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succimer

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Description

Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2724354
CHEMBL ID1201073
CHEBI ID63623
SCHEMBL ID14941
MeSH IDM0006442

Synonyms (85)

Synonym
AC-1366
dimercaptosuccinic acid
dmsa
C07598
meso-2,3-dimercaptosuccinic acid
succimer
304-55-2
dms-a
dim-sa
DB00566
D00572
chemet (tn)
meso-dimercaptosuccinic acid
succimer (usan/inn)
SPECTRUM1505007
chemet
brn 1725150
butanedioic acid, 2,3-dimercapto-, (2r,3s)-rel-
hsdb 6783
succimer [usan:inn:ban]
succimero [inn-spanish]
succinic acid, 2,3-dimercapto-, meso-
(r*,s*)-2,3-dimercaptobutanedioic acid
succimerum [inn-latin]
ro 1-7977
einecs 206-155-2
butanedioic acid, 2,3-dimercapto-, (r*,s*)-
meso-2,3-dimercaptosuccinic acid, ~98%
acid, meso-dimercaptosuccinic
butanedioic acid, 2,3-dimercapto-, (r*,s*)-isomer
meso dimercaptosuccinic acid
chebi:63623 ,
CHEMBL1201073
D1722
(2s,3r)-2,3-bis(sulfanyl)butanedioic acid
succimero
dx1u2629qe ,
unii-dx1u2629qe
succimerum
A820382
(2r,3s)-rel-2,3-dimercaptosuccinic acid
3-03-00-01033 (beilstein handbook reference)
S4692
(2r,3s)-2,3-disulfanylsuccinic acid
meso-2,3-dimercaptobernsteinsaeure
AKOS015892684
BRD-K88701661-001-01-1
succimer [who-dd]
succimer [ii]
succimer [orange book]
succimer [mart.]
succimer [mi]
succimer [usan]
succimer [hsdb]
succimer [vandf]
succimer [inn]
2,3-dimercaptosuccinic acid, meso-
CCG-214189
SCHEMBL14941
Q-201748
2,3-bis-sulfanylbutanedioic acid
mfcd00064799
DTXSID1023601 ,
(2r,3s)-rel-2,3-dimercaptobutanedioic acid
(2r,3s)-2,3-dimercaptosuccinic acid
HY-B1768
DS-7410
CS-0013797
Q423814
meso-2,3-dimercaptosuccinic acid;
A17093
dimercaptosuccinic-acid
dimercaptosuccinic acid;dmsa
dmsa (meso-2,3-dimercaptosuccinic acid)
EN300-1720731
(2r,3s)-2,3-disulfanylbutanedioic acid
Z1255431202
v09ca02
succimer (ii)
meso-2,3-dimercaptobernsteinsaure
succimero (inn-spanish)
meso 2, 3-dimercaptosuccinic acid
succimer (mart.)
succimerum (inn-latin)
dtxcid903601

Research Excerpts

Overview

Succimer is a chelation agent used in the treatment of heavy metal intoxication. Succimer forms stable, water-soluble complexes with lead. It also chelates other toxic heavy metals, such as arsenic and mercury.

ExcerptReferenceRelevance
"Succimer is a chelation agent used in the treatment of heavy metal intoxication."( Toxicokinetics of mercury elimination by succimer in twin toddlers.
Fayez, I; Koren, G; Paiva, M; Thompson, M; Verjee, Z, 2005
)
1.32
"Succimer is considered to be a safe and effective treatment for lead (Pb) poisoning, since it reduces body Pb levels without an apparent diuresis of other essential elements. "( Succimer and the urinary excretion of essential elements in a primate model of childhood lead exposure.
Calacsan, C; Cremin, J; Laughlin, NK; Luck, M; Smith, DR; Woolard, D, 2000
)
3.19
"Succimer is an orally active, heavy-metal chelating agent that forms stable, water-soluble complexes with lead; it also chelates other toxic heavy metals, such as arsenic and mercury."( Succimer, an oral lead chelator.
Mann, KV; Travers, JD, 1991
)
2.45

Treatment

Succimer treatment significantly (p < 0.05) reduced blood Pb levels. Succimer-treated children had an abrupt drop in blood lead level. Treatment with succimer lowered blood lead levels but did not improve scores on tests of cognition, behavior, or neuropsychological function.

