Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C19H22FN3O3 |
| Molecular Weight | 359.3947 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1CN(CCN1)C2=CC3=C(C(=O)C(=CN3C4CC4)C(O)=O)C(C)=C2F
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)
| Molecular Formula | C19H22FN3O3 |
| Molecular Weight | 359.3947 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/nda/97/20-695_Raxar_Pharma.pdf | https://www.drugbank.ca/drugs/DB00365
Curator's Comment: description was created based on several sources, including
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
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2363076 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10824040 |
|||
Target ID: CHEMBL2094255 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10824040 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Curative | RAXAR Approved UseRAXAR 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 Date1997 |
|||
| Curative | RAXAR Approved UseRAXAR 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 Date1997 |
|||
| Curative | RAXAR Approved UseRAXAR 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 Date1997 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.47 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
|
0.93 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
|
1.43 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.08 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
|
11.35 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
|
14.6 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
10.14 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
|
11.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
|
50% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9433650 |
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 |
Doses
| Dose | Population | Adverse 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) Sources: Vomiting (1 patient) Taste perversion (2 patients) Dizziness (3 patients) Diarrhea (2 patients) |
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) Sources: Vomiting (4 patients) Taste perversion (5 patients) Dizziness (3 patients) Diarrhea (1 patient) |
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 |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (1.2%) Sources: Vomiting (1.2%) |
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 |
Disc. AE: Bad taste, Nausea... AEs leading to discontinuation/dose reduction: Bad taste (0.3%) Sources: Nausea (0.8%) Vomiting (0.6%) Headache (0.3%) Dizziness (0.5%) Rash (0.2%) Tachycardia (<0.1%) |
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 |
Disc. AE: Bad taste, Nausea... AEs leading to discontinuation/dose reduction: Bad taste (1%) Sources: Nausea (2.6%) Vomiting (1.4%) Headache (0.6%) Dizziness (0.6%) Rash (0.6%) Tachycardia (0.14%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes | ||||
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes | ||||
| yes |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting. | 2010-12 |
|
| Design, synthesis and activity against Toxoplasma gondii, Plasmodium spp., and Mycobacterium tuberculosis of new 6-fluoroquinolones. | 2006-12 |
|
| Mechanism of the inhibitory effect of zwitterionic drugs (levofloxacin and grepafloxacin) on carnitine transporter (OCTN2) in Caco-2 cells. | 2006-11 |
|
| Multidrug resistance-associated protein 1 functions as an efflux pump of xenobiotics in the skin. | 2005-06 |
|
| Acyl glucuronidation of fluoroquinolone antibiotics by the UDP-glucuronosyltransferase 1A subfamily in human liver microsomes. | 2005-06 |
|
| The activity of grepafloxacin in two murine models of Mycobacterium avium infection. | 2004-06 |
|
| Mycobacterium tuberculosis DNA gyrase: interaction with quinolones and correlation with antimycobacterial drug activity. | 2004-04 |
|
| Torsades de pointes associated with fluoroquinolones: importance of concomitant risk factors. | 2004-03 |
|
| Fluoroquinolones as chemotherapeutics against mycobacterial infections. | 2004 |
|
| Clinical toxicological aspects of fluoroquinolones. | 2002-02-28 |
|
| Comparison of antimycobacterial activity of grepafloxacin against Mycobacterium avium with that of levofloxacin: accumulation of grepafloxacin in human macrophages. | 2001-03 |
|
| Anti-toxoplasma activities of 24 quinolones and fluoroquinolones in vitro: prediction of activity by molecular topology and virtual computational techniques. | 2000-10 |
|
| Prediction of quinolone activity against Mycobacterium avium by molecular topology and virtual computational screening. | 2000-10 |
|
| In vitro activities of six fluoroquinolones against 250 clinical isolates of Mycobacterium tuberculosis susceptible or resistant to first-line antituberculosis drugs. | 2000-09 |
|
| Comparative antimycobacterial activities of ofloxacin, ciprofloxacin and grepafloxacin. | 1999-11 |
|
| [In vitro anti-MAC activities of new quinolones in focus (2)]. | 1996-09 |
|
| [In vitro anti-MAC activities of new quinolones in focus (1)]. | 1996-09 |
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9484871
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
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| Record UNII |
L1M1U2HC31
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| Record Status |
Validated (UNII)
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NCI_THESAURUS |
C795
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WHO-VATC |
QJ01MA11
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CFR |
21 CFR 216.24
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WHO-ATC |
J01MA11
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119914-60-2
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1330
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83719
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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PRIMARY | RxNorm | ||
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72474
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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100000084239
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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L1M1U2HC31
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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SUB07965MIG
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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CHEMBL583
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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DTXSID2048321
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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DB00365
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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GREPAFLOXACIN
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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C075375
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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m5850
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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PRIMARY | Merck Index | ||
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C65817
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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7024
Created by
admin on Mon Mar 31 18:45:33 GMT 2025 , Edited by admin on Mon Mar 31 18:45:33 GMT 2025
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| Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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ENANTIOMER -> RACEMATE | |||
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SALT/SOLVATE -> PARENT | |||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT | |||
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TARGET ORGANISM->INHIBITOR |
18 STRAINS; SOME LESS THE 8 ng/mL for many strains; MIC range listed
MIC90
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BINDER->LIGAND |
BINDING
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ENANTIOMER -> RACEMATE | |||
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SALT/SOLVATE -> PARENT |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Volume of Distribution | PHARMACOKINETIC |
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| Biological Half-life | PHARMACOKINETIC |
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