This book reviews the potential of metallodrugs against different cancer. It summarizes the classification of metal-based anti-cancer drugs, their plausible biochemical and mechanistic pathways, combining drug strategies for hitting multiple therapeutic targets at the intracellular level, and advanced drug delivery strategies. The book covers the metallodrugs for the efficacious treatment of diverse cancerous strains and recent advances in drug delivery strategies that are used for developing these metal-based therapeutics as potent anticancer agents in vitro and in vivo. The book also covers different biophysical and analytical techniques for studying metal-ligand and metal-macromolecular interactions. The book further presents the recent examples of metallomics studies on the different types of cell death induced by metal-based anticancer drugs, especially on the three major forms of programmed cell death (PCD) in mammalian cells: apoptosis, autophagy, and regulated necrosis, also called necroptosis. Lastly, the book explores the modulation of reactive oxygen species (ROS) by metallodrugs.