For many years, chemotherapy has been utilized for the treatment of malignant brain tumors with minimal success. This particularly true with chemotherapy in adult malignant gliomas for which no new drug has been approved for use since the initial studies using nitrosoureas and procarbazine in the early 1960s. However, the results of more recent clinical trials research using newer agents appear to show improved outcome in some tumor types. Better understanding of the basic biology of these diverse tumors also have given rise to new treatment strategies, especially to drug development. A large number of new antineoplastic agents are now being tested in Phase I and II trials; they are very promising and soon may lead to new drug approvals. This review will discuss the results of completed trials for newly diagnosed and recurrent glioma in adults, as well as ongoing, new drug studies with these patients. A discussion of the more common pediatric brain tumors and the use of chemotherapy in that age group is also presented. Chemotherapy is often the primary treatment modality used to control tumor growth in newly diagnosed infants and young children, and it is in this setting that chemotherapy is particularly beneficial in reducing morbidity and increasing survival. As part of a multimodality approach that includes surgery and radiotherapy, chemotherapy has a significant role to play in the treatment of both adults and children with brain neoplasms.