Peperomia pellucida (L.) Kunth (Family Piperaceae) has been utilizing in folk medicine for many years worldwide and much research have been devoted. This review focused to summarize updated most interesting findings on the morphological, phytochemical, ethnopharmacological and toxicological aspects obtained in the research related to the plant. Local communities around the world have been consumed this plant as a leafy vegetable and in the treatment of gastrointestinal disorders including dysentery, diarrhoea, stomachache; respiratory tract disorders including asthma, nasopharyngeal infections, cough; skin diseases including eczema, wounds, abscess, acne, boils, scabies, dermatitis, rash, sores, scar, and warts, mucosae tumors and other ailments such as fever, paralysis, epilepsy, convulsions, heart problems, hypertension, kidney disorders, gout, rheumatic pain, conjunctivitis, and measles. This species has been extensively investigated as a source of natural pharmacologically active compounds with potential antimicrobial, anticancer, antipyretic, anti-inflammatory, antioxidant, analgesic, antidiarrhoeal, antihypertensive and anti-oedematogenic activities. Phytochemical screenings on the plant have revealed the presence of various pharmacologically active principles of medical importance including tannins, flavonoids (acacetin, apigenin, isovitexin, and pellucidatin), cardiac and xanthone (Patuloside A) glycosides, alkaloids (secolignans, tetrahydrofuranlignans, peperomins A, B, C, and E, sesamin, and isoswertisin), saponins, inulins, terpenes, phenolic compounds, phytosterols (stigmasterol, sitosterol, and campesterol) and other steroids, and resins. P. pellucida also contains several essential oils, mainly dillapiole, β-caryophyllene, and carotol. The acute toxicity results revealed that this plant might be considered as a non-toxic plant with high therapeutic index. Much additional work is needed to open new biomedical application of these compounds.