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Abstract Functional subcellular organelle mitochondria are emerging as a crucial player and driver of cancer. For maintaining the sites of cellular respiration, mitochondria experience production, and accumulation of reactive oxygen species (ROS) underlying oxidative damage in electron transport chain carriers. Precision medicine targeting mitochondria can change nutrient availability and redox homeostasis in cancer cells, which might represent a promising strategy for suppressing tumor growth. Herein, this review highlights how the modification capable of manipulating nanomaterials for ROS generation strategies can influence or compensate the state of mitochondrial redox homeostasis. We propose foresight to guide research and innovation with an overview of seminal work and discuss future challenges and our perspective on the commercialization of novel mitochondria‐targeting agents.