suramin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2966 | 145-63-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.27 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
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:
| Source | Code | Description |
|---|---|---|
| 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 drugs |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:36335 | trypanocidal drugs |
| CHEBI has role | CHEBI:37700 | protein kinase C inhibitors |
| CHEBI has role | CHEBI:38999 | GABA-gated chloride channel antagonists |
| CHEBI has role | CHEBI:48422 | angiogenesis antagonist |
| CHEBI has role | CHEBI:65259 | GABA antagonists |
| CHEBI has role | CHEBI:67114 | ryanodine receptor activators |
| CHEBI has role | CHEBI:68494 | apoptosis inhibitors |
| CHEBI has role | CHEBI:91079 | P2 antagonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| African trypanosomiasis | indication | 27031003 | DOID:10112 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 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 | |||||
| Signal transducer and activator of transcription 1-alpha/beta | Unclassified | IC50 | 5.04 | CHEMBL | |||||
| Signal transducer and activator of transcription 5A | Unclassified | IC50 | 5.03 | CHEMBL | |||||
| Signal transducer and activator of transcription 5B | Unclassified | IC50 | 4.98 | 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 |
External reference:
| ID | Source |
|---|---|
| N0000167387 | NUI |
| D00808 | KEGG_DRUG |
| 129-46-4 | SECONDARY_CAS_RN |
| C0038880 | UMLSCUI |
| CHEBI:45906 | CHEBI |
| SVR | PDB_CHEM_ID |
| CHEMBL265502 | ChEMBL_ID |
| D013498 | MESH_DESCRIPTOR_UI |
| DB04786 | DRUGBANK_ID |
| 1728 | IUPHAR_LIGAND_ID |
| 6032D45BEM | UNII |
| 5361 | PUBCHEM_CID |
| 10256 | RXNORM |
| 002969 | NDDF |
| 004968 | NDDF |
| 67928003 | SNOMEDCT_US |
| 714082002 | SNOMEDCT_US |
| 714537005 | SNOMEDCT_US |
| CHEMBL413376 | ChEMBL_ID |
| 2899 | INN_ID |
Pharmaceutical products:
None