Psidium guajava (guava) is widely distributed in tropical and subtropical regions and adapted to various environmental conditions. Guava is an important economic fruit widely used as food and folk medicine. It contains flavonoids, alkaloids, tannins, triterpenoids, reducing sugars, essential oils, carotenoids, polyphenols, etc. The presence of triterpenoid acids such as guavacoumaric, ursolic, jacoumaric, guajavanoic, guavenoic, and Asiatic acids helps to develop novel drugs against various diseases. It is used traditionally for medicinal purposes, mainly for antioxidant, antimicrobial, antispasmodic, antidiabetic, anticancer, antiallergy, anti-inflammatory, and hepato-protective properties. The systematic literature study aims to summarize its botanical description, phytochemicals, pharmacological activities, and clinical trials. This review focuses on the plant's chemical composition and scientific approaches to human welfare. A systematic literature search was done on Psidium guajava through previous literature and online databases such as Google Scholar, Pubmed, Science Direct, etc., to explain its ethnomedicinal uses, phytochemistry, and pharmacological applications. Previous literature studies of Psidium guajava suggest it can serve as antioxidant, antimicrobial, antispasmodic, antidiabetic, anticancer, anti-allergy, anti-inflammatory, and hepatoprotective effects. Successful clinical trials performed on the plant extracts against infantile rotaviral enteritis and infectious gastroenteritis showed future directions to work with the plant for clinical applications. In this review, an attempt is made to show all literature studied, especially in phytochemistry, pharmacology, clinical trials and uses as traditional folk medicine around the world. The leaves have been used by folklore over the years to treat various ailments such as skin ulcers, diarrhoea, vaginal irritation, cough, conjunctivitis, etc. Further studies are required to explore more therapeutic remedies and to develop new medicines for future perspectives.
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