Cereals are the essential staple food in the world. They are also a cheap source of vital and energy providing macronutrients such as carbohydrates, proteins, vitamins, dietary fiber, minerals, and phytochemicals. Despite being so nutritious, a number of nutrients are not able to be utilized by the body due to the presence of some nutritional hurdles, which are known as antinutrients or antinutritional factors (ANFs). The ANFs are secondary metabolites, having specific biological effects depending upon the structure of specific compounds, which range from high molecular weight proteins to simple amino acids and oligosaccharides such as phytic acid, polyphenols, oxalates, saponins, etc. These antinutrients reduce the bioavailability of nutrients and affect the normal growth, reproduction, and health of the human body. Several methods are used to reduce the presence and effects of ANFs. This chapter discusses the ANFs present in cereals, their effects on health, and overcoming strategies.