L-amino acid oxidase (LAAO) is a protein toxin commonly found in snake venom. It has many applications, ranging from biotechnology to potential anticancer therapeutics. LAAO converts L-amino acid into α-keto acid and release ammonia and hydrogen peroxide as by-products. Induction of oxidative stress in cancer cells is one of the cancer treatment strategies as controlled and targeted release of hydrogen peroxide can theoretically induce sufficient oxidative stress to kill cancer cells. Furthermore, L-amino acid oxidase has been shown to selectively bind to cell membranes of specific phospholipid composition and deliver the hydrogen peroxide to localized regions on the cell surface. In this mini review, we discuss the relevance of L-amino acid oxidase, in terms of its structure and enzyme activity, its potential as a cytotoxic agent and exploitation of its cytotoxic nature as an anticancer therapeutic.