Garden cress (Lepidium sativum Linn.), belong to Brassicaceae family, is a fast-growing, edible annual herb and considered as an important medicinal plant and widely grown in several countries. L. sativum seeds, oil, and powder contain high levels of flavonoids, alkaloids, saponins, anthracene glycosides, carbohydrates, proteins, minerals, and fibers, which are incorporated in novel beverages and foods. In Ayurveda, L. sativum is considered as hot, bitter, galactogogue, and aphrodisiac and claimed to prevent Vata and Kapha. L. sativum seed is a good source of phenolics, amino acids, and used as a novel source of hydrocolloids. Seed extracts exhibited strong shear-thinning behavior and are used a substitute for gum arabica. L. sativum seed oil has a balanced amount of poly- and mono-unsaturated fatty acids. L. sativum seed oil contains natural antioxidants including tocols, sterols, carotenoids, and eugenol that help in the protection of oil rancidity. Clinical trials were carried out on the experimental animals to support the efficacy of L. sativum seeds. Seed extracts have been screened for various biological traits like hypotensive, antimicrobial, bronchodilator, hypoglycemic, and allelopathic, whereas its seed coat mucilage has been isolated to make it excipient of desired functionality as a part of pharmaceuticals. Through this article, the readers will get valuable information about L. sativum chemical composition, functional properties, pharmacological profile, and health-promoting applications. © 2020 Elsevier Inc. All rights reserved.