The current treatment for cancer depends on various factors such as the stage of cancer, size of the tumor, receptors expressed on the ECM, etc. Whether the case, the medications used for adjuvant treatment can be divided into three main groups, i.e., hormone-blocking agents, chemotherapy and monoclonal antibodies. With an increased understanding of cancer hallmarks, drug repurposing has gradually positioned itself as a promising strategy for cancer treatment by finding new effects of drugs for which human safety and pharmacokinetics are already well established. Drug repurposing for cancer therapeutics is an emerging topic of research. There are many consequences to developing new drugs for cancer therapy and overcoming this drug repurposing approach has several advantages. A crucial phase of drug research is the safety and effectiveness testing are done in human volunteers in clinical trials that normally comprise four phases, which can take many years and count exorbitant amounts of resources. Thus, the repurposing strategy represents two major advantages. In the first place, prior knowledge of the drug behaviour and characteristics. Secondly, in contrast with the very expensive novel compounds, most of the candidates for repurposing anti-cancer medications are at very low prices. Therefore, drug repurposing incorporates an approach for reducing its morbidity and lethality as well as making the treatment more accessible for everyone. Here, in this book chapter, we provide an overview of the current status of repurposed drugs and compounds that have demonstrated the potential to be used in cancer therapeutics. We will also discuss the barriers that need to be overcome to realize the benefit of this approach.