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Tyrosine kinase inhibitors (TKIs) have been studied extensively in cancer research, ultimately resulting in the approval of many drugs for cancer therapy. Recent evidence from reported clinical cases and experimental studies have suggested that some of these drugs have a potential role in diabetes treatment. These TKIs include imatinib, sunitinib, dasatinib, erlotinib, nilotinib, neratinib, and ibrutinib. As a result of promising findings, imatinib has been used in a phase II clinical trial. In this review, studies that used TKIs in the treatment of both types of diabetes are critically discussed. In addition, the different molecular mechanisms of action of these drugs in diabetes models are also highlighted to understand their antidiabetic mode of action.