ExcerptReferenceRelevance
"Succimer treatment of the Pb-exposed rats significantly improved learning, attention, and arousal regulation, although the efficacy of the treatment varied as a function of the Pb exposure level and the specific functional deficit."( Succimer chelation improves learning, attention, and arousal regulation in lead-exposed rats but produces lasting cognitive impairment in the absence of lead exposure.
Beaudin, SA; Levitsky, DA; Smith, DR; Stangle, DE; Strawderman, MS; Strupp, BJ, 2007
)
2.5
"Succimer treatment significantly (p < 0.05) reduced blood Pb levels when compared to the vehicle group over the treatment period, and concomitantly produced a significant >4-fold increase in urinary Pb excretion."( Succimer and the urinary excretion of essential elements in a primate model of childhood lead exposure.
Calacsan, C; Cremin, J; Laughlin, NK; Luck, M; Smith, DR; Woolard, D, 2000
)
2.47
"Succimer-treated children had an abrupt drop in blood lead level, followed by rebound."( Safety and efficacy of succimer in toddlers with blood lead levels of 20-44 microg/dL. Treatment of Lead-Exposed Children (TLC) Trial Group.
, 2000
)
1.34
"Treatment with succimer lowered blood lead levels but did not improve scores on tests of cognition, behavior, or neuropsychological function in children with blood lead levels below 45 microg per deciliter. "( The effect of chelation therapy with succimer on neuropsychological development in children exposed to lead.
Chisolm, JJ; Dietrich, KN; Dockery, DW; Jones, RL; Radcliffe, J; Ragan, NB; Rhoads, GG; Rogan, WJ; Salganik, M; Ware, JH, 2001
)
0.94

