Moxifloxacin

Identification

Summary

Moxifloxacin is a fluoroquinolone antibiotic used to treat various bacterial infections.

Brand Names

Avelox, Moxeza, Vigamox

Generic Name

Moxifloxacin

DrugBank Accession Number

DB00218

Background

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.

Type

Small Molecule

Groups

Approved, Investigational

Structure

Similar Structures

Weight: Average: 401.4314
Monoisotopic: 401.175084476
Chemical Formula: C₂₁H₂₄FN₃O₄

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
Moxifloxacin
Moxifloxacino

External IDs

BAY 12-8039

Pharmacology

Indication

For 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).

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Associated Conditions

Contraindications & Blackbox Warnings

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Pharmacodynamics

Moxifloxacin 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 action

The 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.

Target	Actions	Organism
ADNA topoisomerase 4 subunit A	inhibitor	Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
ADNA gyrase subunit A	inhibitor	Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
UDNA topoisomerase 2-alpha	inhibitor	Humans

Absorption

Well 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 binding

50% 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 elimination

Approximately 45% of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~20% in urine and ~25% in feces).

Half-life

11.5-15.6 hours (single dose, oral)

Clearance

12 +/- 2 L/hr

Adverse Effects

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Toxicity

Symptoms 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.

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Acarbose	The therapeutic efficacy of Acarbose can be increased when used in combination with Moxifloxacin.
Aceclofenac	Aceclofenac may increase the neuroexcitatory activities of Moxifloxacin.
Acemetacin	Acemetacin may increase the neuroexcitatory activities of Moxifloxacin.
Acenocoumarol	The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Moxifloxacin.
Acetaminophen	The metabolism of Acetaminophen can be decreased when combined with Moxifloxacin.
Acetohexamide	The therapeutic efficacy of Acetohexamide can be increased when used in combination with Moxifloxacin.
Acetylsalicylic acid	Acetylsalicylic acid may increase the neuroexcitatory activities of Moxifloxacin.
Acrivastine	The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Moxifloxacin.
Acyclovir	The metabolism of Acyclovir can be decreased when combined with Moxifloxacin.
Adenosine	The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Adenosine.

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Food Interactions

Drink plenty of fluids.
Take with or without food.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Moxifloxacin hydrochloride	C53598599T	186826-86-8	IDIIJJHBXUESQI-DFIJPDEKSA-N
Moxifloxacin hydrochloride monohydrate	B8956S8609	192927-63-2	SKZIMSDWAIZNDD-WJMOHVQJSA-N

Product Images

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Act Moxifloxacin	Solution	0.5 % w/v	Ophthalmic	TEVA Canada Limited	2015-11-04	Not applicable
Avelox	Tablet	400 mg	Oral	Bayer	2000-10-20	2019-07-04
Avelox	Injection, solution	400 mg/250mL	Intravenous	Bayer HealthCare Pharmaceuticals Inc.	2001-11-30	2020-06-01
Avelox	Tablet, film coated	400 mg/1	Oral	Schering Plough Corporation	1999-12-10	2016-07-29
Avelox	Tablet, film coated	400 mg/1	Oral	Red Pharm Drug, Inc.	2011-02-25	Not applicable
Avelox	Tablet, film coated	400 mg/1	Oral	Remedy Repack	2013-05-24	2017-03-01
Avelox	Injection, solution	400 mg/250mL	Intravenous	Schering Plough Corporation	2001-11-30	2016-07-29
Avelox	Tablet, film coated	400 mg/1	Oral	Cardinal Health	2010-03-02	2015-09-30
Avelox	Tablet, film coated	400 mg/1	Oral	Bayer HealthCare Pharmaceuticals Inc.	1999-12-10	2019-06-30
Avelox	Tablet, film coated	400 mg/1	Oral	Lake Erie Medical DBA Quality Care Products LLC	2011-12-07	2017-12-31

