Psidium guajava Linn is an herbal remedy used in Ayurveda as a traditional system of medicine in ethnomedicine. It is a tropical evergreen plant that grows in tropical and subtropical climates. It has a wide variety of nutritional components. The whole plant and various parts of the plants possess different types of therapeutic activity, such as Tannin, phenols, triterpenes, flavonoids, essential oils, saponins, carotenoids, lectins and vitamins, dietary fiber, fatty acids, and other active components of guava plants demonstrate pharmacological activity. The fruits and leaves can be freely consumed for their good taste and various nutritional benefits and can be used in various treatments. The most active constituents, like tannins, flavonoids, terpenoids, etc., are mainly found in leaf parts. Guava has a high nutritional value, as it is high in dietary fiber, vitamins C and A, folic acid, dietary minerals, potassium, copper, and manganese. Guava leaves have phenolic compounds which are reported to possess antibacterial, antistress, antigenotoxic, antiinflammatory, anti-hyperglycemia, anti-rotavirus, cytotoxic, hepatoprotective, etc. In this review, compile all the knowledge of pharmacogenetic and pharmacological studies to present guava as an herbal drug. Many pharmacological activities have been demonstrated, such as antioxidant, antidiabetic, antihypertensive, laxative, antiallergic, cardiotonic, etc.