Abstract: Theaflavins (TFs) are benzopropenoids containing multiple phenolic hydroxyl groups with broad-spectrum pharmacological activities, which can control and regulate the expression of tumour-initiating enzymes or related factors or promote apoptosis, inhibit tumour cell proliferation and metastasis, thus efficiently participating in both pre-cancer prevention and post-cancer treatment. This review summarizes the available in vitro and in vivo evidence, using various tumour cell lines and animal models, to demonstrate that theophyllin inhibits tumour cell proliferation, growth and metastasis mainly by inducing cell cycle arrest and apoptosis, and identifies the targets of action of theophyllin in some tumours, with far-reaching implications for the prevention and treatment of some tumours.