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Cancer is one of the leading causes of death worldwide, yet considerable efforts are still required to make this pathology curable. Despite the limits of available approaches, kinase inhibitors have marked a turning point in the treatment of different types of tumors. This class of compounds is the first oral targeted therapy approved for neoplasia, and about 30 compounds have entered the market in the last five years. Kinase inhibitors include small molecules and monoclonal antibodies and are endowed with fewer side effects than classical antitumor agents. The potential for application of this class of drugs is substantial, and this Special Issue focuses on the discovery and development of kinase inhibitors in terms of in silico studies, synthesis and identification of new compounds, drug delivery, formulation studies, and biological and pharmacokinetic evaluation.