Neem, the versatile medicinal plant is the unique source of various types of compounds having diverse chemical structure.The biological activity and plausible medicinal applications of these compounds need an extensive investigation to exploit their therapeutic utility to combat diseases.Crude extracts from various parts of neem have medicinal applications from time immemorial, modern drugs can be developed after extensive investigation of its bioactivity, mechanism of action, pharmacotherapeutics, toxicity and after proper standardization and clinical trials. As the global scenario is now changing towards the use of nontoxic plant products having traditional medicinal use, development of modern drugs from neem should be emphasized for the control of various diseases. In fact, time has come to make good use of centuries-old knowledge on neem through modern approaches of drug development.