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brodimoprim 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antimicrobials, dihydrofolate reductase (DHFR) inhibitors, trimethoprim analogues | 398 | 56518-41-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
inhibits dihydrofolate reductase
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 9.27 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 85 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKDC,TEK | 22 | |||
| kinase-selectivity-class | AXL,EIF2AK3,PIK3CD | 3 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 2.223 | High | 0.81 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 0.81 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.028 | % | High | 0.81 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1993 | YEAR INTRODUCED |
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 | J01EA02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Trimethoprim and derivatives |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D005493 | Folic Acid Antagonists |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:50683 | EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
Related Drugs by ATC class:
J01EA Trimethoprim and derivatives 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.01 | Basic |
| pKa2 | 0.6 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Bifunctional dihydrofolate reductase-thymidylate synthase | Enzyme | IC50 | 7.77 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | IC50 | 7.51 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | IC50 | 7.82 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 8.18 | WOMBAT-PK | |||||
| Dihydrofolate reductase | Enzyme | Ki | 7.95 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 4.54 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | IC50 | 8.53 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 8.18 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D07238 | KEGG_DRUG |
| 19727 | RXNORM |
| C0054084 | UMLSCUI |
| CHEBI:131726 | CHEBI |
| CHEMBL31891 | ChEMBL_ID |
| DB13795 | DRUGBANK_ID |
| C037079 | MESH_SUPPLEMENTAL_RECORD_UI |
| 68760 | PUBCHEM_CID |
| 12325 | IUPHAR_LIGAND_ID |
| 4910 | INN_ID |
| V1YC7T6LLI | UNII |
| 006013 | NDDF |
Pharmaceutical products:
None