Evodiamine is the natural component extracted Euodiae Fructus. Recently, growing evidence has proved that evodiamine has great effects on suppressing cell viability and proliferation, arresting cell cycle, inducing apoptosis, promoting autophagy, inhibiting the formation of microvascular angiogenesis as well as affecting epigenetic modification in cancer. Recent studies have continuously revealed related signal pathways involved in evodiamine such as PI3K-Akt and JAK-STAT pathways, as well as the impact of evodiamine on survivin, vascular endothelial growth factor and miRNAs. With the development and synthesis of evodiamine derivatives and related herbal formulations, the understanding of antitumor activity of evodiamine is gradually deepening. The important clinical significance and market value of evodiamine can be prospected.