Receptor tyrosine kinases (RTKs) control the basic activities of cells including proliferation, cell cycle, apoptosis, metabolism and so on. Accordingly, abnormal activation caused by mutations of RTKs plays an important part in the formation and development of tumor. For the past few years, the receptor tyrosine kinase inhibitors (rTKI) developed for RTKs have progressed rapidly and achieved good results in clinical treatment in various tumor types, such as chronic myelogenous leukemia, non-small cell lung cancer, breast cancer and so on. As for acute myeloid leukemia (AML), approval and clinical application of inhibitors against Fms-like tyrosine kinase 3 (FLT3) significantly improve prognosis in patients with FLT3 mutations, which is vital for the treatment of AML. The clinical application of rTKI to AML is summarized in this review, providing a reference for the treatment of AML.