The evaluation of two hundred and forty-three traditional Chinese drugs from one hundred traditional Chinese medicine prescriptions used clinically for the treatment of human cancer, demonstrated that the real action mechanisms are still uncertain, though the inhibition of cancer pathogen and/or stimulation of immune systems have been suggested. In this review article, both the tradition and modern pharmacological view-points of each drug were considered to categorize these prescriptions, and hope it would provide hints for further academic study and reasonable clinical application.