Maintaining and improving the nutritional quality of foods during processing are the main market and industry concerns. Thus, research should focus on novel and sustainable ways for selecting the appropriate processing method that either increases or does not affect the nutrient content of foods. Thermal processing techniques such as extrusion cooking are widely used for producing breakfast cereals, snack foods, pasta, pet food, etc. Extrusion cooking is a continuous process that uses a combination of high-temperature, highpressure, and high shear conditions in a short period of time, which results in molecular transformation and chemical reactions within the extruded products. Extrusion cooking brings on many biochemical changes such as denaturation of proteins, gelatinization of starch, lipid modifications, inactivation of microorganisms and enzymes, formation of volatile flavor components, and increase in soluble dietary fiber. Furthermore, extrusion cooking has the potential to improve the nutritional quality of the products by improving starch and protein digestibility and increasing the retention of bioactive compounds with antioxidant properties. Also, this highly efficient technology minimizes water pollution and energy consumption. This review aims to discuss the current information regarding changes in nutritional properties and bioactive compounds in cereals processed by extrusion cooking.