From Concept to Cure: The Road Ahead for Ruthenium‐Based Anticancer Drugs

• Published in: ChemMedChem 2024-12, Vol.19 (23), p.e202400435-n/a
• Main Authors: Swaminathan, Srividya, Haribabu, Jebiti, Karvembu, Ramasamy
• Format: Article
• Language: English
• Subjects: Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic drugs; Cancer therapies; Cell Proliferation - drug effects; Chemotherapy; Coordination Complexes - chemistry; Coordination Complexes - pharmacology; Cytotoxicity; Drug development; Drug discovery; Drug Screening Assays, Antitumor; Drugs; Effectiveness; Gold; Humans; Molecular Structure; Mustard gas; Neoplasms - drug therapy; Organometallic Compounds - chemical synthesis; Organometallic Compounds - chemistry; Organometallic Compounds - pharmacology; Ruthenium; Ruthenium - chemistry; Ruthenium - pharmacology; Ruthenium compounds
• ISSN: 1860-7179; 1860-7187; 1860-7187
• DOI: 10.1002/cmdc.202400435

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.