The tropical plant species of family Piperaceae had been consumed from ancient time and has reputed place in the Indian Ayurvedic system as a medicine and as a spice in foods. Piper species are also an important part in folklore medicine of Latin America and West Indies. Piper attenuatum Buch.-Ham. ex Miq., an important Piper species, mainly found in the southern tropical and sub-tropical regions of India and is much used in the Ayurvedic system of medicine. However, there is insufficient research about the mechanisms behind the medicinal action of P. attenuatum but diverse pharmacological activities like antibacterial, anti-inflammatory, anti-hyperglycaemic and antioxidant are reported from various extracts of this plant. It contains various important phytochemicals like crotepoxide, piperine, guineensine and piperlonguminine which are responsible for its therapeutic efficacy. Crotepoxide is reported to exhibit significant antitumor activity. The seed extract is reported to have antioxidant activity. Piperine is reported to increase the bioavailability of other drugs by interacting with various enzymes responsible for metabolism. The current article provides an updated literature review on recent advancement on pharmacognosy, chemistry and pharmacological activities of P. attenuatum.