The Warburg effect, characterized by the preferential conversion of glucose to lactate in cancer cells despite oxygen availability, is a key metabolic feature of tumors and a promising therapeutic target. This review summarizes current understanding of the Warburg effect in cancer, its implications, and recent pharmacological strategies targeting glycolytic enzymes. It also discusses the potential of the Warburg effect as an early diagnostic tool and the multifaceted roles of lactate in the tumor microenvironment (TME). The Warburg effect promotes tumor progression and immunosuppression through various mechanisms, including lactate production, acidic pH, and its impact on immune cells. Lactate influences macrophage polarization, T-cell function, and dendritic cell differentiation, contributing to immunosuppression. Therapeutic strategies targeting the Warburg effect include inhibitors of glucose transporters, hexokinase, glycolytic enzymes, and lactate dehydrogenase. While these approaches show promise, challenges remain in achieving therapeutic efficacy and minimizing side effects. The Warburg effect also plays a role in cancer-associated cachexia, highlighting its broader impact on tumor biology. Advances in imaging techniques, such as PET and hyperpolarized 13C MRI, offer new insights into cancer metabolism and therapeutic response. Future research aims to refine therapeutic approaches by targeting the TME and enhancing immunotherapy effectiveness through modulation of lactate and metabolic interactions. Overall, the Warburg effect remains a critical area of research for developing novel cancer therapies.The Warburg effect, characterized by the preferential conversion of glucose to lactate in cancer cells despite oxygen availability, is a key metabolic feature of tumors and a promising therapeutic target. This review summarizes current understanding of the Warburg effect in cancer, its implications, and recent pharmacological strategies targeting glycolytic enzymes. It also discusses the potential of the Warburg effect as an early diagnostic tool and the multifaceted roles of lactate in the tumor microenvironment (TME). The Warburg effect promotes tumor progression and immunosuppression through various mechanisms, including lactate production, acidic pH, and its impact on immune cells. Lactate influences macrophage polarization, T-cell function, and dendritic cell differentiation, contributing to immunosuppression. Therapeutic strategies targeting the Warburg effect include inhibitors of glucose transporters, hexokinase, glycolytic enzymes, and lactate dehydrogenase. While these approaches show promise, challenges remain in achieving therapeutic efficacy and minimizing side effects. The Warburg effect also plays a role in cancer-associated cachexia, highlighting its broader impact on tumor biology. Advances in imaging techniques, such as PET and hyperpolarized 13C MRI, offer new insights into cancer metabolism and therapeutic response. Future research aims to refine therapeutic approaches by targeting the TME and enhancing immunotherapy effectiveness through modulation of lactate and metabolic interactions. Overall, the Warburg effect remains a critical area of research for developing novel cancer therapies.