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Identification
NameMoxifloxacin
Accession NumberDB00218  (APRD00281)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Moxifloxacin is a synthetic fluoroquinolone antibiotic agent. Bayer AG developed the drug (initially called BAY 12-8039) and it is marketed worldwide (as the hydrochloride) under the brand name Avelox (in some countries also Avalox) for oral treatment.

Structure
Thumb
Synonyms
1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-((4as,7as)-octahydro-6H-pyrrolo(3,4-b)pyridin-6-yl)-4-oxo-3-quinolinecarboxylic acid
External Identifiers
  • BAY 12-8039
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Moxifloxacinsolution0.5 %ophthalmicActavis Pharma Company2015-11-04Not applicableCanada
Auro-moxifloxacintablet400 mgoralAuro Pharma Inc2015-11-04Not applicableCanada
Aveloxtablet, film coated400 mg/1oralCardinal Health2010-03-02Not applicableUs
Aveloxtablet, film coated400 mg/1oralPhysicians Total Care, Inc.2009-07-16Not applicableUs
Aveloxtablet400 mgoralBayer Inc2000-10-20Not applicableCanada
Aveloxtablet, film coated400 mg/1oralREMEDYREPACK INC.2013-05-24Not applicableUs
Aveloxtablet, film coated400 mg/1oralRed Pharm Drug Inc.2011-02-25Not applicableUs
Aveloxinjection, solution400 mg/250mLintravenousSchering Plough Corporation2001-11-30Not applicableUs
Aveloxtablet, coated400 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-07Not applicableUs
Aveloxtablet, film coated400 mg/1oralSchering Plough Corporation1999-12-10Not applicableUs
Aveloxtablet, film coated400 mg/1oralPd Rx Pharmaceuticals, Inc.2011-02-25Not applicableUs
Avelox Abc Packtablet, film coated400 mg/1oralStat Rx USA1999-12-10Not applicableUs
Avelox I.V.solution400 mgintravenousBayer Inc2003-06-24Not applicableCanada
Bio-moxifloxacintablet400 mgoralBiomed Pharma2016-01-15Not applicableCanada
Ipg-moxifloxacintablet400 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-moxifloxacintablet400 mgoralJamp Pharma Corporation2015-11-04Not applicableCanada
Jamp-moxifloxacin Tabletstablet400 mgoralJamp Pharma Corporation2016-01-11Not applicableCanada
Mar-moxifloxacintablet400 mgoralMarcan Pharmaceuticals Inc2015-12-21Not applicableCanada
Moxezasolution5 mg/mLophthalmicAlcon Laboratories, Inc.2011-01-18Not applicableUs
Moxifloxacininjection, solution400 mg/250mLintravenousFresenius Kabi USA, LLC2015-03-18Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralPd Rx Pharmaceuticals, Inc.2014-01-29Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralAlvogen, Inc.2014-01-29Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralREMEDYREPACK INC.2015-06-29Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralPd Rx Pharmaceuticals, Inc.2014-01-29Not applicableUs
Mylan-moxifloxacintablet400 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
PMS-moxifloxacinsolution0.5 %ophthalmicPharmascience Inc2015-12-21Not applicableCanada
Priva-moxifloxacintablet400 mgoralPharmapar Inc2016-01-15Not applicableCanada
Riva-moxifloxacintablet400 mgoralLaboratoire Riva Inc2016-03-31Not applicableCanada
Riva-moxifloxacintablet400 mgoralLaboratoire Riva IncNot applicableNot applicableCanada
Sandoz Moxifloxacintablet400 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz Moxifloxacinsolution0.5 %ophthalmicSandoz Canada Incorporated2015-10-29Not applicableCanada
Teva-moxifloxacintablet400 mgoralTeva Canada Limited2015-11-04Not applicableCanada
Teva-moxifloxacinsolution0.5 %ophthalmicTeva Canada LimitedNot applicableNot applicableCanada
Vigamoxsolution5 mg/mLophthalmicREMEDYREPACK INC.2014-10-20Not applicableUs
Vigamoxsolution0.5 %ophthalmicAlcon Canada Inc2004-05-12Not applicableCanada
Vigamoxsolution5 mg/mLophthalmicPhysicians Total Care, Inc.2003-05-22Not applicableUs
Vigamoxsolution5 mg/mLophthalmicRebel Distributors Corp2003-05-07Not applicableUs
Vigamoxsolution/ drops5 mg/mLophthalmicAlcon Laboratories, Inc.2003-05-07Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-moxifloxacintablet400 mgoralApotex Inc2016-01-11Not applicableCanada