Toxicity

ExcerptReferenceRelevance
" The LD50 of HV was 19."( Effect of dimercaptosuccinic acid on toxicity of Habu snake (Trimeresurus flavoviridis, Hallowell) venom.
Kurihara, N, 1978
)
0.26
"A family of four developed toxic blood levels of mercury after the mother vacuumed a spilled jar of liquid mercury from a closet in their apartment."( Toxicity of a family from vacuumed mercury.
Montiel, MM; Schwartz, JG; Snider, TE, 1992
)
0.28
"A daily dosing model for methylmercury (MM) intoxication was developed for the purpose of testing for possible adverse effects resulting from the administration of complexing agents used in the treatment of MM poisoning."( A methylmercury toxicity model to test for possible adverse effects resulting from chelating agent therapy.
Kostyniak, PJ; Soiefer, AI, 1984
)
0.27
" The order of toxicity of the arsenic compounds to the worms was PDA > arsenite > arsenate (24 h LD50 values were 189."( Evaluation of three antidotes on arsenic toxicity in the common earthworm (Lumbricus terrestris).
Chien, PK; Furst, A; Li, W,
)
0.13
" DMSA is orally actively, relatively safe and specific, and can, in some situations, be used on an out-patient basis."( Conceptual and practical advances in the measurement and clinical management of lead toxicity.
Graziano, JH,
)
0.13
" The finding that DMSA administered late in exposure can hasten the recovery of toxic signs suggests that extracellular Pb continues to play a significant role even after toxic signs have appeared."( Effect of chelation with meso-dimercaptosuccinic acid (DMSA) before and after the appearance of lead-induced neurotoxicity in the rat.
Evans, HL; Gong, Z, 1997
)
0.3
" Seven groups of adult male rats were given a single sc toxic dose of HgCl2 (0."( Comparison of the effectiveness of 2,3-dimercaptopropanol (BAL) and meso-2,3-dimercaptosuccinic acid (DMSA) as protective agents against mercuric chloride-induced nephrotoxicity in rats.
Bellés, M; de la Torre, A; Domingo, JL; Llobet, JM; Mayayo, E, 1998
)
0.3
" In dependence on the length of the alkyl chains these organotins exert toxic effects on the immune system, the bile duct, liver and pancreas."( Antidotal effects of 2,3-dimercaptopropane-1-sulfonic acid (DMPS) and meso-2,3-dimercaptosuccinic acid (DMSA) on the organotoxicity of dibutyltin dichloride (DBTC) in rats.
Hennighausen, G; Kröning, G; Merkord, J; Weber, H, 2000
)
0.31
" There were no adverse reactions attributable to dimercaptosuccinic acid; however, 2 of the 59 patients were reexposed to defective lead paint and experienced sharp increases in blood lead concentration while on therapy."( Safety and efficacy of meso-2,3-dimercaptosuccinic acid (DMSA) in children with elevated blood lead concentrations.
Chisolm, JJ, 2000
)
0.31
"Dimercaptosuccinic acid is apparently safe and does mobilize lead into the urine, but not the essential metals, zinc and copper."( Safety and efficacy of meso-2,3-dimercaptosuccinic acid (DMSA) in children with elevated blood lead concentrations.
Chisolm, JJ, 2000
)
0.31
"Mercury exposure is the second-most common cause of toxic metal poisoning."( Mercury toxicity and antioxidants: Part 1: role of glutathione and alpha-lipoic acid in the treatment of mercury toxicity.
Patrick, L, 2002
)
0.31
" Arsenic as an environmental agent is considered to be a toxic substance due to its carcinogenic potential in humans."( Combined efficacies of DL-alpha-lipoic acid and meso 2,3 dimercaptosuccinic acid against arsenic induced toxicity in antioxidant systems of rats.
Devi, MA; Kokilavani, V; Panneerselvam, C; Sivarajan, K, 2005
)
0.33
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Both munitions grade and distilled Lewisite were extremely toxic with LC(50) values in the low ng/ml range, with no significant differences between them."( Therapeutic effects of hypothermia on Lewisite toxicity.
Hancock, JR; Nelson, P; Sawyer, TW, 2006
)
0.33
"To determine if dimercaptosuccinic acid (DMSA), an agent originally developed as a safe non-toxic antidote for heavy metal poisoning, would be useful as a kidney radiation dose reduction agent in patients undergoing radiopeptide therapy for cancer."( Pre-clinical evaluation of 2,3-dimercaptosuccinic acid as a radiation nephrotoxicity protective agent during radiopeptide therapy of neuroendocrine malignancy.
Meyrick, DP; Moorin, RE; Rose, A, 2007
)
0.34
" IR spectroscopy further suggested that MiADMSA bind to arsenic to form adduct, which prevents arsenic from exerting its toxic effect in both models."( Monoisoamyl dimercaptosuccinic acid abrogates arsenic-induced developmental toxicity in human embryonic stem cell-derived embryoid bodies: comparison with in vivo studies.
