The evolution of chemotherapy, especially the dawn of metal-based drugs, represents a transformative era in cancer treatment. From the serendipitous discovery of mustard gas's cytotoxic effects to the sophisticated development of targeted therapies, chemotherapy has significantly refined. Central to this progression is the incorporation of metal-based compounds, such as platinum (Pt), ruthenium (Ru), and gold (Au), which offer unique mechanisms of action, distinguishing them from organic therapeutics. Among these, Ru complexes, exemplified by BOLD-100 and TLD1433, have shown exceptional promise due to their selective activity, lower propensity for resistance, and the ability to target spescific cellular pathways. This paper explores the journey of such Ru candidates, focusing on the mechanisms, efficacy, and clinical potential of these Ru-based drugs, which stand at the forefront of current research, aiming to provide more targeted, less toxic, and highly effective cancer treatments. This article examines the development and potential of five ruthenium-based anticancer drugs, highlighting their unique mechanisms, selective activity, and reduced toxicity. It details the progress of candidates: BOLD-100, TLD1433, RAPTA-C, RM175, and DiRu-1 in clinical or preclinical stages, showcasing their promise in providing targeted, effective cancer treatments. image C1 [Swaminathan, Srividya] Chennai Inst Technol, Ctr Computat Modelling, Chennai 600069, Tamil Nadu, India. [Swaminathan, Srividya] CSIR, CLRI, Inorgan & Phys Chem Lab, Chennai 600020, Tamil Nadu, India. [Haribabu, Jebiti] Univ Atacama, Fac Med, Los Carreras 1579, Copiapo 1532502, Chile. [Karvembu, Ramasamy] Natl Inst Technol, Dept Chem, Tiruchirappalli 620015, Tamil Nadu, India. C3 Chennai Institute of Technology; Council of Scientific & Industrial Research (CSIR) - India; CSIR - Central Leather Research Institute (CLRI); Universidad de Atacama; National Institute of Technology (NIT System); National Institute of Technology Tiruchirappalli