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

Stem definition	Drug id	CAS RN
antibacterials, nalidixic acid derivatives	1330	119914-60-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

grepafloxacin hydrochloride hydrate
grepafloxacin
tomefloxacin
grepafloxacin hydrochloride
grepafloxacin HCl

Molecular weight: 359.40
Formula: C19H22FN3O3
CLOGP: 0.55
LIPINSKI: 0
HAC: 6
HDO: 2
TPSA: 72.88
ALOGS: -2.76
ROTB: 3

Status: OFM

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

Drug dosage:

Dose	Unit	Route
0.40	g	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	70 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	5.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.82 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	9.20 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 6, 1997	FDA	OTSUKA

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	J01MA11	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|

Disease	Relation	SNOMED_ID	DOID
Gonorrhea	indication	15628003	DOID:7551
Acute gonococcal cervicitis	indication	20943002	DOID:10615
Pneumonia due to Streptococcus	indication	34020007
Pneumonia due to Mycoplasma pneumoniae	indication	46970008
Haemophilus influenzae pneumonia	indication	70036007
Urethritis due to Chlamydia trachomatis	indication	179101003
Acute Moraxella catarrhalis bronchitis	indication	195722003
Acute bacterial bronchitis	indication	233598009
Haemophilus Influenzae Bronchitis	indication
Moraxella Catarrhalis Pneumonia	indication
Chlamydia Cervicitis	indication
Streptococcus Pneumoniae Bronchitis	indication

🐶 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	8.66	Basic
pKa3	1.49	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
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.30		CHEMBL
DNA topoisomerase 4	Enzyme		PARC_STRPN PARE_STRPN	INHIBITOR				CHEMBL	CHEMBL
DNA gyrase	Enzyme		GYRB_STRPN GYRA_STRPN	INHIBITOR				CHEMBL	CHEMBL

External reference:

ID	Source
4024097	VUID
N0000022102	NUI
D02178	KEGG_DRUG
161967-81-3	SECONDARY_CAS_RN
4021079	VANDF
4024097	VANDF
C0287721	UMLSCUI
CHEBI:5543	CHEBI
CHEMBL583	ChEMBL_ID
DB00365	DRUGBANK_ID
C075375	MESH_SUPPLEMENTAL_RECORD_UI
72474	PUBCHEM_CID
10818	IUPHAR_LIGAND_ID
7024	INN_ID
L1M1U2HC31	UNII
236862	RXNORM
4802	MMSL
d04246	MMSL
007022	NDDF
007023	NDDF
108679003	SNOMEDCT_US
386892006	SNOMEDCT_US
719852005	SNOMEDCT_US
CHEMBL1200393	ChEMBL_ID

Pharmaceutical products:

None