Genus Alstonia is comprised of around 155 species throughout the world. Phytochemical screening of Alstonia genus has demonstrated the presence of diverse phytochemicals that include at least 800 distinct metabolites. The main classes of metabolites are alkaloids, iridoids, flavonoids, fatty acids, etc. Secondary metabolites from this genus also bring positive results when employed as anticancer, anti-spasmodic, antitussive, antiarthritic, antioxidant, etc. Alstonia boonei is listed as an antimalarial drug in African pharmacopoeia. In China, a formulation consists of A. scholaris leaves-Dengtaiye tablets are used for the treatment of cough and fever symptoms. Recently, A. scholaris leaves-derived indole alkaloids have been registered as an investigational new botanical drug (No. 2011L01436) and China Food and Drug Administration (CFDA) has approved its phase I/II clinical trials for the treatment of respiratory diseases. Pharmacokinetic and safety analysis of this botanical drug in healthy human subjects have revealed a safe profile under the dose regimen experiment. Apart from that, strictamine, an indole alkaloid isolated from A. scholaris exhibited a similar in vitro antiviral activity to that of acyclovir. The present chapter is mainly focused on the critical analysis of various secondary metabolites isolated from Alstonia (approximately 15 species). Apart from that, pharmacological, toxicological and intellectual property rights studies have also been included.