This book presents an overview of cancer and the genesis, and development of different treatment strategies and modalities against cancer. The emergence of gold and its complexes as promising anticancer chemotherapeutic agents have the potential to substitute or replace the platinum based chemotherapeutic agents. Gold complexes have demonstrated considerable anti-proliferative properties, chiefly attributed to their anti-mitochondrial effects, they make gold complexes excellent candidates as anti-cancer agents compared to their platinum-based counterparts. This book provides a critical review of recent advances made in the development of gold complexes as anti-cancer agents. In this context, it examines a number of different ligand architectures, provides comprehensive information on gold complexes’ mechanism of action and toxicity issues and, in closing, outlines future research directions.