This review mainly summarizes results of recent studies on the anticancer activity of the multifunctional protein
lactoferrin (Lf) and its derived peptide lactoferricin (Lfcin). The basic information on Lf and Lfcin, such as their
sources, structures, and biological properties which favor their antitumor activity is introduced. The major anticancer
mechanisms of Lf and Lfcin including cell cycle arrest, apoptosis, anti-angiogenesis, antimetastasis, immune modulation
and necrosis are discussed. Other information from in vivo studies employing a mouse model is also provided. In addition,
the roles of talatoferrin and delta lactoferrin, as well as improvement in drug delivery will be covered.