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cinoxacin 🐶 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 | 657 | 28657-80-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Synthetic antimicrobial related to OXOLINIC ACID and NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 63.69 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 72.50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.943 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.446 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 16.672 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.954 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 38.300 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 38.090 | % | High | 1 |
| herg | hERG pIC50 | 4.271 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.358 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.162 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 14.090 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,MAP3K21,MAP3K7,MAPK7,MTOR,NTRK2,PDK1,PDK2,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1 | 39 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,DYRK1B,EIF2AK3,GRK2,MAP2K6,MAPK7,PIK3CD,PRKDC,STK33,TTK | 12 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.864 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 7.112 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 32.720 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.767 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 22.110 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.360 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 92.020 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 6.400 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 974.990 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 13, 1980 | FDA | LILLY |
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 | J01MB06 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Other quinolones |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
Related Drugs by ATC class:
J01MB Other quinolones 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Urinary tract infectious disease | indication | 68566005 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.94 | acidic |
| pKa2 | 3.27 | Basic |
| pKa3 | 0.83 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Carbonic anhydrase 2 | Enzyme | IC50 | 4.08 | WOMBAT-PK | |||||
| DNA gyrase | Enzyme | INHIBITOR | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019087 | VUID |
| N0000147347 | NUI |
| D00872 | KEGG_DRUG |
| 151514 | RXNORM |
| C0008806 | UMLSCUI |
| CHEBI:3716 | CHEBI |
| CHEMBL1208 | ChEMBL_ID |
| DB00827 | DRUGBANK_ID |
| D002937 | MESH_DESCRIPTOR_UI |
| 2762 | PUBCHEM_CID |
| 12401 | IUPHAR_LIGAND_ID |
| 3513 | INN_ID |
| LMK22VUH23 | UNII |
| 106 | MMSL |
| 109 | MMSL |
| 4450 | MMSL |
| d01129 | MMSL |
| 002865 | NDDF |
| 387549004 | SNOMEDCT_US |
| 96081007 | SNOMEDCT_US |
| 4019087 | VANDF |
Pharmaceutical products:
None