The treatment for malignant tumors in the central nervous system (CNS) mainly consists of surgical resection followed by adjuvant radiation and chemotherapy. Temozolomde (TMZ), a second-generation of oral alkylating agent, plays an increasingly important role in the treatment of malignant glioma in China. However, the history of TMZ use in China, has not been well reviewed. In this study, an extensive literature search of Pubmed and major Chinese electronic databases was performed to identify clinical reports on TMZ use in mainland China. We found that TMZ is a standard addition to postoperative RT for glioblastoma, followed by 6 cycles of adjuvant treatments as Chinese and NCCN guidelines recommended. But since TMZ is relatively expensive to most Chinese patients, especially in undeveloped areas, some other regimens are still commonly used. It is also indicated for relapsed or Grade III glioma, with some potential value in brain metastasis and primary central nerve lymphoma. Extended use or combination therapy including TMZ may benefit more for glioma patients. As the clinical trials have been paid more attention in the recent years, effort and collaboration should be made to conduct well-designed multicenter randomized clinical trials on TMZ, with the aim of improving the prognosis of patients with CNS tumor in mainland China.