Psidium guajava (L.) belongs to the Myrtaceae family and it is an important fruit in tropical areas like India, Indonesia, Pakistan, Bangladesh, and South America. The leaves of the guava plant have been studied for their health benefits which are attributed to their plethora of phytochemicals, such as quercetin, avicularin, apigenin, guaijaverin, kaempferol, hyperin, myricetin, gallic acid, catechin, epicatechin, chlorogenic acid, epigallocatechin gallate, and caffeic acid. Extracts from guava leaves (GLs) have been studied for their biological activities, including anticancer, antidiabetic, antioxidant, antidiarrheal, antimicrobial, lipid-lowering, and hepatoprotection activities. In the present review, we comprehensively present the nutritional profile and phytochemical profile of GLs. Further, various bioactivities of the GL extracts are also discussed critically. Considering the phytochemical profile and beneficial effects of GLs, they can potentially be used as an ingredient in the development of functional foods and pharmaceuticals. More detailed clinical trials need to be conducted to establish the efficacy of the GL extracts.