The present study reviewed preclinical informations of antitumor activity of interferon and discussed on its possible mechanism. In the literature we found not much information of in vivo antitumor potency of interferon. This urged us to analyze and evaluate in vitro biological activities of interferon in association with possible in vivo antitumor activity. A number of in vitro studies showed immunomodulating potency of interferon. However, we did not find sound basis for claiming any of them involved in in vivo antitumor effect of interferon. Instead, direct interaction of interferon with tumor cells was considered more likely involved in interferon-induced in vivo antitumor effect by suppressing tumor cell proliferation.