In recent years, the application of engineering nanomaterials has significantly contributed to the development of various biomedical fields. Zinc oxide nanomaterials (ZnO NMts) have gained wide popularity due to their biocompatibility, unique physical and chemical properties, stability, and cost‐effectiveness for large‐scale production. They have emerged as potential materials for anticancer applications. This article provides a comprehensive review of the synthesis methods of ZnO NMts and highlights the advantages of combining ZnO NMts with anticancer drugs as a nano platform for cancer treatment. Additionally, the article briefly explains the mechanism of action of ZnO NMts in tumor cells, focusing on the mitochondrial pathways that target cell apoptosis and autophagy. It is observed that these pathways are primarily influenced by reactive oxygen species generated through oxidative stress. The article discusses the promising prospects of ZnO NMts combined with anticancer drugs in the field of cancer medicine and emphasizes the need for further in‐depth research on the mitochondrial apoptosis and mitochondrial autophagy pathways.