Tumors reprogram their metabolic pathways to meet the bioenergetic and biosynthetic demands of cancer cells. These reprogrammed activities are now recognized as the hallmarks of cancer, which not only provide cancer cells with unrestricted proliferative and metastatic potentials, but also strengthen their resistance against stress conditions and therapeutic challenges. Although recent progress in nanomedicine has largely promoted the developments of various therapeutic modalities, such as photodynamic therapy, photothermal therapy, nanocatalytic therapy, tumor‐starving/suffocating therapy, etc., the therapeutic efficacies of nanomedicines are still not high enough to achieve satisfactory tumor‐suppressing effects. Therefore, researchers are obliged to look back to the essence of cancer cell biology, such as metabolism, for tailoring a proper therapeutic regimen. In this work, the characteristic metabolic pathways of cancer cells, such as aerobic respiration, glycolysis, autophagy, glutaminolysis, etc. are reviewed, to summarize the very recent advances in the smart design of nanomedicines that can regulate tumor metabolism for enhancing conventional therapeutic modalities. The underlying chemistry of these nanomedicines by which tumor metabolism is harnessed, is also discussed in a comprehensive manner. It is expected that by harnessing tumor metabolism cancer nanotherapeutics will be substantially improved in the future.