Abstract: Anticancer detoxification therapy is a fundamental principle for the treatment of malignant tumors under the guidance of the theory of cancer toxin pathogenesis. Based on historical medical texts, this article traces its historical origins and theoretical progression along two main lines: the formation of the theory of “toxic evil” and the evolution of the “detoxification” therapy. The pre-Qin to Tang-Song periods were the formative period of the toxic evil theory and the detoxification therapy; the Jin-Yuan period was the nascent period of anticancer detoxification therapy; and the Ming-Qing period was the formation period of anticancer detoxification therapy. The paper further notes that in modern times, under the guidance of the “cancer toxin” theory of the TCM Master Zhou Zhongying and the cancer toxin pathogenesis theory of Professor Cheng Haibo, the anticancer detoxification therapy has gradually become systematized, promoting its application in tumor prevention and treatment, and providing historical basis and theoretical support for contemporary clinical application.