Psidium guajava L. (Myrtaceae), also known as guava, is a medicinal tree native to tropical America that has been introduced and is widely available in many countries. Almost all plant parts of P. guajava have a long history of being used to treat a variety of ailments, in addition to applications as foods. Guava leaves are used as both medicine and food purposes, and there are numerous scientific reports on their medicinal uses, chemical composition and pharmacological properties. Cancer, blood pressure, diarrhea, bowel irregularities, diabetes, cough, cold, constipation, dysentery, scurvy, weight loss, improves skins tonicity are some of the diseases treated with guava leaves. Polyphenols, flavonoids, saponins, tannins, terpenoids, glycosides, flavones, cardiac glycosides, cardenolides, phlobatanins, steroids and other classes of bioactive compounds have been identified from the leaves. The primary chemical constituents of guava leaves are phenolic compounds, iso-flavonoids, gallic acid, catechin, quercetin, epicathechin, rutin, naringenin, kaempferol, caryophyllene oxide, p-selinene etc. Several studies have demonstrated its pharmacological activities including antioxidant, antimicrobial, antidiabetic, antitumor, anticancer, antidiarrheal, healing, cytotoxic, hepatoprotective, anti-inflammatory, antimalarial/ anti-plasmodial, dental plaque, antiglycative and many more. This review is aimed on compiling all the literature reported on pharmacological activities and phytochemical compositions of guava leaves as a support to the scientific community for further studies and to provide scientific data to validate its traditional uses.