Flora, SJ; Mehta, A, 2009
)
0.35
"Overall, DMSA therapy seems to be reasonably safe, effective in removing several toxic metals (especially lead), dramatically effective in normalizing RBC glutathione, and effective in normalizing platelet counts."( Safety and efficacy of oral DMSA therapy for children with autism spectrum disorders: Part A--medical results.
Adams, JB; Baral, M; Bradstreet, J; El-Dahr, J; Gehn, E; Geis, E; Hensley, A; Ingram, J; Mitchell, J; Mitchell, K; Newmark, S; Rubin, RA; Zappia, I, 2009
)
0.35
"Overall, both one and seven rounds of DMSA therapy seems to be reasonably safe in children with ASD who have high urinary excretion of toxic metals, and possibly helpful in reducing some of the symptoms of autism in those children."( Safety and efficacy of oral DMSA therapy for children with autism spectrum disorders: part B - behavioral results.
Adams, JB; Baral, M; Bradstreet, J; El-Dahr, J; Gehn, E; Geis, E; Hensley, A; Ingram, J; Mitchell, J; Mitchell, K; Newmark, S; Rubin, RA; Zappia, I, 2009
)
0.35
"Lead causes a broad range of adverse effects in humans and animals."( Lactobacillus plantarum CCFM8661 alleviates lead toxicity in mice.
Chen, W; Liu, X; Tian, F; Wang, G; Zhai, Q; Zhang, H; Zhao, J, 2012
)
0.38
" After exposure from L4-larvae for 24-hr, DMSA coated Fe(2)O(3)-NPs at concentrations more than 50 mg/L exhibited adverse effects on nematodes."( Evaluation of environmental safety concentrations of DMSA Coated Fe2O3-NPs using different assay systems in nematode Caenorhabditis elegans.
Li, Y; Tang, M; Wang, D; Wu, Q, 2012
)
0.38
" Development of intrinsically safe IONP chemistries requires a robust in vivo nanoneurotoxicity screening model."( In vivo nanoneurotoxicity screening using oxidative stress and neuroinflammation paradigms.
Chen, LH; Jin, S; Kim, Y; Kong, SD; Pisanic, TR; Shubayev, VI, 2013
)
0.39
"Exposure to toxic metals remains a widespread occupational and environmental problem in world."( Nanoencapsulation of DMSA monoester for better therapeutic efficacy of the chelating agent against arsenic toxicity.
Babbar, AK; Flora, SJ; Kaushik, MP; Kushwaha, P; Lomash, V; Mathur, R; Mishra, AK; Pathak, U; Samim, M; Yadav, A, 2014
)
0.4
" The results demonstrated that thiol-coating iron oxide magnetic nanoparticles have few toxic effects in cells, whereas S-nitrosated-coated particles did cause toxic effects."( Preparation, characterization, cytotoxicity, and genotoxicity evaluations of thiolated- and s-nitrosated superparamagnetic iron oxide nanoparticles: implications for cancer treatment.
de Lima, R; Ferrarini, AC; Haddad, PS; Pasquôto, T; Santos, Mda C; Seabra, AB, 2014
)
0.4
" The toxic effect of Pb on kidneys was also studied."( Silymarin and dimercaptosuccinic acid ameliorate lead-induced nephrotoxicity and genotoxicity in rats.
Alcaraz-Contreras, Y; Gallegos-Corona, MA; Martínez-Alcaraz, ER; Martínez-Alfaro, M; Mendoza-Lozano, RP; Ramírez-Morales, MA; Vázquez-Guevara, MA, 2016
)
0.43
" Chelating agents work by forming less toxic complexes with the toxic metal ions which are readily excreted from the body."( Nano drug delivery systems: a new paradigm for treating metal toxicity.
Flora, SJ; Yadav, A, 2016
)
0.43
" DMSA has considerably lower toxicity than the classic heavy metal antagonist BAL (2,3-dimercaptopropanol) and is also less toxic than DMPS."( Metal chelators and neurotoxicity: lead, mercury, and arsenic.
Aaseth, J; Bjørklund, G; Mutter, J, 2017
)
0.46
"Copper oxide nanoparticles (CuO-NPs) dispersions are known for their high cell toxic potential but contaminating copper ions in such dispersions are a major hurdle in the investigation of specific nanoparticle-mediated toxicity."( Uptake of Intact Copper Oxide Nanoparticles Causes Acute Toxicity in Cultured Glial Cells.
Dringen, R; Jog, K; Joshi, A; Thiel, K, 2019
)
0.51
"Chelation therapy is considered as a safe and effective strategy to combat metal poisoning."( Comparative efficacy of Nano and Bulk Monoisoamyl DMSA against arsenic-induced neurotoxicity in rats.
Flora, SJS; Kumar, P; Naqvi, S, 2020
)
0.56
" The available chelator drugs used now have many adverse effects."( Synergistic protective effect of Beta vulgaris with meso-2,3-dimercaptosuccinic acid against lead-induced neurotoxicity in male rats.
