The introduction of multifunctionalities for tumour targeting is becoming a popular strategy toward the development of new therapeutic agents. In particular, the multifaceted potential of ruthenium(II)-arene complexes show great promise as chemotherapeutics. An ever-increasing number of papers dealing with the integration of ruthenium complexes with biologically active molecules to derive bioorganometallic molecules of chemotherapeutic significance have been published in recent years. This perspective review presents a short overview of multifunctional ruthenium-based drugs, especially those containing arene ruthenium complexes, with the emphasis on the combination of photosensitizers with ruthenium complexes for the preparation of novel multifunctional photodynamic therapy agents.