Metallodrugs offer potential for unique mechanism of drug action based on the choice of the metal, its oxidation state, the types and number of coordinated ligands and the coordination geometry. This review illustrates notable recent progress in the field of medicinal bioinorganic chemistry as many new approaches to the design of innovative metal-based anticancer drugs are emerging. Current research addressing the problems associated with platinum drugs has focused on other metal-based therapeutics that have different modes of action and on prodrug and targeting strategies in an effort to diminish the side-effects of cisplatin chemotherapy. Examples of metal compounds and chelating agents currently in clinical use, clinical trials or preclinical development are highlighted. This review gives an overview of the relevant medicinal chemistry of platinum, palladium, gold and ruthenium complexes, which could be used for anticancer or biomedical applications. Display omitted •Pt complexes that intercalate with DNA typically exhibit anticancer activity.•Pd complexes showed good binding affinity to DNA and proteins.•The thiol–enzymes are considered key molecular targets of anticancer Au complexes.•Ru complexes has been considered to be an attractive alternative to Pt complexes.