Abd El-Kader, SE; El-Kersh, MAL; Habashy, NH; Mogahed, FAK; Shaban, NZ, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" Elimination half-life of total DMSA (parent drug plus oxidized metabolites) was longer in children with lead poisoning (3."( Pharmacokinetics of meso-2,3-dimercaptosuccinic acid in patients with lead poisoning and in healthy adults.
Aposhian, HV; Dart, RC; Hassen, LV; Hurlbut, KM; Maiorino, RM; Mayersohn, M, 1994
)
0.29
" We also carried out a pharmacokinetic analysis of this drug to support arsenic chelation."( Monoisoamyl 2, 3-dimercaptosuccinic acid (MiADMSA) demonstrates higher efficacy by oral route in reversing arsenic toxicity: a pharmacokinetic approach.
Bhadauria, S; Flora, SJ; Pachauri, V; Yadav, A, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
"The objective of the present study was to investigate the anticancer efficacy of dimercaptosuccinic acid modified iron oxide (DMSA-Fe3O4) magnetic nanoparticles (MNPs) combined with arsenic trioxide (As2O3) and doxorubicin (ADM) in non-Hodgkin's lymphoma (NHL) cell line (Raji cells)."( Antitumor efficacy of DMSA modified Fe3O4 magnetic nanoparticles combined with arsenic trioxide and adriamycin in Raji cells.
Bao, W; Cai, X; Chen, B; Chen, Y; He, Z; Hua, W; Shen, F; Shi, Y; Wang, C; Wang, X; Xia, G; Yu, L; Zhang, Y, 2014
)
0.4
" The objective of this study was to target therapy of MM cancer stem cells using gamma-Fe2O3@DMSA magnetic nanoparticle combination with paclitaxel and anti-ABCG2 monoclonal antibody, and to evaluate the combined therapeutic efficacy."( Gamma-Fe2O3 nanoparticles increase therapeutic efficacy of combination with paclitaxel and anti-ABCG2 monoclonal antibody on multiple myeloma cancer stem cells in mouse model.
Dou, J; Gu, N; He, X; Song, L; Yang, C; Zhan, X; Zhang, Y, 2014
)
0.4
"The purpose of this study was to determine the potential benefits of combination therapy using dimercaptosuccinic acid modified iron oxide (DMSA-Fe3O4) magnetic nanoparticles (MNPs) combined with nontoxic concentration of bortezomib (BTZ) and gambogic acid (GA) on multiple myeloma (MM) RPMI-8226 cells and possible underlying mechanisms."( Inducing cell cycle arrest and apoptosis by dimercaptosuccinic acid modified Fe3O4 magnetic nanoparticles combined with nontoxic concentration of bortezomib and gambogic acid in RPMI-8226 cells.
Chen, B; Qiao, L; Senthilkumar, R; Wang, F; Wang, X; Zhang, W, 2015
)
0.42
"To evaluate the activity of carbapenems alone or combined with DMSA against MBL-producing Escherichia coli in a severe murine peritonitis model."( Dimercaptosuccinic acid in combination with carbapenems against isogenic strains of Escherichia coli producing or not producing a metallo-β-lactamase in vitro and in murine peritonitis.
Chau, F; Cheminet, G; de Lastours, V; Fantin, B; Massias, L; Nordmann, P; Peoc'h, K; Poirel, L, 2020
)
0.56
" MIC determinations and time-kill assays were performed for imipenem, meropenem and ertapenem alone or in combination with DMSA."( Dimercaptosuccinic acid in combination with carbapenems against isogenic strains of Escherichia coli producing or not producing a metallo-β-lactamase in vitro and in murine peritonitis.
Chau, F; Cheminet, G; de Lastours, V; Fantin, B; Massias, L; Nordmann, P; Peoc'h, K; Poirel, L, 2020
)
0.56
"DMSA in combination with each carbapenem caused a significant decrease in the MICs for all MBL-producing strains, in a concentration-dependent manner, but did not provide benefit against non-MBL strains."( Dimercaptosuccinic acid in combination with carbapenems against isogenic strains of Escherichia coli producing or not producing a metallo-β-lactamase in vitro and in murine peritonitis.
Chau, F; Cheminet, G; de Lastours, V; Fantin, B; Massias, L; Nordmann, P; Peoc'h, K; Poirel, L, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
" Although the bioavailability of DMSA was limited in either species, DMSA was detected in the blood of both species within minutes after oral dosing."( The biological fate of 14C-dimercaptosuccinic acid in monkeys and rabbits.
Boswell, G; Kincannon, L; Speckman, CL; Tillotson, JA, 1989
)
0.28
" In vivo effectiveness may depend on bioavailability of Sb in the host and the direct action on the parasite, reflected by its in vitro activity."( Antitrypanosomal activity of trivalent antimonials in vitro and its significance.
Ercoli, N; Minelli, EB; Olivo, N, 1980
)
0.26
" The bioavailability of methylmercury in fish may be affected by other meal components."( Green Tea Increases the Concentration of Total Mercury in the Blood of Rats following an Oral Fish Tissue Bolus.
Chen, TY; Craig, BA; Freiser, H; Janle, EM; Manganais, C; Santerre, CR, 2015
)
0.42

