Ferrocene is a remarkable organometallic compound with an iron ion sandwiched between two cyclopentadienyl rings. This unique molecular structure and diverse characteristics such as improved solubility, altered reactivity, and enhanced biological activity make them potential candidates for drug development and diverse applications including cancer therapy. Additionally, ferrocene-based compounds exhibit a lower tendency to induce severe side effects, making them a safer option for cancer treatment. They also have shown potential in overcoming resistance encountered by platinum compounds in treating certain types of cancer. The three primary metabolic pathways for ferrocene include oxidation, cyclization catalyzed by acid, and hydroxylation, forming quinone methide, cyclic indene, and allylic alcohol, respectively. Building on this foundation, researchers have delved deeper into synthesizing and assessing novel ferrocene derivatives to enhance their effectiveness in addressing cancer and other illnesses. This review comprehensively examines potential derivative reactions, highlighting the possibilities for tailoring these compounds to achieve specific therapeutic objectives.