metallodrugs

Metallodrugs are pharmaceutical agents in which a metal atom or metal-containing moiety is an essential component of the drug’s structure and activity. They span coordination complexes, organometallic compounds, and metal-containing small molecules. Metallodrugs are studied across medicine and biomedicine for their unique reactivity, often enabling modes of action not accessible to purely organic drugs.

Common classes include platinum-based chemotherapeutics (cisplatin, carboplatin, oxaliplatin) that form DNA adducts; gold compounds (auranofin, aurothioglucose) used in rheumatology and investigated in oncology; other metal-based candidates such as ruthenium and titanium complexes; and radio-metal agents used in diagnostic imaging and radiotherapy (e.g., technetium-99m, lutetium-177 complexes).

Mechanisms vary: DNA binding and crosslinking; enzyme inhibition; redox cycling and reactive oxygen species generation; catalysis of biological reactions; photosensitization in photodynamic therapy. Metallodrugs can offer activity in cases of drug resistance and may enable targeted delivery via ligand design.

Challenges include toxicity and off-target effects, limited selectivity, complex pharmacokinetics, and supply or stability concerns. Ongoing research focuses on designing ligands that improve selectivity, reducing side effects, developing metallodrugs for imaging and therapy, and exploring novel metals and oxidation states for new mechanisms.