Corrosion of metals and alloys is a critical challenge across various industries, leading to substantial financial losses and safety risks. The use of corrosion inhibitors has proven to be an effective strategy in mitigating this issue. This review provides a comprehensive overview of the latest advancements in the use of macrocyclic compounds and pharmacological drugs as corrosion inhibitors. These compounds exhibit unique chemical structures and functional groups, which enhance their ability to improve corrosion resistance through adsorption onto metal surfaces, thereby reducing oxidation and electrochemical reactions. The review highlights the effectiveness of these inhibitors in diverse corrosive environments and their compatibility with different metals and alloys, including steel, aluminum, and copper. Key findings reveal their superior performance in creating protective barriers and their potential for offering more sustainable, eco‐friendly solutions compared to conventional inhibitors. This review emphasizes their inhibitory effects, investigates their underlying mechanisms, and underscores the importance of ongoing research and innovation to maximize their use as effective and sustainable corrosion prevention techniques.