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Ag-moxifloxacin	Solution	0.5 % w/v	Ophthalmic	Angita Pharma Inc.	2020-07-09	Not applicable
Ag-moxifloxacin	Tablet	400 mg	Oral	Angita Pharma Inc.	2018-07-23	Not applicable
Apo-moxifloxacin	Tablet	400 mg	Oral	Apotex Corporation	2016-01-11	Not applicable
Apo-moxifloxacin	Solution	0.5 % w/v	Ophthalmic	Apotex Corporation	2015-11-19	Not applicable
Apo-moxifloxacin Hydrochloride	Tablet	400 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Auro-moxifloxacin	Tablet	400 mg	Oral	Auro Pharma Inc	2015-11-04	Not applicable
Bio-moxifloxacin	Tablet	400 mg	Oral	Biomed Pharma	2016-01-15	Not applicable
Dom-moxifloxacin	Tablet	400 mg	Oral	Dominion Pharmacal	Not applicable	Not applicable
Ipg-moxifloxacin	Tablet	400 mg	Oral	Marcan Pharmaceuticals Inc	Not applicable	Not applicable
Jamp-moxifloxacin	Solution	0.5 % w/v	Ophthalmic	Jamp Pharma Corporation	2019-02-28	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
MOFLAG D	Moxifloxacin (5 mg) + Dexamethasone (1 mg)	Solution	Ophthalmic	LABORATORIOS SYNTHESIS S.A.S	2015-05-27	Not applicable
MOXIDEXA 5 MG/1 MG STERIL OFTALMIK ÇÖZELTİ, 1 ADET	Moxifloxacin (5 mg) + Dexamethasone (1 mg)	Solution / drops	Ophthalmic	ABDİ İBRAHİM İLAÇ SAN. VE TİC. A.Ş.	2020-08-14	Not applicable
TQ OFTAMOX D UD®	Moxifloxacin (5 mg) + Dexamethasone (1 mg)	Solution	Conjunctival; Ophthalmic	TECNOFAR TQ S.A.S	2011-06-23	2017-03-28
TQ OFTAMOX® D UD	Moxifloxacin (5 mg) + Dexamethasone (1 mg)	Solution	Ophthalmic	TECNOFAR TQ S.A.S.	2019-10-11	2020-05-29
VIGADEXA	Moxifloxacin (5 MG/1ML) + Dexamethasone (1 MG/1ML)	Solution / drops	Ophthalmic	บริษัท โนวาร์ตีส (ประเทศไทย) จำกัด	2017-11-07	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
ATAFLOKS 400 MG FILM TABLET, 7 ADET	Moxifloxacin (400 mg)	Tablet, film coated	Oral	ATABAY KİMYA SAN. VE TİC. A.Ş.	2020-08-14	Not applicable
Dex-Moxi	Moxifloxacin hydrochloride monohydrate (5 mg/1mL) + Dexamethasone sodium phosphate (1 mg/1mL)	Injection, solution	Ophthalmic	Imprimis Njof, Llc	2018-01-05	Not applicable
Dex-Moxi PF	Moxifloxacin hydrochloride monohydrate (5 mg/1mL) + Dexamethasone sodium phosphate (1 mg/1mL)	Injection, solution	Intraocular	ImprimisRx NJ	2018-01-01	Not applicable
Dex-Moxi-Ketor	Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL) + Dexamethasone sodium phosphate (1 mg/1mL) + Ketorolac tromethamine (0.4 mg/1mL)	Injection, solution	Ophthalmic	Imprimis Njof, Llc	2018-01-05	Not applicable
DexMoxiKetor PF	Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL) + Dexamethasone sodium phosphate (1 mg/1mL) + Ketorolac tromethamine (0.4 mg/1mL)	Injection, solution	Intraocular	ImprimisRx NJ	2018-01-01	Not applicable
Ixoba M	Moxifloxacin hydrochloride monohydrate (5 mg/1mL) + Ketorolac tromethamine (5 mg/1mL) + Prednisolone acetate (10 mg/1mL)	Kit	Ophthalmic	Brisk Pharmaceuticals, Inc.	2021-08-26	Not applicable
Moxifloxacin PF	Moxifloxacin hydrochloride monohydrate (5 mg/1mL)	Injection, solution	Ophthalmic	Imprimis Njof, Llc	2018-01-05	Not applicable
Moxifloxacin PF	Moxifloxacin hydrochloride monohydrate (5 mg/1mL)	Injection, solution	Ophthalmic	Imprimis Njof, Llc	2020-02-10	Not applicable
Moxifloxacin PF	Moxifloxacin hydrochloride monohydrate (5 mg/1mL)	Injection, solution	Intraocular	ImprimisRx NJ	2018-01-01	Not applicable
Triamcinolone-Moxifloxacin PF	Moxifloxacin hydrochloride (1 mg/1mL) + Triamcinolone acetonide (15 mg/1mL)	Suspension	Ophthalmic	ImprimisRx NJ	2018-01-01	Not applicable