Apo-moxifloxacinsolution0.5 %ophthalmicApotex Inc2015-11-19Not applicableCanada
Moxifloxacintablet, film coated400 mg/1oralDr. Reddy's Laboratories Limited2014-03-05Not applicableUs
Moxifloxacintablet, film coated400 mg/1oralMajor Pharmaceuticals2014-03-05Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralTeva Pharmaceuticals USA Inc2014-02-19Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralAurobindo Pharma Limited2014-03-04Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralCitron Pharma LLC2014-03-04Not applicableUs
Moxifloxacin Hydrochloridetablet400 mg/1oralTorrent Pharmaceuticals Limited2014-04-03Not applicableUs
Moxifloxacin Hydrochloridetablet400 mg/1oralFera Pharmaceuticals, LLC2016-01-22Not applicableUs
Moxifloxacin Hydrochloridetablet400 mg/1oralMylan Pharmaceuticals Inc.2015-09-23Not applicableUs
Moxifloxacin Hydrochloridetablet, film coated400 mg/1oralAmerican Health Packaging2014-03-20Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Moxifloxacin hydrochloride
186826-86-8
Thumb
  • InChI Key: IDIIJJHBXUESQI-DFIJPDEKSA-N
  • Monoisotopic Mass: 437.151762215
  • Average Mass: 437.892
DBSALT000387
Categories
UNIIU188XYD42P
CAS number151096-09-2
WeightAverage: 401.4314
Monoisotopic: 401.175084476
Chemical FormulaC21H24FN3O4
InChI KeyInChIKey=FABPRXSRWADJSP-MEDUHNTESA-N
InChI
InChI=1S/C21H24FN3O4/c1-29-20-17-13(19(26)14(21(27)28)9-25(17)12-4-5-12)7-15(22)18(20)24-8-11-3-2-6-23-16(11)10-24/h7,9,11-12,16,23H,2-6,8,10H2,1H3,(H,27,28)/t11-,16+/m0/s1
IUPAC Name
7-[(4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
SMILES
[H][C@]12CN(C[C@@]1([H])NCCC2)C1=C(F)C=C2C(=O)C(=CN(C3CC3)C2=C1OC)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassQuinoline carboxylic acids
Direct ParentQuinoline carboxylic acids
Alternative Parents
Substituents
  • Quinoline-3-carboxylic acid
  • Fluoroquinolone
  • Hydroxyquinoline
  • Dihydroquinolone
  • Aminoquinoline
  • Dihydroquinoline
  • Methoxyaniline
  • Pyrrolopyridine
  • Pyridine carboxylic acid or derivatives
  • Pyridine carboxylic acid
  • Dialkylarylamine
  • Anisole
  • Fluorobenzene
  • Alkyl aryl ether
  • Benzenoid
  • Pyridine
  • Piperidine
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Pyrrolidine
  • Cyclic alcohol
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Monocarboxylic acid or derivatives
  • Ether
  • Secondary aliphatic amine
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of sinus and lung infections such as sinusitis, pneumonia, and secondary infections in chronic bronchitis. Also for the treatment of bacterial conjunctivitis (pinkeye).
PharmacodynamicsMoxifloxacin is a quinolone/fluoroquinolone antibiotic. Moxifloxacin can be used to treat infections caused by the following bacteria: Aerobic Gram-positive microorganisms: Corynebacterium species, Micrococcus luteus, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus warneri, Streptococcus pneumoniae, and Streptococcus viridans group. Aerobic Gram-negative microorganisms: Acinetobacter lwoffii, Haemophilus influenzae, and Haemophilus parainfluenzae. Other microorganisms: Chlamydia trachomatis.
Moxifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Moxifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Mechanism of actionThe bactericidal action of moxifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.
Related Articles
AbsorptionWell absorbed from the gastrointestinal tract. Absolute oral bioavailability is approximately 90%. Food has little effect on absorption.
Volume of distribution
  • 1.7 to 2.7 L/kg
Protein binding50% bound to serum proteins, independent of drug concentration.
Metabolism

Approximately 52% or oral or intravenous dose is metabolized via glucuronide and sulphate conjugation. The cytochrome P450 system is not involved in metabolism. The sulphate conjugate accounts for 38% of the dose, and the glucuronide conjugate accounts for 14% of the dose.

Route of eliminationApproximately 45% of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~20% in urine and ~25% in feces).
