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Hepatocellular carcinoma is the third leading cause of cancer-related mortality in the world. Locoregional therapy is used for early stage hepatocellular carcinoma. Tyrosine kinase inhibitors have been the mainstay of treatment for advanced hepatocellular carcinoma. Sorafenib was the first drug approved based on data from two pivotal phase III trials. Although sorafenib provided a survival benefit, development of adverse events limits its use in some patients. These adverse events, such as hand–foot syndrome and diarrhea, have a significant impact on the quality of life and, in some circumstances, are severe enough to prompt cessation of the drug. In recent times, a range of new therapeutic options have come on the scene including lenvatinib, regorafenib, and cabozantinib. Lenvatinibis now approved as an alternative first-line agent for hepatocellular carcinoma. Regorafenib and cabozantinib are both second-line agents. These medications provide a promising range of treatment options for patients who progress on sorafenib or are intolerant to it. This chapter provides an insight into the range of tyrosine kinase inhibitors available for the treatment of hepatocellular carcinoma.
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