The growing preference for natural remedies has resulted in increased use of medicinal plants. One of the most significant and varied plants is garden cress (Lepidium sativum), which has large concentrations of proteins, fatty acids, minerals, and vitamins. It also contains a wide range of bioactive components, including kaempferol glucuronide, gallic acid, protocatechuic acid, coumaric acid, caffeic acid, terpenes, glucosinolates, and many more. These substances, which include antioxidant, thermogenic, depurative, ophthalmic, antiscorbutic, antianemic, diuretic, tonic, laxative, galactogogue, aphrodisiac, rubefacient, and emmengogue qualities, add to the medicinal and functional potential of garden cress. An extensive summary of the phytochemical profile and biological activity of garden cress seeds is the main goal of this review. Research showed that garden cress is one of the world's most underutilized crops, even with its nutritional and functional profile. Consequently, the goal of this review is to highlight the chemical and nutritional makeup of Lepidium sativum while paying particular attention to its bioactive profile, various health claims, therapeutic benefits, and industrial applications.