Half life11.5-15.6 hours (single dose, oral)
Clearance
  • 12 +/- 2 L/hr
ToxicitySymptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
Affected organisms
  • Enteric bacteria and other eubacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9794
Blood Brain Barrier-0.9597
Caco-2 permeable-0.6093
P-glycoprotein substrateSubstrate0.8607
P-glycoprotein inhibitor INon-inhibitor0.7564
P-glycoprotein inhibitor IINon-inhibitor0.7181
Renal organic cation transporterNon-inhibitor0.7318
CYP450 2C9 substrateNon-substrate0.8018
CYP450 2D6 substrateNon-substrate0.8247
CYP450 3A4 substrateNon-substrate0.5756
CYP450 1A2 substrateNon-inhibitor0.7417
CYP450 2C9 inhibitorNon-inhibitor0.7735
CYP450 2D6 inhibitorNon-inhibitor0.8359
CYP450 2C19 inhibitorNon-inhibitor0.7401
CYP450 3A4 inhibitorNon-inhibitor0.8811
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5536
Ames testAMES toxic0.6227
CarcinogenicityNon-carcinogens0.9038
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3267 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8092
hERG inhibition (predictor II)Non-inhibitor0.6461
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Bayer healthcare pharmaceuticals inc
  • Alcon inc
  • Bayer Healthcare Pharmaceuticals
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous400 mg/250mL
Tabletoral400 mg
Tablet, coatedoral400 mg/1
Tablet, film coatedoral400 mg/1
Solutionintravenous400 mg
Solutionophthalmic5 mg/mL
Tabletoral400 mg/1
Solutionophthalmic0.5 %
Solution/ dropsophthalmic5 mg/mL
Prices
Unit descriptionCostUnit
Vigamox 0.5% Solution 3ml Bottle90.72USD bottle
Vigamox 0.5% eye drops27.22USD ml
Avelox 400 mg tablet16.68USD tablet
Avelox abc pack 400 mg tablet16.35USD tablet
Avelox iv 400 mg/250 ml0.17USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340114 No1998-11-032015-11-03Canada
CA2342211 No2009-05-262019-09-29Canada
US4990517 No1994-12-082011-12-08Us
US5849752 No1996-12-052016-12-05Us
US6548079 No2000-07-252020-07-25Us
US6610327 No1999-10-292019-10-29Us
US6716830 Yes2000-03-292020-03-29Us
US7671070 Yes2000-03-292020-03-29Us
US8450311 No2009-05-292029-05-29Us
US9114168 No2009-05-292029-05-29Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point238-242 °CNot Available
logP2.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.168 mg/mLALOGPS
logP0.01ALOGPS
logP-0.5ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)5.69ChemAxon
pKa (Strongest Basic)9.42ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area82.11 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity106.22 m3·mol-1ChemAxon
Polarizability41.24 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Manne Reddy, Sajja Eswaraiah, Vetukuri Venkata Naga Raju, Rapolu Kumar, Ningam Srinivasreddy, Vedantham Ravindra, “Crystalline form III of anhydrous moxifloxacin hydrochloride and a process for preparation thereof.” U.S. Patent US20050137227, issued June 23, 2005.

US20050137227
General References
  1. Ginsburg AS, Hooper N, Parrish N, Dooley KE, Dorman SE, Booth J, Diener-West M, Merz WG, Bishai WR, Sterling TR: Fluoroquinolone resistance in patients with newly diagnosed tuberculosis. Clin Infect Dis. 2003 Dec 1;37(11):1448-52. Epub 2003 Nov 4. [PubMed:14614666 ]
External Links
ATC CodesJ01MA14S01AE07
AHFS Codes
  • 08:12.18
  • 52:04.04
PDB EntriesNot Available
FDA labelDownload (162 KB)
MSDSDownload (193 KB)
Interactions
Drug Interactions
Drug
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Moxifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Moxifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
CitalopramMoxifloxacin may increase the QTc-prolonging activities of Citalopram.
DicoumarolMoxifloxacin may increase the anticoagulant activities of Dicoumarol.
DidanosineThe serum concentration of Didanosine can be decreased when it is combined with Moxifloxacin.
DofetilideMoxifloxacin may increase the QTc-prolonging activities of Dofetilide.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Moxifloxacin.
GoserelinGoserelin may increase the QTc-prolonging activities of Moxifloxacin.
InfliximabInfliximab may increase the neuroexcitatory activities of Moxifloxacin.
Insulin HumanMoxifloxacin may increase the hypoglycemic activities of Insulin Regular.
Iron DextranThe serum concentration of Moxifloxacin can be decreased when it is combined with Iron Dextran.
IvabradineIvabradine may increase the QTc-prolonging activities of Moxifloxacin.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Moxifloxacin.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Moxifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium SulfateThe serum concentration of Moxifloxacin can be decreased when it is combined with Magnesium Sulfate.
MequitazineMoxifloxacin may increase the arrhythmogenic activities of Mequitazine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Moxifloxacin.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Moxifloxacin.
OctreotideOctreotide may increase the QTc-prolonging activities of Moxifloxacin.
Picosulfuric acidThe therapeutic efficacy of Sodium picosulfate can be decreased when used in combination with Moxifloxacin.
