Considering the limited number of drugs with activity in malignant gliomas, this disease appears as a niche for novel anticancer agents. Receptor tyrosine kinases and downstream RAS/RAF/MAPK and PI3K/AKT/mTOR signaling pathways are frequently activated for proliferation and invasion in malignant gliomas. A number of small molecules and monoclonal antibodies are currently investigated as potential targeted therapy for the treatment of malignant gliomas. Based on demonstrated activity of those agents in other malignancies, it is likely that some of them may also demonstrate activity in malignant gliomas. In this issue, Omuro et al. will review current advances and future avenues for the treatment of malignant gliomas using targeted therapies. For details, see Omuro et al. in this issue.