Platycodin D, a triterpenoid saponin, is one the major active components of the roots of Platycodon grandiflorum and possesses multiple biological and pharmacological properties including, anti-nociceptive, anti-atherosclerosis, antiviral, anti-inflammatory, anti-obesity, immunoregulatory, hepatoprotective and anti-tumor activities. Platycodin D has been shown to exert anti-tumor activity in various cancer cells without affecting normal cells in various in vitro and in vivo models. Platycodin D has been extensively investigated and found to exhibit significant anti-cancer activity against a wide range of human cancers types both in vitro and in vivo through multiple mechanisms which are considered to be crucial and central to cancer development and metastasis. Apart from in vitro anti-cancer activity of Platycodin D, various tumor models and drug administration routes have been tested for Platycodin D in vivo. Both intraperitoneal, as well as oral administration of Platycodin D, has been shown to exhibit significant anti-tumor activity. Intraperitoneal administration of Platycodin D at a dose of 5 mg/kg bodyweight significantly reduced the volume and size of MDA-MB-231 xenograft tumor.