Nature is the best combinatorial chemist and possibly has answers to all diseases of humankind. Till now, natural product compounds discovered from medicinal plants have provided numerous clinically useful drugs. Plant based therapeutics play an important role in the public health care system of any nation. Natural products with medicinal value are gradually gaining importance in clinical research due to their well-known property of no side effects as compared to drugs. In recent years, the growing demand for herbal product has led to a quantum jump in volume of plant metabolite previously with unknown pharmacological activities have been extensively investigated as a source of medicinal agents. Thevetia peruviana Pers.commonly named as “Kaneir or Kaner” is known for its immense application in the treatment of various diseases in the traditional Ayurvedic literature. Plant based therapeutics play an important role in the public health care system of any nation. The plant Thevetia peruviana belongs to the family Apocynaceae. The plants have a significant place in traditional system of medicine of Central and South America and tropical Asia. A number of different classes of secondary metabolites are present in Thevetia peruviana including alkaloids, flavonoids, steroids, cardiac glycosides, terpenoids, tannins, saponins etc. Several researchers had identified various pharmacological activities in different parts of the plant viz. seeds, flowers, bark, fruits, leaves. This review covers detailed ethno pharmacology, toxicology and bioactivities of Thevetia peruvian.