Ferrocene, a stable 18‐electron metallocene, has been readily modified to include other functionalities by reactions such as Friedel–Crafts and Mannich. While ferrocene and its derivatives have many applications, for example, as fuel additives and materials chemistry, they have been heavily researched in the past three decades for their medicinal applications; namely, tamoxifen, a well‐known breast cancer drug, has been modified with ferrocene (ferrocifen) to improve breast cancer selectivity, and chloroquine, an antimalarial drug, was modified with ferrocene to improve its activity in chloroquine‐resistant malarial strains. In these two molecules, ferrocene imparts a metal‐specific effect, enhancing the therapeutic potential of these complexes. Ferrocifen and ferroquine are currently in phase II clinical trials and preclinical evaluation, respectively. No other ferrocene‐containing complexes have reached clinical trial stages. One strategy that could fast‐track these complexes to an advanced stage is to develop heterometallic complexes, as they often exhibit enhanced pharmacological properties and have different biological targets compared to their homometallic/mononuclear counterparts. In this article, we have highlighted the area of heterometallic ferrocenyl complexes and their applications in the treatment of cancer and look at the most promising complexes to date.