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<i>Centella asiatica</i> is a popular herb well-known for its wide range of therapeutic effects and its use as a folk medicine for many years. Its therapeutic properties have been well correlated with the presence of asiaticoside, madecassoside, asiatic and madecassic acids, the pentacyclic triterpenes. The herb has been extensively known to treat skin conditions; nevertheless, several pre-clinical and clinical studies have scientifically demonstrated its effectiveness in other disorders. Among the active constituents that have been identified in <i>Centella asiatica</i>, madecassoside has been the subject of only a relatively small number of scientific reports. Therefore, this review, while including other major constituents of this plant, focuses on the therapeutic potential, pharmacokinetics and toxicity of madecassoside.