OBJECTIVE : This review illustrates heavy metals toxicity, currently available therapies and the role and efficacy of chelation therapy for its management. CONCLUSIONS : Heavy metals are necessary for various biological processes, but they become harmful in excess. Specifically, they induce oxidative stress by generating free radicals and reducing antioxidant levels. Heavy metals also alter the confirmation of protein and DNA and inhibit their function. Chelation therapy is commonly used to treat metals toxicity. Chelation is a chemical process that occurs when interaction between a central metal atom/ion and ligand leads to formation of a complex ring-like structure. The ligand has a donor ion/molecule, which has a lone pair of electrons and may be monodentate to polydentate. Each metal has a different reactivity with a ligand, so a specific chelation agent is required for each metal. Combination therapy with a chelating agent and an antioxidant led to improved outcome. CONCLUSIONS : Heavy metal poisoning is a common health problem because of mining, smelting, industrial, agricultural and sewage waste. Heavy metals can be efficiently excreted from the body following treatment with proper chelation agents.