DT-Web

DB05630 - Sodium stibogluconate


Identification
Name Sodium stibogluconate
Accession Number DB05630
Type small molecule
Description Sodium stibogluconate is a medicine used to treat leishmaniasis and is only available for administration by injection. It belongs to the class of medicines known as the pentavalent antimonials. Sodium stibogluconate is sold in the UK as Pentostam (manufactured by GlaxoSmithKline). Widespread resistance has limited the utility of sodium stibogluconate, and in many parts of the world, amphotericin or miltefosine are used instead. It is also being investigated as an anti-tumor agent.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 907.88
Groups approved
Monoisotopic Weight 905.918601405
Pharmacology
Indication For the treatment of various types of a protozoal infection called leishmaniasis, which may result from sandfly bites in tropical and temperate parts of the world. Also investigated for use/treatment in cancer/tumors (unspecified) and solid tumors.
Mechanism of action Sodium stibogluconate directly inhibits DNA topoisomerase I leading to inhibition of both DNA replication and transcription.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity The main symptoms of antimony overdosage are gastro-intestinal disturbances (nausea, vomiting and severe diarrhoea). Haemorrhagic nephritis and hepatitis may also occur.
Affected organisms
  • Humans and other mammals
  • Protozoa
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


DNA topoisomerase 1
Name DNA topoisomerase 1
Gene Name TOP1
Pharmacological action yes
Actions inhibitor
References
  • Walker J, Saravia NG: Inhibition of Leishmania donovani promastigote DNA topoisomerase I and human monocyte DNA topoisomerases I and II by antimonial drugs and classical antitopoisomerase agents. J Parasitol. 2004 Oct;90(5):1155-62. - Pubmed
  • Chakraborty AK, Majumder HK: Mode of action of pentavalent antimonials: specific inhibition of type I DNA topoisomerase of Leishmania donovani. Biochem Biophys Res Commun. 1988 Apr 29;152(2):605-11. - Pubmed
  • Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. - Pubmed
DTHybrid score 0.9971

Predictions


Id Partner name Gene Name Score
3552 DNA topoisomerase 1 topA 0.9971
4180 DNA-(apurinic or apyrimidinic site) lyase APEX1 0.1088
102 DNA topoisomerase I, mitochondrial TOP1MT 0.0647
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0608
1588 Multidrug resistance protein 1 ABCB1 0.0467
817 DNA topoisomerase 2-alpha TOP2A 0.0423
4512 Cytochrome P450 3A4 CYP3A4 0.0178
4604 Liver carboxylesterase 1 CES1 0.0086
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0076
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0071
6147 Solute carrier family 22 member 3 SLC22A3 0.007
3923 Cholinesterase BCHE 0.0065
862 Multidrug resistance-associated protein 1 ABCC1 0.0064
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0064
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0059
587 Serum albumin ALB 0.0055
6030 Cytochrome P450 2B6 CYP2B6 0.0054
6107 Cytochrome P450 3A7 CYP3A7 0.0052
4118 Cytochrome P450 3A5 CYP3A5 0.005
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