suramin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

ADMET properties:

PropertyValueReference
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.54 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.01 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1200 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

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:35610 antineoplastic agent
CHEBI has role CHEBI:36335 trypanocidal drug
CHEBI has role CHEBI:37700 EC 2.7.11.13 (protein kinase C) inhibitor
CHEBI has role CHEBI:38999 GABA-gated chloride channel antagonist
CHEBI has role CHEBI:48422 angiogenesis inhibitor
CHEBI has role CHEBI:65259 GABA antagonist
CHEBI has role CHEBI:67114 ryanodine receptor agonist
CHEBI has role CHEBI:68494 apoptosis inhibitor
CHEBI has role CHEBI:70868 antileishmanial agent
CHEBI has role CHEBI:91079 purinergic receptor P2 antagonist
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

P01CX Other agents against leishmaniasis and trypanosomiasis 3 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
African trypanosomiasis indication 27031003 DOID:10112




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.86 acidic
pKa2 9.47 acidic
pKa3 12.22 acidic
pKa4 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
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 Enzyme Ki 6.58 CHEMBL
Tyrosine-protein phosphatase non-receptor type 1 Enzyme IC50 5.85 CHEMBL
P2X purinoceptor 1 Ion channel IC50 5.37 CHEMBL
NAD-dependent protein deacetylase sirtuin-1 Enzyme IC50 6.52 CHEMBL
P2Y purinoceptor 6 GPCR ANTAGONIST Kb 4 IUPHAR
P2Y purinoceptor 1 GPCR ANTAGONIST Ki 5.30 IUPHAR
NAD-dependent protein deacetylase sirtuin-2 Enzyme IC50 5.96 CHEMBL
P2Y purinoceptor 2 GPCR ANTAGONIST IC50 4.30 IUPHAR
P2Y purinoceptor 11 GPCR ANTAGONIST IC50 6 IUPHAR
Protein arginine N-methyltransferase 1 Enzyme IC50 5.27 CHEMBL
P2Y purinoceptor 13 GPCR ANTAGONIST IC50 5.60 IUPHAR
DNA-dependent protein kinase catalytic subunit Kinase IC50 5.77 CHEMBL
P2X purinoceptor 4 Ion channel Ki 6.75 PDSP
Protein kinase C (PKC) Kinase IC50 4.54 CHEMBL
P2X purinoceptor 3 Ion channel Ki 5.96 PDSP
NAD-dependent protein deacylase sirtuin-5, mitochondrial Enzyme IC50 4.85 CHEMBL
Heparanase Enzyme IC50 4.58 CHEMBL
Signal transducer and activator of transcription 1-alpha/beta Transcription factor IC50 5.04 CHEMBL
Signal transducer and activator of transcription 5A Transcription factor IC50 5.03 CHEMBL
Signal transducer and activator of transcription 5B Transcription factor IC50 4.98 CHEMBL
P2X purinoceptor 7 Ion channel IC50 4.48 CHEMBL
Pyruvate kinase PKLR Enzyme Ki 5.96 CHEMBL
Pyruvate kinase PKM Enzyme Ki 5 CHEMBL
Protein argonaute-2 Enzyme IC50 6.16 CHEMBL
Reverse transcriptase/RNaseH Enzyme IC50 5.03 CHEMBL
RmtA Enzyme IC50 5.23 CHEMBL
ATP-dependent 6-phosphofructokinase Kinase IC50 5.52 CHEMBL
Nucleoside triphosphate diphosphohydrolase 3 Enzyme Ki 4.90 CHEMBL
Ectonucleoside triphosphate diphosphohydrolase 2 Enzyme Ki 4.18 CHEMBL
P2X purinoceptor 3 Ion channel ANTAGONIST IC50 5.52 IUPHAR
P2X purinoceptor 2 Ion channel ANTAGONIST IC50 4.98 IUPHAR
P2X purinoceptor 1 Ion channel ANTAGONIST IC50 6 IUPHAR
P2X purinoceptor 5 Ion channel ANTAGONIST IC50 5.40 IUPHAR
Replicase polyprotein 1ab Enzyme IC50 6.58 CHEMBL
Genome polyprotein Polyprotein EC50 5.71 CHEMBL
NAD-dependent protein deacetylase Enzyme IC50 5.16 CHEMBL

External reference:

IDSource
N0000167387 NUI
D00808 KEGG_DRUG
C0038880 UMLSCUI
CHEBI:45906 CHEBI
SVR PDB_CHEM_ID
CHEMBL265502 ChEMBL_ID
CHEMBL413376 ChEMBL_ID
D013498 MESH_DESCRIPTOR_UI
DB04786 DRUGBANK_ID
1728 IUPHAR_LIGAND_ID
129-46-4 SECONDARY_CAS_RN
6032D45BEM UNII
5361 PUBCHEM_CID
10256 RXNORM
002969 NDDF
004968 NDDF
67928003 SNOMEDCT_US
714082002 SNOMEDCT_US
714537005 SNOMEDCT_US
2899 INN_ID
6032D45BEM INXIGHT DRUGS

Pharmaceutical products:

None