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Details

Stereochemistry RACEMIC
Molecular Formula C19H22FN3O3
Molecular Weight 359.3954
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GREPAFLOXACIN

SMILES

CC1CN(CCN1)c2cc3c(c(C)c2F)c(=O)c(cn3C4CC4)C(=O)O

InChI

InChIKey=AIJTTZAVMXIJGM-UHFFFAOYSA-N
InChI=1S/C19H22FN3O3/c1-10-8-22(6-5-21-10)15-7-14-16(11(2)17(15)20)18(24)13(19(25)26)9-23(14)12-3-4-12/h7,9-10,12,21H,3-6,8H2,1-2H3,(H,25,26)

HIDE SMILES / InChI

Molecular Formula C19H22FN3O3
Molecular Weight 359.3954
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment:: http://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20-695_Raxar_Pharma.pdf | https://www.drugbank.ca/drugs/DB00365

Grepafloxacin is a monofluorinated quinolone with a cyclopropyl group at position 1, a 3-methyl-1piperazinyl group at position 7 and a methyl substitution at the 5 position, that was synthesized by Otsuka in Japan. It exhibited in vitro activity against a wide variety of both Gram-positive and Gram-negative bacteria including anaerobic species. The compound was reported to have a broad spectrum of activity, particularly against pathogens responsible for community-acquired respiratory infections including those caused by beta-lactam and macrolide-resistant strains of Streptococcus pneumoniae and Haemophilus influenzae. Japanese researchers also reported that unlike other quinolones, grepafloxacin reached high levels in the bile and might also be useful in the treatment of biliary tract infection. Grepafloxacin was administered once daily and did not require dosage adjustment for renal insufficiency, but grepafloxacin tablets were contraindicated in patients with hepatic failure. Otsuka Pharmaceutical signed a licensing agreement for grepafloxacin with GlaxoSmithKline. According to this agreement, GlaxoSmithKline had marketing rights to grepafloxacin in Europe, USA, and certain other markets. Otsuka retained rights for Japan and some Asian countries

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
RAXAR

Approved Use

RAXAR Tablets are Indicated for treatment of adults with mild to moderate infections caused by susceptible strains of the designated microorganisms in the infections listed below: Acute Bacterial Exacerbations of Chronic Bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis. Community-acquired Pneumonia caused by Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, or Mycoplasma pneumonia. Uncomplicated Gonorrhea (urethral In males and endocervical and rectal in females) caused by Neissen'a gononrhoeae. Nongonococcal Urethritis and Cervicitis caused by Chlamydia trachomatis

Launch Date

878774400000
Curative
RAXAR

Approved Use

RAXAR Tablets are Indicated for treatment of adults with mild to moderate infections caused by susceptible strains of the designated microorganisms in the infections listed below: Acute Bacterial Exacerbations of Chronic Bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis. Community-acquired Pneumonia caused by Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, or Mycoplasma pneumonia. Uncomplicated Gonorrhea (urethral In males and endocervical and rectal in females) caused by Neissen'a gononrhoeae. Nongonococcal Urethritis and Cervicitis caused by Chlamydia trachomatis

Launch Date

878774400000
Curative
RAXAR

Approved Use

RAXAR Tablets are Indicated for treatment of adults with mild to moderate infections caused by susceptible strains of the designated microorganisms in the infections listed below: Acute Bacterial Exacerbations of Chronic Bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis. Community-acquired Pneumonia caused by Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, or Mycoplasma pneumonia. Uncomplicated Gonorrhea (urethral In males and endocervical and rectal in females) caused by Neissen'a gononrhoeae. Nongonococcal Urethritis and Cervicitis caused by Chlamydia trachomatis

