BALOFLOXACIN

Details

Stereochemistry	RACEMIC
Molecular Formula	C20H24FN3O4
Molecular Weight	389.4207
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CNC1CCCN(C1)C2=C(F)C=C3C(=O)C(=CN(C4CC4)C3=C2OC)C(O)=O

InChI

InChIKey=MGQLHRYJBWGORO-UHFFFAOYSA-N

InChI=1S/C20H24FN3O4/c1-22-11-4-3-7-23(9-11)17-15(21)8-13-16(19(17)28-2)24(12-5-6-12)10-14(18(13)25)20(26)27/h8,10-12,22H,3-7,9H2,1-2H3,(H,26,27)

HIDE SMILES / InChI

Molecular Formula	C20H24FN3O4
Molecular Weight	389.4207
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.tabletwise.com/baloxin-tablet
Curator's Comment: description was created based on several sources, including: https://www.medicineindia.org/pharmacology-for-generic/2923/balofloxacin http://www.ajptr.com/archive/volume-2/february-2012-issue-1/article-92.html

Balofloxacin (Q-35), is an orally active fluoroquinolone antibiotic. It has been developed for the treatment of urinary tract infection. The bactericidal action of Balofloxacin results from interference with the enqyme DNA gyrase which is needed for the synthesis of bacterial DNA. Balofloxacin is efficacious against Gram-negative bacteria. It also has enhanced activity against Gram positive bacteria, including MRSA and Streptococcus pneumoniae. Side effects of Balofloxacin are: sensitivity to light, abdominal pain, nausea, heartburn, urticarial, irritation when applied locally. Balofloxacin may interact with the following medicines and salts: antacids, non-steroidal anti-inflammatory drug, quinolones, theophylline.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial DNA gyrase 66 Target ID: CHEMBL2311224 Sources: http://www.ncbi.nlm.nih.gov/pubmed/8000379	Inhibitor 8504
Topoisomerase IV subunit A 7 Target ID: CHEMBL1895 Sources: http://www.ncbi.nlm.nih.gov/pubmed/19478540	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Urinary tract infections 207 Sources: https://www.medchemexpress.com/DataSheet/balofloxacin.html https://www.ncbi.nlm.nih.gov/pubmed/12669387	Curative	Approved 8583	Q-Roxin Approved Use Treatment of uncomplicated urinary tract infections Launch Date 2000
Respiratory tract infections 85 Sources: https://www.medchemexpress.com/DataSheet/balofloxacin.html	Curative	Phase II 1147	Unknown Approved Use Unknown
Infective ophthalmitis 2 Sources: https://www.1mg.com/generics/balofloxacin-209419	Curative	Approved 8583	Barofloxacin Approved Use Barofloxacin is a quinolone antibiotic, prescribed for the treatment of infective ophthalmitis.
Skin infections 59 Sources: https://www.1mg.com/generics/balofloxacin-209419	Curative	Approved 8583	Balofloxacin Approved Use Barofloxacin is a quinolone antibiotic, prescribed for the treatment of skin infections.

C_max

Value	Dose	Analyte	Population
1.39 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.89 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
2.09 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.46 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
2.31 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.73 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1.05 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.99 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.64 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1.07 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.72 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9124849/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
2.17 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9124849/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
7.41 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.86 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
13.21 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
15.91 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
18.66 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
19.67 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
5.53 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6.56 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
22.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9124849/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
17.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9124849/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
7.57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.94 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
9.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.65 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
6.66 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.16 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
7.67 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.02 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
7.72 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
7.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17161665/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9124849/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
7.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9124849/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BALOFLOXACIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

Doses

Dose	Population	Adverse events
200 mg single, oral Studied dose Dose: 200 mg Route: oral Route: single Dose: 200 mg Sources: https://pubmed.ncbi.nlm.nih.gov/9124849/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/9124849/	Sources: https://pubmed.ncbi.nlm.nih.gov/9124849/

PubMed

Title	Date	PubMed
Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.	2010-08	20493593
Aquatic photochemistry of fluoroquinolone antibiotics: kinetics, pathways, and multivariate effects of main water constituents.	2010-04-01	20205456
Gatifloxacin, moxifloxacin, and balofloxacin resistance due to mutations in the gyrA and parC genes of Staphylococcus epidermidis strains isolated from patients with endophthalmitis, corneal ulcers and conjunctivitis.	2009	19478540
Ethyl 1-cyclo-propyl-6,7-difluoro-8-meth-oxy-4-oxo-1,4-dihydro-quinoline-3-carboxyl-ate.	2008-10-31	21581071
[Synthesis and antibacterial activity of 7-(3-amino-4-alkoxyimino-1 -piperidyl) -quinolones].	2008-08	18956774
[Determination of balofloxacin in human plasma by HPLC with solid-phase extraction].	2007-11	18257322
High performance liquid chromatography-electrospray ionization mass spectrometric determination of balofloxacin in human plasma and its pharmacokinetics.	2007-05-01	17161665
[Studies on the reaction of balofloxacin with bovine serum albumin].	2006-08	17058955
Electrophysiological safety of novel fluoroquinolone antibiotic agents gemifloxacin and balofloxacin.	2006	16777708
[Interaction between balofloxacin and DNA and the influence of Mg2+ on the interaction].	2005-07	16196277
Balofloxacin Choongwae.	2003-02	12669387
[In vitro antimycobacterial activities of a new quinolone, balofloxacin].	2001-01	11211780
History of quinolones and their side effects.	2001	11549783
[In vitro anti-MAC activities of new quinolones in focus (2)].	1996-09	8999137
[Determination of antimycobacterial activities of fluoroquinolones against clinical isolates of Mycobacterium tuberculosis: comparative determination with egg-based Ogawa and agar-based Middlebrook 7H10 media].	1996-08	8831190

Patents

Sample Use Guides

In Vivo Use Guide

100 to 400 mg once or twice daily.

Route of Administration: Oral

In Vitro Use Guide

MIC90 of Balofloxacin against clinical isolates of Staphylococcus aureus, methicillin-resistant staphylococcus aureus (MRSA), Staphylococcus epidermidis, Streptococcus pneumoniae, and Streptococcus pyogenes is 6,25 ug/ml.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 06:53:37 GMT 2025` Edited by `admin` on `Wed Apr 02 06:53:37 GMT 2025`
Record UNII	Q022B63JPM
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BALOFLOXACIN [MI]

Preferred Name

English

BALOFLOXACIN

Official Name

English

(±)-1-CYCLOPROPYL-6-FLUORO-1,4-DIHYDRO-8-METHOXY-7-(3-(METHYLAMINO)PIPERIDINO)-4-OXO-3-QUINOLINECARBOXYLIC ACID

Systematic Name

English

BALOFLOXACIN [MART.]

Common Name

English

balofloxacin [INN]

Common Name

English

Balofloxacin [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C795