sitafloxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 2449 127254-12-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • DU-6859a
  • sitafloxacin sesquihydrate
  • sitafloxacin
  • gracevit
  • sitafloxacin hydrate
  • DU-6859
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.
  • Molecular weight: 409.82
  • Formula: C19H18ClF2N3O3
  • CLOGP: 0.59
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 86.87
  • ALOGS: -3.87
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
Jan. 25, 2008 PMDA Daiichi Sankyo

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:

SourceCodeDescription
ATC J01MA21 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
QUINOLONE ANTIBACTERIALS
Fluoroquinolones
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D059005 Topoisomerase II Inhibitors
MeSH PA D059003 Topoisomerase Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
DNA gyrase subunit B Enzyme WOMBAT-PK
DNA topoisomerase 4 subunit A Enzyme WOMBAT-PK

External reference:

IDSource
D02475 KEGG_DRUG
C0171447 UMLSCUI
CHEBI:4304 CHEBI
CHEMBL3989504 ChEMBL_ID
CHEMBL108821 ChEMBL_ID
DB13261 DRUGBANK_ID
C076246 MESH_SUPPLEMENTAL_RECORD_UI
461399 PUBCHEM_CID
11040 IUPHAR_LIGAND_ID
9TD681796G UNII
163253-35-8 SECONDARY_CAS_RN

Pharmaceutical products:

None