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

Stem definition	Drug id	CAS RN
antibacterials, nalidixic acid derivatives	1013	74011-58-8

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

enoxacin
enofloxacin
enofloxacine
enoksetin
enoxacine

A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.

Molecular weight: 320.32
Formula: C15H17FN4O3
CLOGP: -1.34
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 85.77
ALOGS: -2.47
ROTB: 3

Status: OFM

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

Drug dosage:

Dose	Unit	Route
0.80	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.60 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	45 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	62.44 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	87 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	2 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.80 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5.10 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 31, 1991	FDA

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	J01MA04	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones
CHEBI has role	CHEBI:36047	antibacterial drugs
CHEBI has role	CHEBI:59517	DNA synthesis inhibitors
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D065609	Cytochrome P-450 CYP1A2 Inhibitors
MeSH PA	D065607	Cytochrome P-450 Enzyme Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D065606	Metabolic Side Effects of Drugs and Substances
MeSH PA	D059005	Topoisomerase II Inhibitors
MeSH PA	D059003	Topoisomerase Inhibitors

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
Acute gonococcal urethritis	indication	29864006
Gonorrhea of rectum	indication	42746002
Urinary tract infectious disease	indication	68566005
Gonorrhea of pharynx	indication	74372003
Chancroid	off-label use	266143009	DOID:13778

🐶 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	8.63	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
V-type proton ATPase subunit B, brain isoform	Enzyme	P21281	VATB2_HUMAN		IC50	5		CHEMBL
RISC-loading complex subunit TARBP2	Unclassified	Q15633	TRBP2_HUMAN		Kd	7.03		CHEMBL
Topoisomerase IV	Enzyme		PARC_NEIGO Q5EP76_NEIGO	INHIBITOR				CHEMBL	CHEMBL
DNA gyrase	Enzyme		GYRB_NEIGO GYRA_NEIGO	INHIBITOR				CHEMBL	CHEMBL
DNA gyrase subunit A	Enzyme		GYRA_HAEIN					WOMBAT-PK

External reference:

ID	Source
4020144	VUID
N0000148115	NUI
D00310	KEGG_DRUG
4020144	VANDF
C0014310	UMLSCUI
CHEBI:157175	CHEBI
CHEMBL826	ChEMBL_ID
DB00467	DRUGBANK_ID
D015365	MESH_DESCRIPTOR_UI
3229	PUBCHEM_CID
8882	IUPHAR_LIGAND_ID
5351	INN_ID
325OGW249P	UNII
3925	RXNORM
4658	MMSL
d00099	MMSL
003660	NDDF
387550004	SNOMEDCT_US
96084004	SNOMEDCT_US

Pharmaceutical products:

None