Piper retrofractum Vahl. which belongs to the family Piperaceae, is a popular spice possessing high medicinal properties. The present article aims to provide a review of the studies done on phytochemistry and biological activities of P. retrofractum. This review is based on a literature study of scientific journals from electronic sources, such as Science Direct, PubMed, Google Scholar, Scopus, and Web of Science. The main chemical constituents that have been isolated and identified from P. retrofractum are amides, alkaloids, phenylpropanoids, alkyl glycosides, and lignans. This plant possesses antioxidant, hepatoprotective, cytotoxic, larvicidal, antiproliferation, antitubercular, antileishmanial, antiphotoaging, and anti- obesity properties. P. retrofractum has the potential for the treatment of several diseases and disorders, but there are only a few studies done to investigate the plant phytochemicals, thus further studies should be focused on isolation and identification of active compounds with pharmacological activities. Besides, the majority of pharmacological studies have been performed using aerial parts of the plant, however, further studies are needed to investigate bioactivity of other parts of the plant.