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sitafloxacin 🐶 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 | 2449 | 127254-12-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Sitafloxacin hydrate is a fluoroquinolone antibiotic. It is indicated for the treatment of various infections such as respiratory infection, urologic infection, gynecologic infection, otorhinological infections, and dental infection.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 75 % | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 89 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.51 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 6.60 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 | -0.387 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 8.166 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.607 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 0.989 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 69.220 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 69.470 | % | High | 1 |
| herg | hERG pIC50 | 4.414 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.096 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.090 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 67.230 | % | High | 1 |
| kinase-safety-class | GRK2,PDK1,PDK2,PDK4 | 4 | |||
| kinase-selectivity-class | AXL,CDK9,DYRK1B,EIF2AK3,GRK2,MAPK7,PRKDC,STK33 | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.998 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.472 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 53.850 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 11.455 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 71.900 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.089 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.870 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 50.860 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 781.628 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 25, 2008 | PMDA | Daiichi Sankyo |
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 |
|---|---|---|---|---|---|---|
| Pneumatosis intestinalis | 207.68 | 52.68 | 29 | 204 | 3408 | 90624806 |
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 |
|---|---|---|---|---|---|---|
| Pneumatosis intestinalis | 168.82 | 44.41 | 29 | 396 | 8500 | 110580374 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01MA21 | 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:33231 | antitubercular 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 |
|---|---|---|---|
| Urinary tract infectious disease | indication | 68566005 | |
| Respiratory tract infection | indication | 275498002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.69 | acidic |
| pKa2 | 10.5 | Basic |
| pKa3 | 1.75 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| DNA gyrase subunit B | Enzyme | WOMBAT-PK | |||||||
| DNA topoisomerase 4 subunit A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D02475 | KEGG_DRUG |
| 163253-35-8 | SECONDARY_CAS_RN |
| C0171447 | UMLSCUI |
| CHEBI:4304 | CHEBI |
| CHEMBL3989504 | ChEMBL_ID |
| DB13261 | DRUGBANK_ID |
| C076246 | MESH_SUPPLEMENTAL_RECORD_UI |
| 461399 | PUBCHEM_CID |
| 11040 | IUPHAR_LIGAND_ID |
| 9TD681796G | UNII |
| 020099 | NDDF |
| CHEMBL108821 | ChEMBL_ID |
Pharmaceutical products:
None