Saussurea costus (Falc.) Lipsch. Syn. Saussurea lappa C.B. Clarke belongs to family Asteraceae and is a critically endangered plant that is monetarily very vital as a therapeutic herb of North - West Himalaya. Saussurea costus has been traditionally used to treat a variety of ailments in different indigenous health systems viz., carminative, expectorant, antiarthritic, antiseptic, aphrodisiac, anodyne and vermifuge without any noticeable adverse effects. Textbooks on ethnobotany, peer-reviewed academic publications, unpublished materials, and research repositories were used to collect the widespread review of literature on Saussurea costus. The scientific names were authenticated by using Kew Botanical Garden, International Plant Name Index and Plant List databases. Costunolide, dihydrocostunolide, sesquiterpene lactones and cynaropicrin have been identified as major phytoconstituents of Saussurea costus with great potency to develop as a drug candidate. Different pharmacological experiments convincingly confirmed the potential of Saussurea costus with anticancer, anti-ulcer, hepatoprotective activities, etc. providing support to the various traditional uses associated with Saussurea costus. Saussurea costus will be a preferable alternative for novel drug discovery due to its notable pharmacological properties. Although the existing information to far indicates the security and possibly efficacy of Saussurea costus, bioactive ingredients, physiological mechanisms, pharmacokinetics, accessibility, and the impact on human health are not fully understood. The present review piles up the up-to-date and widespread information on botany, traditional uses, phytochemistry and pharmacology of Saussurea costus, to assess its therapeutic potential, with a focus on in vitro, biomedical, and histopathological experiments.