ozenoxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 5058 245765-41-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • xepi
  • ozenoxacin
  • zebiax
  • T-3912
  • T 3912
Ozenoxacin is a quinolone antimicrobial drug. The mechanism of action involves the inhibition of bacterial DNA replication enzymes, DNA gyrase A and topoisomerase IV. Ozenoxacin has been shown to be bactericidal against S. aureus and S. pyogenes organisms. Ozenoxacin is used as topical treatment for impetigo and other infectious dermatological conditions.
  • Molecular weight: 363.42
  • Formula: C21H21N3O3
  • CLOGP: 3.39
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 82.53
  • ALOGS: -3.55
  • ROTB: 4

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.627 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.881 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 80.538 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 7.482 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 7.840 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 17.550 % High 1
herg hERG pIC50 4.668 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.950 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 7.379 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 6.760 % High 1
kinase-safety-class ACVR2B,GRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKDC 9
kinase-selectivity-class ACVR2B,AXL,DYRK1B,EIF2AK3,GRK2,MAP2K6,MAPK7,PIK3CB,PIK3CD,PIK3CG,PRKDC,TGFBR1 12
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.518 High 1
mh-clint Mouse hepatocyte intrinsic clearance 12.246 High 1
mppb Mouse plasma protein binding (% unbound) 6.250 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 6.427 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 11.580 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.246 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 62.670 % High 1
rppb Rat plasma protein binding (% unbound) 2.700 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 46.452 uM High 1

Approvals:

DateAgencyCompanyOrphan
Dec. 11, 2017 FDA FERRER INTERNACIONAL S.A.
Sept. 28, 2015 PMDA Maruho Co., Ltd.

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 D06AX14 DERMATOLOGICALS
ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE
ANTIBIOTICS FOR TOPICAL USE
Other antibiotics for topical use
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
FDA CS M0023650 Quinolones
FDA EPC N0000175937 Quinolone Antimicrobial
CHEBI has role CHEBI:73336 vulnerary

Related Drugs by ATC class:

D06AX Other antibiotics for topical use 12 drugs

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

DiseaseRelationSNOMED_IDDOID
Acne vulgaris indication 88616000
Superficial bacterial infection of skin indication 275441009
Staphylococcal infection of skin indication 402938009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.46 acidic
pKa2 5.8 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1% XEPI LNHC N208945 Dec. 11, 2017 DISCN CREAM TOPICAL 9399014 Dec. 15, 2029 TREATMENT OF IMPETIGO DUE TO STAPHYLOCOCCUS AUREUS OR STREPTOCOCCUS PYOGENES
1% XEPI LNHC N208945 Dec. 11, 2017 DISCN CREAM TOPICAL 9180200 Jan. 29, 2032 TREATMENT OF IMPETIGO DUE TO STAPHYLOCOCCUS AUREUS OR STREPTOCOCCUS PYOGENES

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
V0LH498RFO UNII
D09544 KEGG_DRUG
4037917 VANDF
C2983945 UMLSCUI
CHEBI:136050 CHEBI
CHEMBL3990047 ChEMBL_ID
9863827 PUBCHEM_CID
DB12924 DRUGBANK_ID
8788 INN_ID
C000592413 MESH_SUPPLEMENTAL_RECORD_UI
10841 IUPHAR_LIGAND_ID
C464965 MESH_SUPPLEMENTAL_RECORD_UI
1994739 RXNORM
267098 MMSL
33338 MMSL
017429 NDDF
763879001 SNOMEDCT_US
763887000 SNOMEDCT_US

Pharmaceutical products:

None