Melarsoprol

Melarsoprol
Clinical data
Trade namesArsobal[1]
Other namesMel B, Melarsen Oxide-BAL[2]
AHFS/Drugs.comMicromedex Detailed Consumer Information
Routes of
administration		IV
ATC code
Pharmacokinetic data
Elimination half-life35 hours
ExcretionKidney
Identifiers
IUPAC name
  • (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)
SMILES
  • OCC1S[As](SC1)c3ccc(Nc2nc(nc(n2)N)N)cc3
InChI
  • 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).[1] It is specifically used for second-stage disease caused by Trypanosoma brucei rhodesiense when the central nervous system is involved.[1] For Trypanosoma brucei gambiense, eflornithine or fexinidazole is usually preferred.[1] It is effective in about 95% of people.[3] It is given by injection[2] and is known by patients as "fire in the veins".[4]

Melarsoprol has a high number of side effects.[5] Common side effects include brain dysfunction, numbness, rashes, and kidney and liver problems.[2] 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.[3] In those with glucose-6-phosphate dehydrogenase (G6PD) deficiency, red blood cell breakdown may occur.[2] It has not been studied in pregnancy.[2] It works by blocking pyruvate kinase, an enzyme required for aerobic metabolism by the parasite.[2]

Melarsoprol has been used medically since 1949.[1] It is on the World Health Organization's List of Essential Medicines.[6] In regions of the world where the disease is common, melarsoprol is provided for free by the World Health Organization.[5] It is not commercially available in Canada or the United States.[2] 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.[1][2]

  1. ^ a b c d e f "Our Formulary". Infectious Diseases Laboratories. CDC. 22 September 2016. Archived from the original on 16 December 2016. Retrieved 7 December 2016.
  2. ^ a b c d e f g h "Melarsoprol Drug Information, Professional". Drugs.com. 20 December 1994. Archived from the original on 30 December 2016. Retrieved 7 December 2016.
  3. ^ a b "WHO Model Prescribing Information: Drugs Used in Parasitic Diseases - Second Edition: Protozoa: African trypanosomiasis: Melarsoprol". WHO. 1995. Archived from the original on 2016-11-10. Retrieved 2016-11-09.
  4. ^ Tarral A, Strub-Wourgaft N, Mordt OV (2022-05-11). "Development and Introduction of Fexinidazole into the Global Human African Trypanosomiasis Program". The American Journal of Tropical Medicine and Hygiene. 106 (5_Suppl): 61–66. doi:10.4269/ajtmh.21-1176. ISSN 0002-9637. PMC 9154641. PMID 35292581.
  5. ^ a b "Trypanosomiasis, human African (sleeping sickness)". World Health Organization. February 2016. Archived from the original on 4 December 2016. Retrieved 7 December 2016.
  6. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
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