suramin Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
2966 145-63-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • suramin
  • metaret
  • naganol
  • suramine
  • suramin sodium
  • suramin hexasodium
A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
  • Molecular weight: 1297.26
  • Formula: C51H40N6O23S6
  • CLOGP: -8.58
  • LIPINSKI: 3
  • HAC: 29
  • HDO: 12
  • TPSA: 483.75
  • ALOGS: -5.17
  • ROTB: 16

Drug dosage:

DoseUnitRoute
0.27 g P

Approvals:

None

FDA Adverse Event Reporting System

None

Pharmacologic Action:

SourceCodeDescription
ATC P01CX02 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTIPROTOZOALS
AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS
Other agents against leishmaniasis and trypanosomiasis
MeSH PA D000871 Anthelmintics
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000969 Antinematodal Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D000981 Antiprotozoal Agents
MeSH PA D014344 Trypanocidal Agents
CHEBI has role CHEBI:35444 antinematodal drug
CHEBI has role CHEBI:36335 trypanocidal drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
African trypanosomiasis indication 27031003 DOID:10112

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 -1.42 acidic
pKa2 -1.3 acidic
pKa3 -0.7 acidic
pKa4 8.86 acidic
pKa5 9.47 acidic
pKa6 12.22 acidic
pKa7 12.82 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
P2Y purinoceptor 11 GPCR ANTAGONIST IC50 6 IUPHAR
P2Y purinoceptor 13 GPCR ANTAGONIST IC50 5.60 IUPHAR
P2Y purinoceptor 1 GPCR ANTAGONIST Ki 5.30 IUPHAR
P2Y purinoceptor 2 GPCR ANTAGONIST IC50 4.30 IUPHAR
P2X purinoceptor 4 Ion channel Ki 6.75 PDSP
P2X purinoceptor 3 Ion channel Ki 5.96 PDSP
Protein kinase C (PKC) Kinase IC50 4.54 CHEMBL
DNA-dependent protein kinase catalytic subunit Kinase IC50 5.77 CHEMBL
NAD-dependent protein deacylase sirtuin-5, mitochondrial Enzyme IC50 4.85 CHEMBL
Protein arginine N-methyltransferase 1 Enzyme IC50 5.27 CHEMBL
NAD-dependent protein deacetylase sirtuin-2 Enzyme IC50 5.96 CHEMBL
NAD-dependent protein deacetylase sirtuin-1 Enzyme IC50 6.52 CHEMBL
P2Y purinoceptor 6 GPCR ANTAGONIST Kb 4 IUPHAR
Nucleoside triphosphate diphosphohydrolase 3 Unclassified Ki 4.90 CHEMBL
ATP-dependent 6-phosphofructokinase Kinase IC50 5.52 CHEMBL
RmtA Enzyme IC50 5.23 CHEMBL
Reverse transcriptase/RNaseH Enzyme IC50 5.03 CHEMBL
Ectonucleoside triphosphate diphosphohydrolase 2 Unclassified Ki 4.18 CHEMBL
P2X purinoceptor 1 Unclassified ANTAGONIST IC50 6 IUPHAR
P2X purinoceptor 2 Unclassified ANTAGONIST IC50 4.98 IUPHAR
P2X purinoceptor 3 Unclassified ANTAGONIST IC50 5.52 IUPHAR
P2X purinoceptor 5 Unclassified ANTAGONIST IC50 5.40 IUPHAR

External reference:

IDSource
1728 IUPHAR_LIGAND_ID
N0000167387 NUI
C0038880 UMLSCUI
D00808 KEGG_DRUG
CHEMBL265502 ChEMBL_ID
6032D45BEM UNII
CHEMBL413376 ChEMBL_ID
N0000167387 NDFRT
10256 RXNORM
004968 NDDF
714082002 SNOMEDCT_US
714537005 SNOMEDCT_US
2899 INN_ID
129-46-4 SECONDARY_CAS_RN
DB04786 DRUGBANK_ID
5361 PUBCHEM_CID
D013498 MESH_DESCRIPTOR_UI
CHEBI:45906 CHEBI
SVR PDB_CHEM_ID

Pharmaceutical products:

None