Cancer incidence rate has been increasing drastically in recent years. One of the many cancer treatment methods is chemotherapy. Traditional medicine, in the form of complementary and alternative therapy, is actively used to treat cancer, and many herbs and active ingredients of such therapies are being intensely studied to integrate them into modern medicine. Ginseng is traditionally used as a nourishing tonic and for treating various diseases in Asian countries. The therapeutic potential of ginseng in modern medicine has been studied extensively; the main bioactive component of ginseng is ginsenosides, which have gathered attention, particularly for their prospects in the treatment of fatal diseases such as cancer. Ginsenosides displayed their anticancer and antimetastatic properties not only via restricting cancer cell proliferation, viability, invasion, and migration but also by promoting apoptosis, cell cycle arrest, and autophagy in several cancers, such as breast, brain, liver, gastric, and lung cancer. Additionally, ginsenosides can work synergistically with already existing cancer therapies. Thus, ginsenosides may be used alone or in combination with other pharmaceutical agents in new therapeutic strategies for cancer. To date however, there is little systematic summary available for the anticancer effects and therapeutic potential of ginsenosides. Therefore, we have reviewed and discussed all available literature in order to facilitate further research of ginsenosides in this manuscript.