In the 1920’s, Otto Warburg, one of the greatest biochemists of all time, uncovered an intriguing bioenergetic phenotype shared by most tumor cells: a higher than normal reliance on lactic acid fermentation for energy generation. Warburg’s seminal finding gave rise to a new field of cancer research that came to be known as oncometabolism. Research in this fascinating field, which has since expanded its scope well beyond the metabolic processes of energy generation, has already translated into one of the most successful imaging techniques for the diagnosis and staging of tumors, 18F-deoxyglucose positron emission tomography (FDG-PET). Targeting the metabolic peculiarities of tumor cells for cancer treatment, on the other hand, has only yielded modest results. Recently, the Food and Drug Administration (FDA) granted approval to two inhibitors of mutated forms of isocitrate dehydrogenase (IDH)—IDHIFA® (enasidenib) and Tibsovo® (ivosidenib)—but only for certain forms of acute myeloid leukemia (AML). In this context, it must be stressed that drugs targeting nucleotide metabolism, which have been in the clinic for many decades, target proliferating cells in general, not tumor cells specifically. Nonetheless, it is still believed that a more detailed and comprehensive understanding of the metabolic rewiring that accompanies neoplastic transformation will ultimately translate into highly effective metabolic anticancer agents.