Natural products have been used as medicine since ancient times. With the advancement of research methods nowadays, the pharmacological properties of herbal plants have become an important role in the development and designation of drugs for different diseases. Calophyllum inophyllum is a large tree which grows well in different parts of the world. Various parts of Calophyllum inophyllum have been investigated for the pharmacological actions and some of the active constituents have been identified and isolated successfully. Furthermore, certain molecular mechanisms underlying the pharmacological effects have been revealed by different research groups across the world in recent years. This paper aims to review the different pharmacological actions of Calophyllum inophyllum together with recently discovered active constituents and mechanistic details. The published information on the pharmacological properties of Calophyllum inophyllum was gathered by using different database platforms including Google Scholar, PubMed, ScienceDirect, Scopus and SciFinder. The results show different pharmacological actions including anti-inflammatory, anticancer, antioxidant, wound healing, osteogenic, antimicrobial, lipid-lowering and antidiabetic effects of different parts of Calophyllum inophyllum. This review will provide the researchers with the background of the therapeutic potential of Calophyllum inophyllum and the extent of discovery that will lead to develop therapeutic agents for different pathological states in future.