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Background: RNA splicing, a fundamental step in gene expression, is aimed at intron removal and ordering of exons to form the protein’s reading frame. Objective: This review is focused on the role of RNA splicing in cancer biology; the splicing abnormalities that lead to tumor progression emerge as targets for therapeutic intervention. Methods: We discuss the role of aberrant mRNA splicing in carcinogenesis and drug response. Results and Conclusion: Pharmacological modulation of RNA splicing sets the stage for treatment approaches in situations where mRNA splicing is a clinically meaningful mechanism of the disease.