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naftidrofuryl 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1870 | 31329-57-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A drug used in the management of peripheral and cerebral vascular disorders. It is claimed to enhance cellular oxidative capacity and to be a spasmolytic. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1310) It may also be an antagonist at 5HT-2 serotonin receptors.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.98 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 10.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.20 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.35 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 30 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.951 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.746 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 33.651 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 64.121 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 7.550 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 9.300 | % | High | 1 |
| herg | hERG pIC50 | 5.679 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 116.413 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 271.644 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 4.560 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,TEK | 25 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,PDK4 | 4 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.904 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 169.434 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 15.370 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.913 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 20.980 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 283.792 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 29.230 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 14.860 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 776.247 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Renal cell carcinoma | 71.53 | 62.98 | 12 | 262 | 3839 | 90624334 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Acute kidney injury | 75.00 | 42.29 | 60 | 1206 | 635370 | 109952663 |
| Hyperkalaemia | 49.03 | 42.29 | 26 | 1240 | 135770 | 110452263 |
| Lactic acidosis | 48.98 | 42.29 | 23 | 1243 | 92788 | 110495245 |
| Renal cell carcinoma | 47.37 | 42.29 | 12 | 1254 | 7518 | 110580515 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C04AX21 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Other peripheral vasodilators |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C04AX Other peripheral vasodilators 16 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Cerebrovascular disease | indication | 62914000 | DOID:6713 |
| Chronic Occlusive Peripheral Arterial Disease | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.43 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.82 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D05107 | KEGG_DRUG |
| 3200-06-4 | SECONDARY_CAS_RN |
| C0027329 | UMLSCUI |
| CHEBI:749811 | CHEBI |
| CHEMBL1439099 | ChEMBL_ID |
| CHEMBL1620794 | ChEMBL_ID |
| CHEMBL1443491 | ChEMBL_ID |
| DB13588 | DRUGBANK_ID |
| 2177 | INN_ID |
| 42H8PQ0NMJ | UNII |
| 4417 | PUBCHEM_CID |
| 7236 | RXNORM |
| 003746 | NDDF |
| 003776 | NDDF |
| 006857 | NDDF |
| 006858 | NDDF |
| 350627007 | SNOMEDCT_US |
| 395807000 | SNOMEDCT_US |
| 395992001 | SNOMEDCT_US |
| D009257 | MESH_DESCRIPTOR_UI |
Pharmaceutical products:
None