Drug/Small Molecule:
sodium stibogluconate

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • sodium stibogluconate
Trade Names
  • Lenocta
  • Myostibin
  • Pentostam
  • Stibanate
  • Stibanose
  • Stibatin
  • Stibinol
Brand Mixture Names

PharmGKB Accession Id:
PA164743129

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.

Source: Drug Bank

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.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Sodium stibogluconate directly inhibits DNA topoisomerase I leading to inhibition of both DNA replication and transcription.

Source: Drug Bank

Pharmacology

The mode of action of sodium stibogluconate is not clearly understood. In vitro exposure of amastigotes to 500 mg pentavalent antimony/ml results in a greater than 50% decrease in parasite DNA, RNA protein and purine nucleoside triphosphate levels. It has been postulated that the reduction in ATP (adenosine triphosphate) and GTP (guanosine triphosphate) synthesis contributes to decreased macromolecular synthesis.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Toxicity

The main symptoms of antimony overdosage are gastro-intestinal disturbances (nausea, vomiting and severe diarrhoea). Haemorrhagic nephritis and hepatitis may also occur.

Source: Drug Bank

Chemical Properties

Chemical Formula

C12H35Na3O26Sb2

Source: Drug Bank

Isomeric SMILES

O.O.O.O.O.O.O.O.O.[Na+].[Na+].[Na+].OCC(O)C1O[Sb]2(O)(O[Sb]34([O-])OC(C(O)CO)C(O3)C(O4)C([O-])=O)OC1C(O2)C([O-])=O

Source: Drug Bank

Canonical SMILES

O.O.O.O.O.O.O.O.O.[Na+].[Na+]

Source: Drug Bank

Average Molecular Weight

907.88

Source: Drug Bank

Monoisotopic Molecular Weight

905.918601405

Source: Drug Bank

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB05630
ChEBI:
28148
KEGG Drug:
D00582
PubChem Compound:
16685683
Therapeutic Targets Database:
DCL000001

Clinical Trials

These are trials that mention sodium stibogluconate and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.