Dhurrin, a cyanogenic glucoside, is a plant defensive chemical synthesized from aliphatic amino acids and consists of β-d-glucopyranose linked to α-hydroxy nitrile. It is catabolized by the consecutive action of hydroxynitrilase and β-glucosidase to release hydrogen cyanide on tissue disruption during herbivory. These phytoanticipins are widely distributed across various monocot and dicot plants such as Sorghum, Macadamia, Ostrya sp., and many other plant species with ornamental, pharmaceutical, medicinal, and food value. Although repellent properties of dhurrin against herbivores are often reported, less is known about its distribution, metabolism, mode of action against insects, and application for pest control. Herein, we highlight recent updates on dhurrin distribution, biosynthesis, and catabolism along with the cyanide detoxification pathway. Additionally, this article focuses on biological activities of dhurrin against various herbivores and opportunities to explore the utilization of dhurrin as a natural pest control agent and a substitute for chemically synthesized pesticides.