The medicinal benefits of P. lanceolata L. have been acknowledged worldwide for hundreds of years. The plant is now distributed worldwide, especially in temperate zones. This review gives an overview of ethnomedicinal use, phytochemistry, pharmacological activities, and other potential application of P. lanceolate L. Several effective chemical constituents such as polyphenols, tannins, flavonoids, alkaloids, terpenoids, iridoid glycosides, fatty acids, and polysaccharides are found in P. lanceolata L., which contribute to its exerting specific therapeutic effects. Correspondingly, studies have found that P. lanceolata L. has different biological activities, including antioxidant, antibacterial, wound-healing, anti-inflammatory, cytotoxic, and antiulcerogenic activity. The plant also treats various diseases related to the skin, respiratory organs, digestive organs, reproduction, circulation, cancer, pain relief, and infections. The plant has many applications in cosmetics such as lotion and creams; it is also used as an excellent indicator to know the presence and absence of heavy metals and the accumulation in industrial and urban areas. The plant suppresses soil nitrogen mineralization in agriculture due to allelochemicals such as aucubin. The biological activities, medicinal properties, and industrial application of P. lanceolata mainly depend on the activities of the responsible, active chemical constituents. However, this field still needs more study to determine the exact mechanisms and the main bioactive compound activity accountable for these activities. Also, most of the studies have been performed in vitro, so further in vivo studies are recommended for the future.