Lawsonia inermis Linn, commonly known as henna, is a member of the Lythraceae family and has been found to contain a variety of compounds with both industrial and medicinal applications in its stem, bark, roots, flowers, and seeds. This report provides a comprehensive review of the bioactive components, pharmacological activities, pharmacokinetics, and pharmacological side effects of Lawsonia inermis. Relevant materials were gathered from Google Scholar, PubMed, Scopus, and Web of Science and reviewed for important properties and updates about the plant. Lawsonia inermis contains a variety of bioactive compounds, including flavonoids, coumarins, triterpenoids, steroids, xanthones, polyphenols, fatty acids, alkaloids, quinones, tannins, leucocyandin, epicatechin, catechin, and quercetin. The plant is been traditionally used to treat numerous conditions, including ulcers, bronchitis, lumbago, hemicrania, leukoderma, scabies, boils, ophthalmic disorders, hair loss, and jaundice. It has also been found to possess a range of pharmacological activities, including antioxidant, anti-inflammatory, analgesic, antiparasitic, hepatoprotective, antifungal, antitumor, wound healing, and hypoglycemic effects. The potential of Lawsonia inermis for various biological applications is promising, and further studies are needed to fully explore its therapeutic benefits for various diseases of public health. Concern advances in drug development could enable the characterization of various bioactive constituents and facilitate their development and application for the benefit of humanity.