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mebendazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anthelminthics, tiabendazole derivatives | 1641 | 31431-39-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 22 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 15 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.09 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.10 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.756 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.839 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 80.168 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 22.751 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 13.410 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 26.730 | % | High | 1 |
| herg | hERG pIC50 | 4.296 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 12.735 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 23.550 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 7.170 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,IRAK1,ITK,JAK1,JAK2,KIT,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP4K1,MAP4K3,MAPK10,MAPK7,MARK4,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,TEK,TNIK,TTK,ULK1 | 50 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,CAMK2D,CDK9,CSF1R,DDR1,DYRK1B,FLT3,JAK1,MAP2K6,MAP3K1,MAP3K21,MAPK7,MARK4,PDK1,PDK4,PIK3CD,SIK2,SIK3,STK33 | 23 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.581 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 62.087 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 10.670 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.312 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 19.750 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 30.130 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 72.080 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 7.960 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 5.741 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 28, 1974 | FDA |
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 |
|---|---|---|---|---|---|---|
| Exposure during pregnancy | 106.06 | 43.01 | 41 | 423 | 238369 | 90389614 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Foetal exposure during pregnancy | 69.44 | 50.44 | 19 | 155 | 47292 | 42573869 |
| Foetal megacystis | 53.32 | 50.44 | 6 | 168 | 70 | 42621091 |
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 |
|---|---|---|---|---|---|---|
| Exposure during pregnancy | 60.65 | 42.60 | 24 | 468 | 167400 | 110421407 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | P02CA01 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTHELMINTICS ANTINEMATODAL AGENTS Benzimidazole derivatives |
| ATC | P02CA51 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTHELMINTICS ANTINEMATODAL AGENTS Benzimidazole derivatives |
| FDA EPC | N0000175481 | Anthelmintic |
| MeSH PA | D000871 | Anthelmintics |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000969 | Antinematodal Agents |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D050256 | Antimitotic Agents |
| MeSH PA | D050257 | Tubulin Modulators |
| CHEBI has role | CHEBI:35443 | anthelminthic drug |
| CHEBI has role | CHEBI:35444 | antinematodal drug |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:60832 | tubulin modulator |
| CHEBI has role | CHEBI:61951 | microtubule-destabilising agent |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
Related Drugs by ATC class:
P02CA Benzimidazole derivatives 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ascariasis | indication | 2435008 | DOID:456 |
| Trichuriasis | indication | 3752003 | |
| Enterobiasis | indication | 266162007 | |
| Ancylostoma Duodenale Infection | indication | ||
| Necator Americanus Infection | indication | ||
| Infection by Gnathostoma | off-label use | 44086001 | DOID:11379 |
| Capillaria infection | off-label use | 52979002 | DOID:12474 |
| Echinococcus granulosus infection | off-label use | 75006000 | DOID:1495 |
| Echinococcus multilocularis | off-label use | 86648009 | |
| Infection by larvae of Trichinella spiralis | off-label use | 88264003 | |
| Angiostrongyliasis due to Angiostrongylus cantonensis | off-label use | ||
| Angiostrongyliasis due to Angiostrongylus costaricensis | off-label use | ||
| Disease of liver | contraindication | 235856003 | DOID:409 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Dogs | Treatment of infections with roundworms, Toxocara canis | Indication |
| Dogs | Treatment of infections with hookworms, Ancylostoma caninum | Indication |
| Dogs | Treatment of infections with Uncinaria stenocephala | Indication |
| Dogs | Treatment of infections with whipworms, Trichuris vulpis | Indication |
| Dogs | Treatment of infections with tapeworms, Taenia pisiformis | Indication |
| Horses | Treatment of infections caused by large roundworms, Parascaris equorum | Indication |
| Horses | Treatment of infections caused by large strongyles, Strongylus edentatus | Indication |
| Horses | Treatment of infections caused by large strongyles, S equinus | Indication |
| Horses | Treatment of infections caused by large strongyles, S vulgaris | Indication |
| Horses | Treatment of infections caused by small strongyles | Indication |
| Horses | Treatment of infections caused by 4th larval stage pinworms, Oxyuris equi | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Telmin Equine Wormer | Intervet Inc. | 1 |
| Telmin Syringe Formula | Intervet Inc. | 1 |
| Telmin B Equine Wormer | Intervet Inc. | 2 |
| Telmintic Powder | Intervet Inc. | 1 |
| Telmin | Intervet Inc. | 1 |
| Telmin B Paste | Intervet Inc. | 2 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.61 | acidic |
| pKa2 | 13.2 | acidic |
| pKa3 | 2.93 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase ABL1 | Kinase | Ki | 5.34 | CHEMBL | |||||
| Vascular endothelial growth factor receptor 2 | Kinase | IC50 | 5.44 | CHEMBL | |||||
| Tubulin | Structural | INHIBITOR | CHEMBL | CHEMBL | |||||
| Tubulin | Structural | INHIBITOR | CHEMBL | CHEMBL | |||||
| Calmodulin-domain protein kinase 1 | Kinase | IC50 | 6.17 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019270 | VUID |
| N0000147469 | NUI |
| D00368 | KEGG_DRUG |
| 4019270 | VANDF |
| C0025023 | UMLSCUI |
| CHEBI:6704 | CHEBI |
| V95 | PDB_CHEM_ID |
| CHEMBL685 | ChEMBL_ID |
| DB00643 | DRUGBANK_ID |
| D008463 | MESH_DESCRIPTOR_UI |
| 4030 | PUBCHEM_CID |
| 13427 | IUPHAR_LIGAND_ID |
| 2942 | INN_ID |
| 81G6I5V05I | UNII |
| 202972 | RXNORM |
| 1672 | MMSL |
| 5026 | MMSL |
| 789 | MMSL |
| d00154 | MMSL |
| 002987 | NDDF |
| 387311004 | SNOMEDCT_US |
| 56059005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VERMOX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50458-675 | TABLET, CHEWABLE | 500 mg | ORAL | NDA | 28 sections |
| MEBENDAZOLE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-3732 | TABLET, CHEWABLE | 100 mg | ORAL | ANDA | 21 sections |
| Emverm | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-669 | TABLET, CHEWABLE | 100 mg | ORAL | ANDA | 26 sections |