Launch Date

878774400000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.43 mg/L
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.63 mg/L
800 mg 1 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
0.93 mg/L
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1.41 mg/L
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.26 mg/L
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
3.17 mg/L
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
0.47 mg/L
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
14.6 mg × h/L
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
32.2 mg × h/L
800 mg 1 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
11.35 mg × h/L
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
19.73 mg × h/L
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
27.69 mg × h/L
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
45.04 mg × h/L
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5.08 mg × h/L
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
11.68 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
12.67 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
12.25 h
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
11.68 h
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
10.14 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
50%
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
50%
800 mg 1 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
50%
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
50%
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
50%
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
50%
1200 mg single, oral
dose: 1200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
50%
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GREPAFLOXACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 47.7 years
Health Status: unhealthy
Age Group: 47.7 years
Sex: M+F
Sources:
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (3 patients)
Vomiting (1 patient)
Taste perversion (2 patients)
Dizziness (3 patients)
Diarrhea (2 patients)
Sources:
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 48.4 years
Health Status: unhealthy
Age Group: 48.4 years
Sex: M+F
Sources:
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (8 patients)
Vomiting (4 patients)
Taste perversion (5 patients)
Dizziness (3 patients)
Diarrhea (1 patient)
Sources:
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (1.2%)
Vomiting (1.2%)
Sources:
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Bad taste, Nausea...
AEs leading to
discontinuation/dose reduction:
Bad taste (0.3%)
Nausea (0.8%)
Vomiting (0.6%)
Headache (0.3%)
Dizziness (0.5%)
Rash (0.2%)
Tachycardia (<0.1%)
Sources:
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Bad taste, Nausea...
AEs leading to
discontinuation/dose reduction:
Bad taste (1%)
Nausea (2.6%)
Vomiting (1.4%)
Headache (0.6%)
Dizziness (0.6%)
Rash (0.6%)
Tachycardia (0.14%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Vomiting 1 patient
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 47.7 years
Health Status: unhealthy
Age Group: 47.7 years
Sex: M+F
Sources:
Diarrhea 2 patients
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 47.7 years
Health Status: unhealthy
Age Group: 47.7 years
Sex: M+F
Sources:
Taste perversion 2 patients
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 47.7 years
Health Status: unhealthy
Age Group: 47.7 years
Sex: M+F
Sources:
Dizziness 3 patients
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 47.7 years
Health Status: unhealthy
Age Group: 47.7 years
Sex: M+F
Sources:
Nausea 3 patients
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 47.7 years
Health Status: unhealthy
Age Group: 47.7 years
Sex: M+F
Sources:
Diarrhea 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 48.4 years
Health Status: unhealthy
Age Group: 48.4 years
Sex: M+F
Sources:
Dizziness 3 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 48.4 years
Health Status: unhealthy
Age Group: 48.4 years
Sex: M+F
Sources:
Vomiting 4 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 48.4 years
Health Status: unhealthy
Age Group: 48.4 years
Sex: M+F
Sources:
Taste perversion 5 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 48.4 years
Health Status: unhealthy
Age Group: 48.4 years
Sex: M+F
Sources:
Nausea 8 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 48.4 years
Health Status: unhealthy
Age Group: 48.4 years
Sex: M+F
Sources:
Nausea 1.2%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting 1.2%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Rash 0.2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Bad taste 0.3%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Headache 0.3%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dizziness 0.5%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting 0.6%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea 0.8%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Tachycardia <0.1%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Tachycardia 0.14%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dizziness 0.6%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Headache 0.6%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Rash 0.6%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Bad taste 1%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting 1.4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea 2.6%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as perpetrator​

Drug as perpetrator​

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
[In vitro anti-MAC activities of new quinolones in focus (2)].
1996 Sep
[In vitro anti-MAC activities of new quinolones in focus (1)].
1996 Sep
Comparative antimycobacterial activities of ofloxacin, ciprofloxacin and grepafloxacin.
1999 Nov
Anti-toxoplasma activities of 24 quinolones and fluoroquinolones in vitro: prediction of activity by molecular topology and virtual computational techniques.
2000 Oct
Prediction of quinolone activity against Mycobacterium avium by molecular topology and virtual computational screening.
2000 Oct
In vitro activities of six fluoroquinolones against 250 clinical isolates of Mycobacterium tuberculosis susceptible or resistant to first-line antituberculosis drugs.
2000 Sep
Fluoroquinolones as chemotherapeutics against mycobacterial infections.
2004
Mycobacterium tuberculosis DNA gyrase: interaction with quinolones and correlation with antimycobacterial drug activity.
2004 Apr
The activity of grepafloxacin in two murine models of Mycobacterium avium infection.
2004 Jun
Torsades de pointes associated with fluoroquinolones: importance of concomitant risk factors.
2004 Mar
Multidrug resistance-associated protein 1 functions as an efflux pump of xenobiotics in the skin.
2005 Jun
Acyl glucuronidation of fluoroquinolone antibiotics by the UDP-glucuronosyltransferase 1A subfamily in human liver microsomes.
2005 Jun
Design, synthesis and activity against Toxoplasma gondii, Plasmodium spp., and Mycobacterium tuberculosis of new 6-fluoroquinolones.
2006 Dec
Mechanism of the inhibitory effect of zwitterionic drugs (levofloxacin and grepafloxacin) on carnitine transporter (OCTN2) in Caco-2 cells.
2006 Nov
Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting.
2010 Dec
Patents