Chemical Identifiers

UNII: U188XYD42P
CAS number: 151096-09-2
InChI Key: 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

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

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. [Article]

External Links

Human Metabolome Database: HMDB0014363
KEGG Drug: D08237
KEGG Compound: C07663
PubChem Compound: 152946
PubChem Substance: 46508509
ChemSpider: 134802
BindingDB: 50366824
RxNav: 139462
ChEBI: 63611
ChEMBL: CHEMBL32
ZINC: ZINC000003826253
Therapeutic Targets Database: DAP000158
PharmGKB: PA450555
PDBe Ligand: MFX
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
PDRhealth: PDRhealth Drug Page
Wikipedia: Moxifloxacin

PDB Entries

2xkk / 3fof / 4z2c / 4z3o / 5bs8 / 5bta / 5cdq

FDA label

Download (162 KB)

MSDS

Download (193 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Periodontitis, Aggressive	1
4	Completed	Not Available	Abscesses / Cysts	1
4	Completed	Not Available	Bacterial Conjunctivitis	1
4	Completed	Not Available	Cataract Surgery	1
4	Completed	Not Available	Cataract Surgery / Corneal Health	1
4	Completed	Basic Science	Antibiotic Resistance, Bacterial	1
4	Completed	Basic Science	Cataracts	2
4	Completed	Basic Science	Healthy Subjects (HS)	1
4	Completed	Basic Science	Side-effect of Antibiotic	1
4	Completed	Other	Antibiotic Side Effect / Endophthalmitis / Safety Issues / Senile Cataract	1

Pharmacoeconomics

Manufacturers

Bayer healthcare pharmaceuticals inc
Alcon inc
Bayer Healthcare Pharmaceuticals

Packagers

Advanced Pharmaceutical Services Inc.
Alcon Laboratories
A-S Medication Solutions LLC
Bayer Healthcare
Cardinal Health
Dispensing Solutions
Diversified Healthcare Services Inc.
Fresenius Kabi AB
H.J. Harkins Co. Inc.
Lake Erie Medical and Surgical Supply
Murfreesboro Pharmaceutical Nursing Supply
PD-Rx Pharmaceuticals Inc.
Physicians Total Care Inc.
Prepackage Specialists
Redpharm Drug
Schering Corp.
Southwood Pharmaceuticals
Stat Rx Usa

Dosage Forms

Form	Route	Strength
Solution	Ophthalmic	0.5 % w/v
Injection, solution	Parenteral	400 MG/250ML
Tablet	Oral	400 mg
Tablet, film coated	Oral
Solution	Parenteral
Tablet, film coated	Oral	400 mg/1
Solution	Intravenous	400 mg / 250 mL
Solution		400 mg/250ml
Solution	Intravenous
Injection	Intravenous	400 mg/250ml
Solution	Intravenous	160 mg
Solution	Ophthalmic
Injection, solution	Ophthalmic
Injection, solution	Intraocular
Solution	Intravenous	400 mg
Tablet, film coated	Oral	400 mg
Kit	Ophthalmic
Injection, solution	Intravenous	400 MG
Solution	Ophthalmic	5 mg/ml
Solution	Conjunctival; Ophthalmic
Injection, solution	Intravenous
Solution / drops	Ophthalmic
Tablet, film coated	Oral	400.00 mg
Tablet	Oral
Solution / drops	Ophthalmic
Injection, solution	Intravenous	400 mg/250mL
Solution / drops	Ophthalmic	5 mg/1mL
Tablet	Oral	400 mg/1
Solution	Intramuscular; Intravenous
Solution	Intravenous	400 mg/250ml
Injection, solution	Intraocular	5 mg/1mL
Injection, solution	Ophthalmic	5 mg/1mL
Injection, solution
Solution	Ophthalmic	5 mg
Injection	Intravenous
Solution	Intravenous	1.6 mg
Suspension	Conjunctival; Ophthalmic
Solution	Ophthalmic	0.5 %
Solution	Ophthalmic
Solution	Conjunctival; Ophthalmic	5 mg
Injection, suspension	Ophthalmic
Suspension	Ophthalmic
Solution	Ophthalmic	5 mg/1mL
Solution / drops	Ophthalmic	5 MG/ML
Liquid	Ophthalmic	5 mg/1ml
Tablet, coated	Oral	400 mg

Prices

Unit description	Cost	Unit
Vigamox 0.5% Solution 3ml Bottle	90.72USD	bottle
Vigamox 0.5% eye drops	27.22USD	ml
Avelox 400 mg tablet	16.68USD	tablet
Avelox abc pack 400 mg tablet	16.35USD	tablet
Avelox iv 400 mg/250 ml	0.17USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US4990517	No	1991-02-05	2011-12-08
CA2342211	No	2009-05-26	2019-09-29
CA1340114	No	1998-11-03	2015-11-03
US5849752	No	1998-12-15	2016-12-05
US6610327	No	2003-08-26	2019-10-29
US6548079	No	2003-04-15	2020-07-25
US7671070	Yes	2010-03-02	2020-03-29
US6716830	Yes	2004-04-06	2020-03-29
US8450311	No	2013-05-28	2029-05-29
US9114168	No	2015-08-25	2029-05-29

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	238-242 °C	Not Available
logP	2.9	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.168 mg/mL	ALOGPS
logP	0.01	ALOGPS
logP	-0.5	ChemAxon
logS	-3.4	ALOGPS
pKa (Strongest Acidic)	5.69	ChemAxon
pKa (Strongest Basic)	9.42	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	7	ChemAxon
Hydrogen Donor Count	2	ChemAxon
Polar Surface Area	82.11 Å²	ChemAxon
Rotatable Bond Count	4	ChemAxon
Refractivity	106.22 m³·mol^-1	ChemAxon
Polarizability	41.24 Å³	ChemAxon
Number of Rings	5	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9794
Blood Brain Barrier	-	0.9597
Caco-2 permeable	-	0.6093
P-glycoprotein substrate	Substrate	0.8607
P-glycoprotein inhibitor I	Non-inhibitor	0.7564
P-glycoprotein inhibitor II	Non-inhibitor	0.7181
Renal organic cation transporter	Non-inhibitor	0.7318
CYP450 2C9 substrate	Non-substrate	0.8018
CYP450 2D6 substrate	Non-substrate	0.8247
CYP450 3A4 substrate	Non-substrate	0.5756
CYP450 1A2 substrate	Non-inhibitor	0.7417
CYP450 2C9 inhibitor	Non-inhibitor	0.7735
CYP450 2D6 inhibitor	Non-inhibitor	0.8359
CYP450 2C19 inhibitor	Non-inhibitor	0.7401
CYP450 3A4 inhibitor	Non-inhibitor	0.8811
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.5536
Ames test	AMES toxic	0.6227
Carcinogenicity	Non-carcinogens	0.9038
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.3267 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.8092
hERG inhibition (predictor II)	Non-inhibitor	0.6461

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Available
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0udi-0176900000-5ca9cd234a2a93f05658
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0udi-0391000000-7a74ddcc516a82243c1a

Targets

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insights and accelerate drug research.

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Details1. DNA topoisomerase 4 subunit A

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
Uniprot Name: DNA topoisomerase 4 subunit A
Molecular Weight: 83366.24 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]

Details2. DNA gyrase subunit A

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, inc...
Gene Name: gyrA
Uniprot ID: P43700
Uniprot Name: DNA gyrase subunit A
Molecular Weight: 97817.145 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]

Details3. DNA topoisomerase 2-alpha

Kind: Protein
Organism: Humans
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 segr...
Gene Name: TOP2A
Uniprot ID: P11388
Uniprot Name: DNA topoisomerase 2-alpha
Molecular Weight: 174383.88 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
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. [Article]
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. [Article]

Enzymes

Details1. Cytochrome P450 1A2

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Inhibitor

General Function: Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP1A2
Uniprot ID: P05177
Uniprot Name: Cytochrome P450 1A2
Molecular Weight: 58293.76 Da

References

Zhou SF, Yang LP, Zhou ZW, Liu YH, Chan E: Insights into the substrate specificity, inhibitors, regulation, and polymorphisms and the clinical impact of human cytochrome P450 1A2. AAPS J. 2009 Sep;11(3):481-94. doi: 10.1208/s12248-009-9127-y. Epub 2009 Jul 10. [Article]

Drug created at June 13, 2005 13:24 / Updated at December 03, 2021 01:12

Moxifloxacin

Identification

Structure for Moxifloxacin (DB00218)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

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Enzymes

References