Gymnema sylvestre is one of the valuable medicinally important herbs that belong to family Apocynaceae. G. Sylvester is a woody climber mostly found in India, Srilanka, China, Indonesia, Malaysia and Tropical Africa. Traditionally the leaf of the herb is used as antidiabetic, antihelmentic, antiobesity, anti-inflammatory, hypolipidaemic, antivenom and antimicrobial. The herb is used by some ethnic community in constipation, haemorrhoids, jaundice, leucoderma, asthma, bronchitis, cardiac problems and dyspepsia. Most important phytochemicals of the plant are gymnemic acid, deacyl gymnemic acid and gymnemagenol which help in the controlling of blood cholesterol, triglyceride levels, inflammation and body weight. The present review aims to document the traditional and modern pharmacological uses of the plant to provide better scope for further experiments and future application. The botanical description, cultivation practices, phytochemical constituents and safety issues of the plant has also been described in the chapter.