Dosage Studied

There is limited information defining the optimal dosing regimen in the treatment of children with chronic lead poisoning. Lead and lead-vehicle dosing were discontinued while succimer was administered.

ExcerptRelevanceReference
" At 24 hr after the intramuscular dosing of 1 mg of HV into rats, lymphopenia, acute involution of lymphatic tissue, decrease in liver glycogen and lipid granules in zona fasiculata were apparent, indicating the mark of a stressor."( Effect of dimercaptosuccinic acid on toxicity of Habu snake (Trimeresurus flavoviridis, Hallowell) venom.
Kurihara, N, 1978
)
0.26
" DMSA effectiveness was assessed at dosage levels of 0, 80, 160, and 320 mg/kg/day."( meso-2,3-Dimercaptosuccinic acid and prevention of arsenite embryotoxicity and teratogenicity in the mouse.
Bosque, MA; Domingo, JL; Piera, V, 1991
)
0.28
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of succimer when used for the treatment of lead poisoning are reviewed."( Succimer, an oral lead chelator.
Mann, KV; Travers, JD, 1991
)
1.94
" Examination of fetuses for gross external abnormalities, visceral and skeletal malformations, or ossification variations revealed that DMSA did not produce teratogenicity at any dosage level."( Oral meso-2,3-dimercaptosuccinic acid in pregnant Sprague-Dawley rats: teratogenicity and alterations in mineral metabolism. I. Teratological evaluation.
Corbella, J; Domingo, JL; Llobet, JM; Ortega, A; Paternain, JL, 1990
)
0.28
" Equimolar dosing schedules were used based upon realistic doses for the most toxic agent, BAL."( Evaluation of the efficacy of dimercapto chelating agents for the treatment of systemic organic arsenic poisoning in rabbits.
Bright, JE; Inns, RH; Marrs, TC; Rice, P, 1990
)
0.28
" The reductions caused by MEDMS and EEDMS were approximately 20 and 26%, respectively, whereas under similar dosage regimens BAL effected about only a 12% reduction."( The mobilization of intracellular cadmium by alkoxyethyl esters of meso-2,3-dimercaptosuccinic acid.
Atkins, LM; Gale, GR; Jones, MM; Singh, PK; Smith, AB, 1990
)
0.28
" The utility of the method was demonstrated by analyzing the urine of rats orally dosed with DMSA."( Gas chromatographic analysis of urinary dimercaptosuccinic acid.
Knudsen, JJ; McGown, EL, 1988
)
0.27
"6 mmol/kg, a value which allows it to be given at a higher dosage than other known lipid-soluble dithiols."( Mobilization of aged in vivo cadmium deposits by diethyl dimercaptosuccinate.
Gale, GR; Jones, MM; Jones, SG; Singh, PK, 1988
)
0.27
" A dose-response study was made of the mobilization of cadmium from the liver and kidney of cadmium-loaded mice by NaB; this showed that NaB is one of the most effective cadmium mobilizing agents developed to date."( Meso-2,3-dimercaptosuccinic acid and sodium N-benzyl-N-dithiocarboxy-D-glucamine as antagonists for cadmium intoxication.
Basinger, MA; Gale, GR; Holscher, MA; Jones, MM; Jones, SG; Topping, RJ, 1988
)
0.27
"A daily dosing model for methylmercury (MM) intoxication was developed for the purpose of testing for possible adverse effects resulting from the administration of complexing agents used in the treatment of MM poisoning."( A methylmercury toxicity model to test for possible adverse effects resulting from chelating agent therapy.
Kostyniak, PJ; Soiefer, AI, 1984
)
0.27
"The effects of Astiban, Lucanthone, Hycanthone and Niridazole on autophagic activities in the gastrodermis of Schistosoma mansoni were determined in vivo, using different dosage levels and dosage times."( Schistosoma mansoni: an in vivo study of drug-induced autophagy in the gastrodermis.
Clarkson, J; Erasmus, DA, 1984
)
0.27
" An earlier dose of EDTA also modified the relation between ALAU and DMSA-chelatable lead in that workers who received EDTA before DMSA showed a much steeper dose-response relation between these two measures."( Provocative chelation with DMSA and EDTA: evidence for differential access to lead storage sites.
