EDTA was first synthesized during the late 1930's in Germany. In 1941, EDTA was used to treat people for health metal toxicity from poison gas. Later research established that EDTA contained a highly effective antidote to heavy metal toxicity (lead poisoning). EDTA chelated just as well with lead as it did calcium when it was infused into the blood stream and without any side effects.

In the 1950's, EDTA was first used for clinical use in Michigan to treat battery factory workers who were suffering from lead poisoning. Following the treatment, the patients who were suffering from angina and coronary artery disease symptoms dropped dramatically. This prompted the first studies to discover other therapeutic effects of EDTA. The first study of EDTA in occlusive vascular disease (clogged arteries) reported subsequent improvement. Navy sailors who were exposed to lead based paints were also treated in the mid 1950's. EDTA successfully dealt with this problem and the Food and Drug Administration (FDA) approved that EDTA is the ideal method for treating heavy metal poisoning. The FDA also agrees that EDTA is an effective emergency treatment for hypocalcaemia. The analysis of effectiveness was often marked to have improvement in the cardiovascular system of patients with heavy metal poisoning.