Ruthenium complex is an important compound group for antitumor drug research and development. NAMI-A, KP1019, TLD1433 and other ruthenium complexes have entered clinical research. In recent years, the research on ruthenium antitumor drugs has not been limited to single chemotherapy drugs; other applications of ruthenium complexes have emerged such as in combination therapy. During the development of ruthenium complexes, drug delivery forms of ruthenium antitumor drugs have also evolved from single-molecule drugs to nanodrug delivery systems. The review summarizes the following aspects: (1) ruthenium complexes from monotherapy to combination therapy, including the development of single-molecule compounds, carrier nanomedicine, and self-assembly of carrier-free nanomedicine; (2) ruthenium complexes in the process of ADME in terms of absorption, distribution, metabolism and excretion; (3) the applications of ruthenium complexes in combination therapy, including photodynamic therapy (PDT), photothermal therapy (PTT), photoactivated chemotherapy (PACT), immunotherapy, and their combined application; (4) the future prospects of ruthenium-based antitumor drugs.