Ahn, KD; Lee, BK; Schwartz, BS; Stewart, W, 1995
)
0.29
" The low toxicity of DMPS and DMSA compared to BAL enabled doses of 160 mumol kg-1 on a more prolonged dosing schedule to be used for DMPS and DMSA."( Efficacy of dimercapto chelating agents for the treatment of poisoning by percutaneously applied dichloro(2-chlorovinyl)arsine in rabbits.
Inns, RH; Rice, P, 1993
)
0.29
" At the same dosage monoisoamyl meso-2,3-dimercaptosuccinate (Mi-ADMS) and a dithiocarbamate, sodium N-benzyl-4-O-(beta-D-galactopyranosyl)-D-glucamine-N-carbodithioate++ + (BLDTC) induced reductions of 65% and 57%, respectively."( Cadmium mobilization by monoaralkyl- and monoalkyl esters of meso-2,3-dimercaptosuccinic acid and by a dithiocarbamate.
Basinger, MA; Gale, GR; Jones, MM; Singh, PK; Smith, AB, 1994
)
0.29
" Determination of the comparative dose-response relationships of DMSA and Mi-ADMS on corporal and renal mercury concentrations revealed the monoester to be more active than DMSA on both parameters at each dose used."( meso-2,3-dimercaptosuccinic acid monoalkyl esters: effects on mercury levels in mice.
Gale, GR; Jones, MM; Singh, PK; Smith, AB, 1993
)
0.29
" Compared to BGDTC, the new compounds were, except at the highest dosage studied, equally or more effective in decreasing retention of hepatic cadmium, while mostly less effective in decreasing renal cadmium."( Meso-2,3-dimercaptosuccinic acid mono-N-alkylamides: syntheses and biological activity as novel in vivo cadmium mobilizing agents.
Blanusa, M; Jones, MM; Piasek, M; Restek-Samarzija, N; Rostial, K; Singh, PK, 1996
)
0.29
" Dosing was conducted daily beginning on day 8 postpartum."( The effects of elevated blood lead levels and succimer chelation therapy on physical growth in developing rhesus monkeys.
Lasky, RE; Laughlin, NK; Luck, ML, 2001
)
0.57
"There is limited information defining the optimal dosing regimen of succimer in the treatment of children with chronic lead poisoning."( A comparison of two dosing regimens of succimer in children with chronic lead poisoning.
Farrar, HC; McLeane, LR; Wallace, M; Watson, J; White, K, 1999
)
0.81
" Lead and lead-vehicle dosing were discontinued while succimer was administered."( The effects of succimer chelation therapy on auditory function in rhesus monkeys.
Lasky, RE; Laughlin, NK; Luck, ML,
)
0.73
" Calves in groups 2 to 5 were dosed daily with lead (5 mg/kg, PO) for 10 days."( Effects of calcium disodium EDTA and meso-2,3-dimercaptosuccinic acid on tissue concentrations of lead for use in treatment of calves with experimentally induced lead toxicosis.
Ko, KW; Meldrum, JB, 2003
)
0.32
" In some patients, the diagnosis of mercury poisoning has been made based on urine mercury excretions following oral dosing of meso-dimercaptosuccinic acid (DMSA), a metal chelator."( Urine mercury excretion following meso-dimercaptosuccinic acid challenge in fish eaters.
Caldwell, KL; Curry, SC; Gerkin, RD; Osterloh, JD; Ruha, AM; Wax, PM, 2009
)
0.35
"The D-AMB-coated PLGA-DMSA nanoparticle showed antifungal efficacy, fewer undesirable effects and a favourable extended dosing interval."( Amphotericin B in poly(lactic-co-glycolic acid) (PLGA) and dimercaptosuccinic acid (DMSA) nanoparticles against paracoccidioidomycosis.
Amaral, AC; Bentes, R; Bocca, AL; Felipe, MS; Lacava, ZG; Morais, PC; Nunes, J; Peixoto, DL; Primo, FL; Ribeiro, AM; Simioni, AR; Tedesco, AC; Titze-de-Almeida, R, 2009
)
0.35
" For this, AMB nanoencapsulated in poly(lactic-co-glycolic acid) (PLGA) and dimercaptosuccinic acid (DMSA) nanoparticles (Nano-D-AMB) has been developed, and its efficacy was evaluated in the treatment of experimental cutaneous leishmaniasis in C57BL/6 mice, to test if our nano-drug delivery system could favor the reduction of the dose frequency required to achieve the same therapeutic level of free D-AMB, and so, an extended dosing interval."( Leishmanicidal activity of amphotericin B encapsulated in PLGA-DMSA nanoparticles to treat cutaneous leishmaniasis in C57BL/6 mice.
