Recent years have witnessed an explosion of promising therapies for cancer patients. New insights into the biology of malignancies have led to the development of targeted agents with the potential to improve survival and quality of life. One of the most important classes of these compounds are tyrosine kinase inhibitors. These agents are beginning to offer a clinically relevant benefit to patients with tumors that until recently have been refractory to medical therapies. High-grade gliomas represent one class of medically refractory solid tumors. This article summarizes the state of the art of tyrosine kinase inhibitors in the management of patients with high-grade gliomas.