The use of bismuth and its compounds in biomedicine has developed rapidly in recent years. Due to their unique properties, there are great opportunities for the development of new non-invasive strategies for the early diagnosis and effective treatment of cancers. This perspective highlights key fabrication methods to generate well-defined and clinically relevant bismuth materials of varying characteristics. On the one hand, this opens up a wide range of possibilities for unimodal and multimodal imaging. On the other hand, effective treatment strategies, which are increasingly based on combinatorial therapies, are given a great deal of attention. One of the biggest challenges remains the selective tumour targeting, whether active or passive. Here we present an overview on new developments of bismuth based materials moving forward from a simple enrichment at the tumour site via uptake by the mononuclear phagocytic system (MPS) to a more active tumour specific targeting via covalent modification with tumour-seeking molecules based on either small or antibody-derived molecules.