Melarsoprol

Melarsoprol
Clinical data
Trade namesArsobal
Other namesMel B, Melarsen Oxide-BAL
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration
IV
ATC code
Pharmacokinetic data
Elimination half-life35 hours
ExcretionKidney
Identifiers
  • (2-{4-[(4,6-Diamino-1,3,5-triazin-2-yl)amino]phenyl}-1,3,2-dithiarsolan-4-yl)methanol
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.007.086
Chemical and physical data
FormulaC12H15AsN6OS2
Molar mass398.33 g·mol−1
3D model (JSmol)
  • OCC1S[As](SC1)c3ccc(Nc2nc(nc(n2)N)N)cc3
  • InChI=1S/C12H15AsN6OS2/c14-10-17-11(15)19-12(18-10)16-8-3-1-7(2-4-8)13-21-6-9(5-20)22-13/h1-4,9,20H,5-6H2,(H5,14,15,16,17,18,19) Y
  • Key:JCYZMTMYPZHVBF-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

Melarsoprol is an arsenic-containing medication used for the treatment of sleeping sickness (African trypanosomiasis). It is specifically used for second-stage disease caused by Trypanosoma brucei rhodesiense when the central nervous system is involved. For Trypanosoma brucei gambiense, eflornithine or fexinidazole is usually preferred. It is effective in about 95% of people. It is given by injection and is known by patients as "fire in the veins" .

Melarsoprol has a high number of side effects. Common side effects include brain dysfunction, numbness, rashes, and kidney and liver problems. About 1–5% of people die during treatment, although this is tolerated due to sleeping sickness itself having a practically 100% mortality rate when untreated. In those with glucose-6-phosphate dehydrogenase (G6PD) deficiency, red blood cell breakdown may occur. It has not been studied in pregnancy. It works by blocking pyruvate kinase, an enzyme required for aerobic metabolism by the parasite.

Melarsoprol has been used medically since 1949. It is on the World Health Organization's List of Essential Medicines. In regions of the world where the disease is common, melarsoprol is provided for free by the World Health Organization. It is not commercially available in Canada or the United States. In the United States, it may be obtained from the Centers for Disease Control and Prevention, while in Canada it is available from Health Canada.