This review article focuses on small molecule tyrosine kinase inhibitors (TKIs) that have shown promising activity in glioblastoma multiforme (GBM) treatment. GBM is an aggressive brain cancer with a poor prognosis, characterized by high recurrence rates and treatment resistance. The authors report on compounds published in the last five years that have demonstrated efficacy in preclinical models as TKIs. These compounds are grouped based on the targeted kinase, including receptor TKIs and cytoplasmic and peculiar kinase inhibitors. The chemical structures and interactions with the target for some representative compounds are provided to elucidate their mechanism of action. The article also cites relevant clinical trials involving TKIs alone or in combination with other agents. Key targets discussed include ALK, AXL, DDR1, IGF1R, MER, c-Met, EGFR, PDGFR, VEGFR, FAK, JAK, LCK, SYK, Src, DYRK1A, and MEK. The review highlights the potential of these TKIs in improving the treatment of GBM, emphasizing the need for further research and development of new pharmacological agents.This review article focuses on small molecule tyrosine kinase inhibitors (TKIs) that have shown promising activity in glioblastoma multiforme (GBM) treatment. GBM is an aggressive brain cancer with a poor prognosis, characterized by high recurrence rates and treatment resistance. The authors report on compounds published in the last five years that have demonstrated efficacy in preclinical models as TKIs. These compounds are grouped based on the targeted kinase, including receptor TKIs and cytoplasmic and peculiar kinase inhibitors. The chemical structures and interactions with the target for some representative compounds are provided to elucidate their mechanism of action. The article also cites relevant clinical trials involving TKIs alone or in combination with other agents. Key targets discussed include ALK, AXL, DDR1, IGF1R, MER, c-Met, EGFR, PDGFR, VEGFR, FAK, JAK, LCK, SYK, Src, DYRK1A, and MEK. The review highlights the potential of these TKIs in improving the treatment of GBM, emphasizing the need for further research and development of new pharmacological agents.