Sample Use Guides

RAXAR (Grepafloxacin) Tablets may be taken with or without meals. The usual dose for RAXAR is 400 mg or 600 mg orally every 24 hours. Sucralfate; antacids containing magnesium, calcium, or aluminum; multivitamins containing iron or zinc; or VIDEX (didanosine) chewable/buffered tablets or the pediatric powder for oral solution should not be taken within 4 hours before or 4 hours after taking grepafloxacin.
Route of Administration: Oral
In Vitro Use Guide
The activity of grepafloxacin was evaluated against five isolates of Chlamydia pneumonia and 21 isolates of Chlamydia trachomatis. MICs were determined using a tissue culture incorporation technique in McCoy cell monolayers treated with Grepafloxacin. After 48–72 h incubation, cover slips were fixed in methanol and stained with an immunofluorescent monoclonal antibody against the major outer membrane protein. Grepafloxacin MIC range was 0.06–0.12 mg/L.
Substance Class Chemical
Created
by admin
on Sat Jun 26 16:28:06 UTC 2021
Edited
by admin
on Sat Jun 26 16:28:06 UTC 2021
Record UNII
L1M1U2HC31
Record Status Validated (UNII)
Record Version
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Name Type Language
GREPAFLOXACIN
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
3-QUINOLINECARBOXYLIC ACID, 1-CYCLOPROPYL-6-FLUORO-1,4-DIHYDRO-5-METHYL-7-(3-METHYL-1-PIPERAZINYL)-4-OXO-, (+/-)-
Common Name English
3-QUINOLINECARBOXYLIC ACID, 1-CYCLOPROPYL-6-FLUORO-1,4-DIHYDRO-5-METHYL-7-(3-METHYL-1-PIPERAZINYL)-4-OXO-
Systematic Name English
GREPAFLOXACIN [WHO-DD]
Common Name English
(+/-)-1-CYCLOPROPYL-6-FLUORO-1,4-DIHYDRO-5-METHYL-7-(3-METHYL-1-PIPERAZINYL)-4-OXO-3-QUINOLINECARBOXYLIC ACID
Systematic Name English
GREPAFLOXACIN [MI]
Common Name English
GREPAFLOXACIN [INN]
Common Name English
GREPAFLOXACIN [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C795
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
WHO-VATC QJ01MA11
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
WHO-ATC J01MA11
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
Code System Code Type Description
CAS
119914-60-2
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
DRUG CENTRAL
1330
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
RXCUI
83719
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY RxNorm
PUBCHEM
72474
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
FDA UNII
L1M1U2HC31
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
EVMPD
SUB07965MIG
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
ChEMBL
CHEMBL583
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
EPA CompTox
119914-60-2
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
DRUG BANK
DB00365
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
WIKIPEDIA
GREPAFLOXACIN
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
MESH
C075375
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
MERCK INDEX
M5850
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C65817
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
INN
7024
Created by admin on Sat Jun 26 16:28:07 UTC 2021 , Edited by admin on Sat Jun 26 16:28:07 UTC 2021
PRIMARY
Related Record Type Details
ENANTIOMER -> RACEMATE
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
ENANTIOMER -> RACEMATE
TRANSPORTER -> INHIBITOR
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC