This article reviews the pharmacological properties and the uses of two important antidotes for heavy metal poisoning. Meso-dimercaptosuccinic acid (DMSA) and 2,3-dimercapto-l-propanesulfonic acid, Na salt (DMPS) are relatively new antidotes-new, that is, to the western world. Although DMSA was introduced originally by Friedheim et al (1) to increase uptake of antimony during schistosomiasis therapy, Liang et al (77) at Shanghai in 1957 were the first to report its effectiveness as an antidote for heavy metallpoisoning. The synthesis and some of the metal binding properties of DMPS were reported in 1956 by Petrunkin from Kiev (3). Shortly thereafter, DMPS became an official drug in the Soviet Union, where it is known as Unithiol (4). Between 1956 and 1975, DMSA and DMPS were studied extensively, at both the basic science and clinical levels, in the People's Republic of China, the Soviet Union, and Japan. Some of these investigations have been cited and can be found in an earlier review (5). In the USA and western Europe, however, these two compounds received very little attention until recently. A paper by Friedheim & Corvi (6) in 1975, dealing with DMSA for the treatment of mercury poisoning, and the recent production and availability of DMPS from Heyl & Co., Berlin, stimulated investigators to "rediscover" and study these two metal-binding agents. DMSA and DMPS are water soluble chemical analogs of dimercaprol (British Anti-Lewisite, BAL). In contrast to BAL, they have less toxicity, greater water solubility, and limited lipid solubility, and are effective when given orally. * Important notes are marked. 193 If levels of heavy metals such as arsenic, lead, mercury, and cadmium continue to increase in the environment (7), the need will increase also for more effective, therapeutically useful antidotes to treat poisoning by these metals. This need might be met, in the future, by either DMSA, DMPS, or both. They are replacing BAL in the experimental laboratory and in some clinical situations, as discussed below. All of the papers published on DMSA and DMPS cannot be cited in this review. Space limitations have been imposed on an already lengthy bibliography. Many Chinese, Soviet, and Japanese papers have been translated, reviewed, and included. An emphasis has been placed, though, on important articles published since 1975. GENERAL AND CHEMICAL PROPERTIES DMSA and the sodium salt of DMPS are available as white crystalline powders. BAL is an oily liquid. Chemical formulas can be found in an earlier review (5). DMPS has been prepared as the racemic mixture (3), dextro-rotatory form and levo-rotatory form (W. Parr, personal communication). Studies using the D-or L-form, however are rare. In the literature and in this article, the abbreviation DMPS, unless otherwise stated, denotes the racemic mixture of the sodium salt of 2,3-dimercapto-l-propanesulfonic acid. Since DMSA has two asymmetric carbon atoms, the compound exists as the meso form and the DL form. Meso-DMSA is easier to prepare, more readily available, and h...