Substance
ID:1044
Names and Identifiers
Brand Name
ArsodentClaudeliteArseniteClaudetiteArsenoliteTrisenox
Synonyms
Diarsenic TrioxideWhite ArsenicArsenic trioxideArsenic OxideArsenic Blanc [French]Arsenigen Saure [German]Arsenious OxideArsenous Oxide AnhydrideArsentrioxideOxyde Arsenieux [ISO-French]Diarsonic TrioxideHSDB 419Crude ArsenicArsenous AcidAnhydride Arsenieux [French]Acide Arsenieux [French]Arsenious AcidArsenous Acid AnhydrideArsenous OxideDi-Arsenic TrioxideArsenicum Albumarsenic trioxideArsenic Trioxide [UN1561] [Poison]Arsenic, WhiteArsenic SesquioxideArsenic Oxidearsenous TrioxideArseni TrioxydumArsenious Acid AnhydrideArsenious TrioxideArsenous AnhydridePoison Flour
IUPAC Traditional name
arsenic trioxide
IUPAC name
bicyclo[1.1.1]diarsoxane
Properties
Physical Property
Solubility
17 mg/mL at 16 oC [SHIU,WY et al. (1990)]
Molecule Details
Drug Groups
approved; investigational
Description
Arsenic trioxide is a chemotheraputic agent of idiopathic function used to treat leukemia that is unresponsive to first line agents. It is suspected that arsenic trisulfide induces cancer cells to undergo apoptosis. Due to the toxic nature of arsenic, this drug carries significant health risks. The enzyme thioredoxin reductase has recently been identified as a target for arsenic trioxide.
Indication
For induction of remission and consolidation in patients with acute promyelocytic leukemia (APL), and whose APL is characterized by the presence of the t(15;17) translocation or PML/RAR-alpha gene expression
Pharmacology
Arsenic Trioxide is indicated for induction of remission and consolidation in patients with acute promyelocytic leukemia (APL) who are refractory to, or have relapsed from, retinoid and anthracycline chemotherapy.
Toxicity
Symptoms of overdose include convulsions, muscle weakness and confusion.
Affected Organisms
Humans and other mammals
Biotransformation
The metabolism of arsenic trioxide involves reduction of pentavalent arsenic to trivalent arsenic by arsenate reductase and methylation of trivalent arsenic to monomethylarsonic acid and monomethylarsonic acid to dimethylarsinic acid by methyltransferases. The main site of methylation reactions appears to be the liver. Arsenic is stored mainly in liver, kidney, heart, lung, hair and nails.
Protein Binding
75% bound
Elimination
Trivalent arsenic is mostly methylated in humans and excreted in urine.
References
•
Lu J, Chew EH, Holmgren A: Targeting thioredoxin reductase is a basis for cancer therapy by arsenic trioxide. Proc Natl Acad Sci U S A. 2007 Jul 24;104(30):12288-93. Epub 2007 Jul 18.
[Pubmed]
External Links
Molecular Spectra
No Data Available
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References
• Lu J, Chew EH, Holmgren A: Targeting thioredoxin reductase is a basis for cancer therapy by arsenic trioxide. Proc Natl Acad Sci U S A. 2007 Jul 24;104(30):12288-93. Epub 2007 Jul 18. Pubmed