Citrus macroptera (family Rutaceae), commonly known as Sat Kara, is a pharmacologically diverse medicinal plant. Various parts of this plant, specifically fruit, have an immense range of medicinal uses in folk medicine directed for a number of ailments. A plethora of active phytochemical constituents of this plant have been revealed so far, namely, limonene, beta-caryophyllene, beta-pinene, geranial edulinine, ribalinine, isoplatydesmine, and so forth. Several studies demonstrated the exploration of pharmacological potential of various parts such as fruits, leaves, and stems of C. macroptera as antioxidant, cytotoxic, antimicrobial, thrombolytic, hypoglycemic, anxiolytic, antidepressant, cardioprotective, and hepatoprotective. Furthermore, inhibition of in vitro α-amylase, inhibition of paracetamol induced hepatotoxicity, and potentiation of brain antioxidant enzyme are also ascertained. In present review, comprehensive study focused on knowledge regarding several phytopharmacological activities of Citrus macroptera has been described.