During the last few decades, the discovery of novel targets for therapeutic intervention led to the development of chemotherapeutic agents that specifically interfere with altered cellular functions of tumour cells. Genetic alterations in glioblastoma affect cell proliferation and cell cycle control, as well as invasive and metastatic growth. Therefore, innovative therapeutic strategies have been based on drugs targeting cellular proliferation, invasion, angiogenesis, metastasis and differentiation of tumour cells. Furthermore, disruption of cell-death pathways also contributes to the pathogenesis of glioblastoma and may result in resistance to chemotherapy and radiation. Therefore, additional treatment strategies that target intracellular survival and/or apoptotic pathways are under current laboratory investigation. The progress in the understanding of glioblastoma tumour biology and the refined diagnosis of individual patients together with the exploration of targeted drugs may allow a risk-adapted, individualised therapeutic strategy and will hopefully improve prognosis of glioblastoma patients in the future.