The exploitation of altered cancer metabolism has emerged as a promising approach for anti-cancer drug development. This systematic literature review aimed to capture the latest advancements in targeting cancer metabolism, focusing on glycolysis, glutaminolysis, and lipid metabolism. A comprehensive search of databases identified significant developments in each metabolic pathway. Inhibitors such as 3-bromopyruvate, targeting glycolysis, CB-839, modulating glutaminolysis, and orlistat and bempedoic acid, impacting lipid metabolism, have shown promising preclinical and early clinical trial results across multiple cancer types. Combination therapies, pairing these metabolic inhibitors with traditional chemotherapy or immunotherapy, have shown enhanced efficacy, revealing the potential of a multi-targeted approach to overcoming therapeutic resistance. However, challenges including non-specific cytotoxicity, development of resistance, and the need for improved biomarkers, persist. This review highlights the promise and challenges of targeting cancer metabolism, offering insights for future research towards improved anti-cancer therapies.