituents of the plant have exhibited antioxidant, anti-microbial, and antifungal properties, which are considered due to the presence of polyphenols and flavonoids as chief chemical constituents. Flavonoids like quercetin, landenein, chrysin, and 5, 6, 7-trimethoxy flavones cause protein denaturation of the microbial cell wall.To comprehend and assemble the fragmented pieces of evidence presented on the traditional uses, botany, phytochemistry, and pharmacology of the plant to reconnoiter its therapeutic perspective and forthcoming research opportunities.The available information on Colebrookea oppositifolia has been established by electronically searching peer-reviewed literature from PubMed, Google Scholar, Springer, Scopus, Web of Science, and Science Direct over the earlier few years.The plant has been greatly used for the preparation of many herbal medicines which are used for treating traumatic injuries, fever, rheumatoid arthritis, headache, and gastric problems. From the aerial parts of the plant, a phenylethanoid glycoside named acteoside has been isolated and evaluated for its therapeutic potential viz. immunomodulatory, neuroprotective, hepatoprotective, analgesic, anti-tumour, antispasmodic, antioxidant, antibacterial, free radical scavenger, and improving sexual function. Acteoside showed neuroprotective activities against Aβ-peptide, which is neurotoxic and causes apoptosis. The petroleum ether extract of the plant leaves offers many active compounds like sitosterol, n-triacontane, hydroxydotriacontyl ferulate, acetyl alcohol, and 3,7,4,2-tetramethoxyflavones which have shown hepatoprotective potential.The plant should be evaluated further for the estimation of some other health benefits. The consequences of restricted pharmacological screening and reported phytomolecules of Colebrookea oppositifolia Sm. advocate that there is still an exigent requisite for in-depth pharmacological studies of the plant.Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.