Ginseng is a natural product best known for its curative properties in diverse physiological processes such as cancer, neurodegenerative disorders, hypertension, and maintenance of hemostasis in the immune system. In previous decades, there have been some promising studies into the pharmacology and chemistry of ginseng components and the relationship between their structure and function. The emerging use of modified ginseng and development of new compounds from ginseng for clinical studies have been topics of study for many researchers. The present review deals with the anticancer, anti-inflammatory, antioxidant, and chemopreventive effects, and recent advances in microRNA technology related to red ginseng. The review also summarizes the current knowledge on the effect of ginsenosides in the treatment of cancer.