Báo, SN; Cintra e Silva, Dde O; de Carvalho, RF; de Souza Filho, J; Lacava, ZG; Martins, OP; Miranda-Vilela, AL; Ribeiro, IF; Sampaio, RN; Tedesco, AC, 2013
)
0.39
" Cd(2+) is a related environmental pollutant that is of increasing public health concern due to a demonstrated dose-response between urinary Cd level and an increased risk of diabetes."( Structural characterization of Cd²⁺ complexes in solution with DMSA and DMPS.
Gailer, J; George, GN; Pickering, IJ; Zeini Jahromi, E, 2014
)
0.4
" They were dosed with each of the treatments with each meal."( Green Tea Increases the Concentration of Total Mercury in the Blood of Rats following an Oral Fish Tissue Bolus.
Chen, TY; Craig, BA; Freiser, H; Janle, EM; Manganais, C; Santerre, CR, 2015
)
0.42
" A nasogastric tube was immediately placed and the patient received treatment with a chelating agent dimercaptosuccinic acid (DMSA)/succimer 800 mg orally three times a day, a dosage decided on the basis of her body weight, plus phenytoin 125 mg intravenously three times a day."( Elemental mercury mixed with alcohol injected intravenously as a suicide attempt.
Karatapanis, S; Kotis, A; Lamprianou, F; Ntetskas, G, 2015
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
chelatorA ligand with two or more separate binding sites that can bind to a single metallic central atom, forming a chelate.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
dicarboxylic acidAny carboxylic acid containing two carboxy groups.
dithiol
sulfur-containing carboxylic acidAny carboxylic acid having a sulfur substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Replicase polyprotein 1abBetacoronavirus England 1IC50 (µMol)10.00000.00403.43889.5100AID1640022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)1.72000.00022.45859.9600AID1640021
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID1594144Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme acti2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1594145Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity 2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,577)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990427 (27.08)18.7374
1990's576 (36.53)18.2507
2000's281 (17.82)29.6817
2010's226 (14.33)24.3611
2020's67 (4.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 52.09

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index52.09 (24.57)
Research Supply Index7.45 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index88.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (52.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials57 (3.42%)5.53%
Reviews81 (4.86%)6.00%
Case Studies269 (16.16%)4.05%
Observational2 (0.12%)0.25%
Other1,256 (75.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Individual Therapy for Patients With Wilson's Disease [NCT03957720]Early Phase 1400 participants (Anticipated)Interventional2019-03-15Recruiting
DMSA Treatment of Children With Autism and Heavy Metal Toxicity [NCT00811083]Phase 1/Phase 280 participants (Actual)Interventional2005-05-31Completed
Monitoring, Detoxifying, and Rebalancing Metals During Acute Myeloid Leukemia (AML) and Myelodysplastic Syndrome (MDS) Therapy [NCT03630991]Phase 158 participants (Anticipated)Interventional2018-10-11Recruiting
Treatment of Lead-Exposed Children (TLC) Trial [NCT00342849]Phase 3780 participants (Actual)Interventional1994-07-15Completed
[NCT00004838]175 participants Interventional1997-09-30Completed
[NCT00374894]500 participants Observational2004-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]