Page last updated: 2024-12-06

melarsomine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Melarsomine is an arsenic-containing drug used to treat late-stage African trypanosomiasis (sleeping sickness). It is a synthetic compound derived from melarsen oxide, a naturally occurring compound with trypanocidal activity. Melarsomine targets the enzyme trypanothione reductase, which is essential for the survival of Trypanosoma brucei, the parasite that causes African trypanosomiasis. Melarsomine inhibits this enzyme, leading to the death of the parasite. It is administered intravenously and can have serious side effects, including encephalopathy, which can be fatal. Melarsomine is the only drug available for treating late-stage African trypanosomiasis, and it is used as a last resort due to its toxicity. Its importance stems from the lack of effective alternative treatments for late-stage disease. Research into melarsomine is driven by the need to develop safer and more effective drugs for African trypanosomiasis, a neglected tropical disease that affects millions of people in sub-Saharan Africa.'

melarsomine: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65962
CHEMBL ID1650564
SCHEMBL ID204211
MeSH IDM0205183

Synonyms (31)

Synonym
bis(2-aminoethyl) p-((4,6-diamino-s-triazin-2-yl)amino)dithiobenzenearsonite
melarsomine
melarsominum [inn-latin]
melarsomine [inn]
melarsomina [inn-spanish]
2-n-[4-[bis(2-aminoethylsulfanyl)arsanyl]phenyl]-1,3,5-triazine-2,4,6-triamine
128470-15-5
melarsomine (inn)
D08168
CHEMBL1650564
melarsominum
unii-374gj0s41a
arsonodithious acid, as-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)-, bis(2-aminoethyl) ester
melarsomina
374gj0s41a ,
M-1160
melarsomine [mi]
melarsomine [mart.]
melarsamin
bdbm50421414
SCHEMBL204211
NCGC00261972-01
DTXSID40155907 ,
Q15409394
CS-0148512
HY-138502
dtxcid8078398
melarsomina (inn-spanish)
melarsomine (mart.)
melarsominum (inn-latin)
AKOS040756618

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Following randomised trypanocidal treatment (diminazene diaceturate, melarsomine dihydrochloride or isometamidium chloride), animals were observed for immediate adverse drug reactions and follow-up assessment was performed at 1 and 2 weeks."( Safety and efficacy of three trypanocides in confirmed field cases of trypanosomiasis in working equines in The Gambia: a prospective, randomised, non-inferiority trial.
Jallow, S; Raftery, AG; Rodgers, J; Sutton, DGM, 2019
)
0.75

Dosage Studied

Ten falcons treated with melarsomine (Cymelarsan) at a dosage of 0.7%) out of 1,706 captive falcons examined between May 2003 and April 2005.

ExcerptRelevanceReference
" Cumulative dose-response relations to norepinephrine, nitroglycerin, and methacholine were determined."( Effect of arsenical drugs on in vitro vascular responses of pulmonary artery from heartworm-infected dogs.
Bell, TG; Kaiser, L; Maksimowich, DS; Williams, JF, 1997
)
0.3
" We recommend that veterinarians prescribe the recommended 10 mg/kg doxycycline for canine heartworm treatment and reduce the dosage to 5 mg/kg in cases of severe gastrointestinal side effects in order to improve owner compliance in administration of medications."( Efficacy and side effects of doxycycline versus minocycline in the three-dose melarsomine canine adulticidal heartworm treatment protocol.
Bradner, JL; Day, KM; Dzimianski, MT; Moorhead, AR; Savadelis, MD; Wolstenholme, AJ, 2018
)
0.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency5.01190.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID565600Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.03125 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID565598Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as complete cure from microbial infection at 0.0625 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID636823Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1/Colombia infected in human A+ve erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake preincubated for 24 hrs prior to [G-3H]hypoxanthine addition measured after 12011Journal of natural products, Oct-28, Volume: 74, Issue:10
Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark.
AID636825Antitrypanosomal activity against Trypanosoma brucei brucei2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark.
AID565597Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.125 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID565599Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.0625 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID636824Antileishmanial activity against Leishmania donovani MHOM/ET/L82/LV9 promastigotes after 3 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark.
AID565596Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as complete cure from microbial infection at 0.125 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID636826Cytotoxicity against african green monkey Vero cells2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark.
AID34012Compound was tested for inhibition of Adenosine transporter P2 type by using [2-3H]adenosine as radioligand in Trypanosoma equiperdum2000Bioorganic & medicinal chemistry letters, Jun-19, Volume: 10, Issue:12
Synthesis and uptake of nitric oxide-releasing drugs by the P2 nucleoside transporter in Trypanosoma equiperdum.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (44)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's6 (13.64)18.2507
2000's16 (36.36)29.6817
2010's18 (40.91)24.3611
2020's4 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 50.76

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index50.76 (24.57)
Research Supply Index3.97 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index89.45 (26.88)
Search Engine Supply Index2.28 (0.95)

This Compound (50.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (8.33%)5.53%
Reviews2 (4.17%)6.00%
Case Studies8 (16.67%)4.05%
Observational0 (0.00%)0.25%
Other34 (70.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]