The article discusses the emerging role of mitochondrial metabolism in cancer therapy. Mitochondria are crucial for ATP production, biosynthesis of macromolecules, and signaling pathways. Historical views of mitochondrial dysfunction in cancer cells have been challenged by recent evidence showing that mitochondrial metabolism is essential for tumor growth. The article highlights three main areas where targeting mitochondrial metabolism can be effective: bioenergetics, biosynthetic function, and redox capacity. Metformin, a widely used antidiabetic drug, has shown promise in preclinical studies by inhibiting mitochondrial complex I and reducing tumor growth. Other compounds, such as phenformin and VLX600, also target mitochondrial bioenergetics. Targeting mitochondrial biosynthetic functions, such as glutamine catabolism and autophagy, can further impede tumor growth. Additionally, inhibiting mitochondrial redox capacity, particularly ROS generation, can be a therapeutic strategy. The article concludes by discussing the challenges and potential of targeting mitochondrial metabolism in cancer therapy.The article discusses the emerging role of mitochondrial metabolism in cancer therapy. Mitochondria are crucial for ATP production, biosynthesis of macromolecules, and signaling pathways. Historical views of mitochondrial dysfunction in cancer cells have been challenged by recent evidence showing that mitochondrial metabolism is essential for tumor growth. The article highlights three main areas where targeting mitochondrial metabolism can be effective: bioenergetics, biosynthetic function, and redox capacity. Metformin, a widely used antidiabetic drug, has shown promise in preclinical studies by inhibiting mitochondrial complex I and reducing tumor growth. Other compounds, such as phenformin and VLX600, also target mitochondrial bioenergetics. Targeting mitochondrial biosynthetic functions, such as glutamine catabolism and autophagy, can further impede tumor growth. Additionally, inhibiting mitochondrial redox capacity, particularly ROS generation, can be a therapeutic strategy. The article concludes by discussing the challenges and potential of targeting mitochondrial metabolism in cancer therapy.