PorfimerMoxifloxacin may increase the photosensitizing activities of Porfimer.
ProbenecidThe serum concentration of Moxifloxacin can be increased when it is combined with Probenecid.
QuinaprilThe serum concentration of Moxifloxacin can be decreased when it is combined with Quinapril.
SevelamerSevelamer can cause a decrease in the absorption of Moxifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Strontium ranelateThe serum concentration of Moxifloxacin can be decreased when it is combined with Strontium ranelate.
SucralfateThe serum concentration of Moxifloxacin can be decreased when it is combined with Sucralfate.
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Moxifloxacin.
VerteporfinMoxifloxacin may increase the photosensitizing activities of Verteporfin.
Food Interactions
  • Take without regard to meals. Drink liberally. Absorption is not affected by lipid-rich meals or yogourt.

Targets

Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.
Gene Name:
gyrA
Uniprot ID:
P43700
Molecular Weight:
97817.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Schmitz FJ, Hofmann B, Hansen B, Scheuring S, Luckefahr M, Klootwijk M, Verhoef J, Fluit A, Heinz HP, Kohrer K, Jones ME: Relationship between ciprofloxacin, ofloxacin, levofloxacin, sparfloxacin and moxifloxacin (BAY 12-8039) MICs and mutations in grlA, grlB, gyrA and gyrB in 116 unrelated clinical isolates of Staphylococcus aureus. J Antimicrob Chemother. 1998 Apr;41(4):481-4. [PubMed:9598779 ]
  4. Brisse S, Milatovic D, Fluit AC, Verhoef J, Martin N, Scheuring S, Kohrer K, Schmitz FJ: Comparative in vitro activities of ciprofloxacin, clinafloxacin, gatifloxacin, levofloxacin, moxifloxacin, and trovafloxacin against Klebsiella pneumoniae, Klebsiella oxytoca, Enterobacter cloacae, and Enterobacter aerogenes clinical isolates with alterations in GyrA and ParC proteins. Antimicrob Agents Chemother. 1999 Aug;43(8):2051-5. [PubMed:10428935 ]
  5. Dridi L, Tankovic J, Burghoffer B, Barbut F, Petit JC: gyrA and gyrB mutations are implicated in cross-resistance to Ciprofloxacin and moxifloxacin in Clostridium difficile. Antimicrob Agents Chemother. 2002 Nov;46(11):3418-21. [PubMed:12384345 ]
Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
Gene Name:
parC
Uniprot ID:
P43702
Molecular Weight:
83366.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Schafer J, Hovde LB, Simonson D, Rotschafer JC: In vitro pharmacodynamics of moxifloxacin versus levofloxacin against 4 strains of Streptococcus pneumoniae: 1 wild type, 2 first-step parC mutants, and 1 pump mutant. Diagn Microbiol Infect Dis. 2008 Feb;60(2):155-61. Epub 2007 Oct 29. [PubMed:17910998 ]
  4. Deryke CA, Du X, Nicolau DP: Evaluation of bacterial kill when modelling the bronchopulmonary pharmacokinetic profile of moxifloxacin and levofloxacin against parC-containing isolates of Streptococcus pneumoniae. J Antimicrob Chemother. 2006 Sep;58(3):601-9. Epub 2006 Jul 19. [PubMed:16857688 ]
  5. Perez-Vazquez M, Roman F, Aracil B, Canton R, Campos J: Laboratory detection of Haemophilus influenzae with decreased susceptibility to nalidixic acid, ciprofloxacin, levofloxacin, and moxifloxacin due to GyrA and ParC mutations. J Clin Microbiol. 2004 Mar;42(3):1185-91. [PubMed:15004073 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Ubiquitin binding
Specific Function:
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segregation of daughter chromosomes. May play a role in regulating the period length of ARNTL/BMAL1 transcriptional oscillation (By similarity).
Gene Name:
TOP2A
Uniprot ID:
P11388
Molecular Weight:
174383.88 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Reuveni D, Halperin D, Shalit I, Priel E, Fabian I: Moxifloxacin enhances etoposide-induced cytotoxic, apoptotic and anti-topoisomerase II effects in a human colon carcinoma cell line. Int J Oncol. 2010 Aug;37(2):463-71. [PubMed:20596674 ]
  3. Wohlkonig A, Chan PF, Fosberry AP, Homes P, Huang J, Kranz M, Leydon VR, Miles TJ, Pearson ND, Perera RL, Shillings AJ, Gwynn MN, Bax BD: Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance. Nat Struct Mol Biol. 2010 Sep;17(9):1152-3. doi: 10.1038/nsmb.1892. Epub 2010 Aug 29. [PubMed:20802486 ]
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Drug created on June 13, 2005 07:24 / Updated on August 24, 2016 03:05