Dimercaptosuccinic acid is indicated for the treatment of lead poisoning in children with blood level measured above 45 µg/dl. The use of DMSA is not approved for prevention of lead poisoning in anticipation of exposure in known lead-contaminated environments. DMSA can cross the blood-brain barrier of mice, but it is not if this is also the case in humans. Even if DMSA cannot reverse the damages done to the central nervous system, it might prevent further deterioration.
DMSA facilitates urinary excretion of lead, and with sufficiently aggressive treatment, can reduce lead content in the brain. It also increases urinary excretion of copper and zinc. DMSA improved cognitive function in rats that had been exposed to lead, but reduced cognitive function in rats that had not been exposed to lead.
Meso 2,3-dimercaptosuccinic acid binds to "soft" heavy metals such as Hg2+ and Pb2+, mobilizing these ions for excretion. It binds to metal cations through the thiol groups, which ionize upon complexation.
DMSA was first synthesized by V. Nirenburg in the Urals Polytechnic Institute, commissioned by one of the electrical enterprises of Sverdlovsk, which consumed many tons of mercury and was looking for a medicine to prevent poisoning of personnel. In 1957, Chinese scientists found that DMSA can effectively treat antimony poisoning due to overdose of tartar emetic. Pronounced protective effect in animal poisoning with arsenic and mercury was first shown by I. Okonishnikova in 1962. In 1984, the now-defunct Bock Pharmaceutical Company requested the FDA grant approval for orphan drug status under the trade name Chemet and the FDA approved of this in 1991, providing exclusivity until 1998 which was conveyed to the successor Sanofi in 1996.
^Aasath, Jan; Dag Jacobsen; Ole Andersen; Elsa Wickstrøm (March 1995). "Treatment of Mercury and Lead Poisonings with Dimercaptosuccinic Acid (DMSA) and Sodium Dimercaptopropanesulfonate (DMPS)". Analyst. 120 (3): 853ff. doi:10.1039/an9952000853.
^Clarkson, Thomas W.; Magos, Laszlo; Myers, Gary J. (2003-10-30). "The Toxicology of Mercury -- Current Exposures and Clinical Manifestations". New England Journal of Medicine. 349 (18): 1731-1737. doi:10.1056/nejmra022471. ISSN0028-4793. PMID14585942.
^Liang, Y., Chu. C, Tsen, Y., Ting, K. (1957). "Studies on antibilharzial drugs. Vl. The antidotal effects of sodium dimercaptosuccinate and BAL-glucoside against tartar emetic". Acta Physiol. Sin. 21: 24-32.CS1 maint: Multiple names: authors list (link)
Aposhian, H.V.; Aposhian, M.M. (1990). "Meso-2,3-dimercaptosuccinic acid: Chemical, pharmacological and toxicological properties of an orally effective metal chelating agent". Annual Review of Pharmacology and Toxicology. 30 (1): 279-306. doi:10.1146/annurev.pa.30.040190.001431. PMID2160791.