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grepafloxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, nalidixic acid derivatives | 1330 | 119914-60-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 70 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| CL (Clearance) | 5.90 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.82 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 9.20 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 | 0.333 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.162 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 11.194 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.211 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 59.390 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 64.960 | % | High | 1 |
| herg | hERG pIC50 | 4.545 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.102 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.013 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 56.410 | % | High | 1 |
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| kinase-selectivity-class | AXL,DYRK1B,EIF2AK3,EPHB4,GRK2,MAPK7,PDK4,PIK3CB,PRKDC,STK33,SYK,TEK,TGFBR1,TTK | 14 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 12.023 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 3.148 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 53.390 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 23.121 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 62.890 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.077 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.361 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 83.460 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 40.010 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 801.678 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 6, 1997 | FDA | OTSUKA |
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 | J01MA11 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059003 | Topoisomerase Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
Related Drugs by ATC class:
J01MA Fluoroquinolones 22 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Gonorrhea | indication | 15628003 | DOID:7551 |
| Acute gonococcal cervicitis | indication | 20943002 | DOID:10615 |
| Pneumonia due to Streptococcus | indication | 34020007 | |
| Pneumonia due to Mycoplasma pneumoniae | indication | 46970008 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Urethritis due to Chlamydia trachomatis | indication | 179101003 | |
| Acute Moraxella catarrhalis bronchitis | indication | 195722003 | |
| Acute bacterial bronchitis | indication | 233598009 | |
| Haemophilus Influenzae Bronchitis | indication | ||
| Moraxella Catarrhalis Pneumonia | indication | ||
| Chlamydia Cervicitis | indication | ||
| Streptococcus Pneumoniae Bronchitis | 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 | 6.14 | acidic |
| pKa2 | 8.66 | Basic |
| pKa3 | 1.49 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.30 | CHEMBL | |||||
| DNA topoisomerase 4 | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| DNA gyrase | Enzyme | INHIBITOR | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4024097 | VUID |
| N0000022102 | NUI |
| D02178 | KEGG_DRUG |
| 4021079 | VANDF |
| 4024097 | VANDF |
| C0287721 | UMLSCUI |
| CHEBI:5543 | CHEBI |
| CHEMBL583 | ChEMBL_ID |
| DB00365 | DRUGBANK_ID |
| CHEMBL1200393 | ChEMBL_ID |
| C075375 | MESH_SUPPLEMENTAL_RECORD_UI |
| 72474 | PUBCHEM_CID |
| 10818 | IUPHAR_LIGAND_ID |
| 7024 | INN_ID |
| 161967-81-3 | SECONDARY_CAS_RN |
| L1M1U2HC31 | UNII |
| 236862 | RXNORM |
| 4802 | MMSL |
| d04246 | MMSL |
| 007022 | NDDF |
| 007023 | NDDF |
| 108679003 | SNOMEDCT_US |
| 386892006 | SNOMEDCT_US |
| 719852005 | SNOMEDCT_US |
Pharmaceutical products:
None