Abstract: Glioblastoma multiforme (GBM) is a common primary malignant brain tumor of the adult central nervous system. Due to the poor prognosis, the median survival time of patients is less than one year, due mainly to the resistance of the main therapeutic drug temozolomide (TMZ)for GBM treatment failure. Anti-GBM drugs include those already approved by the U.S. FDA, candidate drugs under clinical trials and active compounds in preclinical research. Currently, four drugs have been approved for the market by FDA. The first-line drug used is mainly TMZ, while the others are rarely used due to their toxic and side effects or poor efficacy. This paper introduces the pharmacological action, mechanism of action, clinical trials and adverse reactions of anti-GBM drugs.