Abstract: Since ancient era, herbal therapy remained as medicine’s backbone which is economic, safer and easily available to most of people in world. Among diverse herbal treasure, Azadirachta indica (Neem) is a highly esteemed tree with several beneficial properties and applications especially known for its incredible therapeutic and ethnomedicinal values for humankind. Neem is regarded as “free tree of India”, “wonder tree”, “Nature’s drug store”, Village dispensary”, “Divine tree”, “heal all”, “Materia medica” and “Panacea of all Diseases”. It is among highly exploited medicinal plant of Indian origin. It has been used in different medicinal systems: ayurveda, unani, homoeopathic medicine, therefore, considered as cynosure of modern medicine. All parts of the plant have some biological and medicinal properties hence valuable source of natural medicinal products. Compounds isolated from neem are broadly classified into two: (1) Isoprenoids (2) Non-isoprenoids. Isoprenoid compounds consists of diterpenoids, triterpenoids and steroids while while non-isoprenoids contains proteins and/or amino acids, polysaccharides, flavonoids etc. It is found beneficial in leprosy, gastro-intestinal problems, malaria, intestinal helminthiasis, tuberculosis, ringworms, skin disorders, boils, epilepsy, fever, respiratory distress, nausea, ulcers and in many other health related problems. This review gives a bird’s eye view particularly on history, classification, active principles, mechanism of action and potential uses of neem in safeguarding human and animal health along with the several commercial preparations available in the market.