Moxifloxacin
Identification
- Name
- Moxifloxacin
- Accession Number
- DB00218
- 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.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Moxifloxacin (DB00218)
- 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
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- 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).
- Associated Conditions
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- 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 inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) ADNA gyrase subunit A inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) UDNA topoisomerase 2-alpha inhibitorHumans - 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
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data- 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.
- Affected organisms
- Enteric bacteria and other eubacteria
- 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 Integrate drug-drug
interactions in your softwareAcarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Moxifloxacin. Acebutolol The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Acebutolol. 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. 
Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more - Food Interactions
- Drink plenty of fluids.
- Take with or without food.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- 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 Region Image Act Moxifloxacin Solution Ophthalmic TEVA Canada Limited 2015-11-04 Not applicable Canada 
Avelox Tablet 400 mg Oral Bayer 2000-10-20 2019-07-04 Canada Avelox Tablet, film coated 400 mg/1 Oral Bayer HealthCare Pharmaceuticals Inc. 1999-12-10 2019-06-30 US 
Avelox Injection, solution 400 mg/250mL Intravenous Schering Plough Corporation 2001-11-30 2016-07-29 US Avelox Injection, solution 400 mg/250mL Intravenous Bayer HealthCare Pharmaceuticals Inc. 2001-11-30 2020-06-01 US Avelox Tablet, film coated 400 mg/1 Oral Remedy Repack 2013-05-24 2017-03-01 US 
Avelox Tablet, film coated 400 mg/1 Oral Lake Erie Medical DBA Quality Care Products LLC 2011-12-07 2017-12-31 US Avelox Tablet, film coated 400 mg/1 Oral Physicians Total Care, Inc. 2009-07-16 Not applicable US 
Avelox Tablet, film coated 400 mg/1 Oral PD-Rx Pharmaceuticals, Inc. 1999-12-10 2018-08-01 US Avelox Tablet, film coated 400 mg/1 Oral Cardinal Health 2010-03-02 2015-09-30 US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ag-moxifloxacin Solution Ophthalmic Angita Pharma Inc. 2020-07-09 Not applicable Canada Ag-moxifloxacin Tablet Oral Angita Pharma Inc. 2018-07-23 Not applicable Canada Apo-moxifloxacin Solution Ophthalmic Apotex Corporation 2015-11-19 Not applicable Canada Apo-moxifloxacin Tablet Oral Apotex Corporation 2016-01-11 Not applicable Canada Auro-moxifloxacin Tablet Oral Auro Pharma Inc 2015-11-04 Not applicable Canada Bio-moxifloxacin Tablet Oral Biomed Pharma 2016-01-15 Not applicable Canada Dom-moxifloxacin Tablet Oral Dominion Pharmacal Not applicable Not applicable Canada Ipg-moxifloxacin Tablet Oral Marcan Pharmaceuticals Inc Not applicable Not applicable Canada Jamp-moxifloxacin Solution Ophthalmic Jamp Pharma Corporation 2019-02-28 Not applicable Canada Jamp-moxifloxacin Tablet Oral Jamp Pharma Corporation 2015-11-04 Not applicable Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 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 US 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 US 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 US 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 US Moxifloxacin PF Moxifloxacin hydrochloride monohydrate (5 mg/1mL) Injection, solution Intraocular ImprimisRx NJ 2018-01-01 Not applicable US Moxifloxacin PF Moxifloxacin hydrochloride monohydrate (5 mg/1mL) Injection, solution Ophthalmic Imprimis Njof, Llc 2018-01-05 Not applicable US Moxifloxacin PF Moxifloxacin hydrochloride monohydrate (5 mg/1mL) Injection, solution Ophthalmic Imprimis Njof, Llc 2020-02-10 Not applicable US Triamcinolone-Moxifloxacin PF Moxifloxacin hydrochloride (1 mg/1mL) + Triamcinolone acetonide (15 mg/1mL) Suspension Ophthalmic ImprimisRx NJ 2018-01-01 Not applicable US Triamcinolone-Moxifloxacin PF Moxifloxacin hydrochloride monohydrate (1 mg/1mL) + Triamcinolone acetonide (15 mg/1mL) Injection, suspension Ophthalmic Imprimis Njof, Llc 2018-01-05 Not applicable US
Categories
- ATC Codes
- S01AE07 — MoxifloxacinJ01MA14 — Moxifloxacin
- Drug Categories
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antiinfectives for Systemic Use
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (moderate)
- Cytochrome P-450 Enzyme Inhibitors
- Enzyme Inhibitors
- Fluoroquinolones
- Heterocyclic Compounds, Fused-Ring
- Moderate Risk QTc-Prolonging Agents
- Ophthalmologicals
- QTc Prolonging Agents
- Quinolines
- Quinolone Antimicrobial
- Quinolones
- Sensory Organs
- Topoisomerase II Inhibitors
- Topoisomerase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This 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.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Quinolines and derivatives
- Sub Class
- Quinoline carboxylic acids
- Direct Parent
- Quinoline carboxylic acids
- Alternative Parents
- Fluoroquinolones / Haloquinolines / Hydroquinolones / Aminoquinolines and derivatives / Hydroquinolines / Pyrrolopyridines / Pyridinecarboxylic acids / Methoxyanilines / Dialkylarylamines / Anisoles show 15 more
- Substituents
- Alkyl aryl ether / Amine / Amino acid / Amino acid or derivatives / Aminoquinoline / Anisole / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle show 33 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- aromatic ether, cyclopropanes, quinolone antibiotic, fluoroquinolone antibiotic, quinolone, quinolinemonocarboxylic acid, pyrrolidinopiperidine (CHEBI:63611)
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. [PubMed:14614666]
- External Links
- Human Metabolome Database
- HMDB0014363
- KEGG Drug
- D08237
- KEGG Compound
- C07663
- PubChem Compound
- 152946
- PubChem Substance
- 46508509
- ChemSpider
- 134802
- BindingDB
- 50366824
- 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
- AHFS Codes
- 52:04.04 — Antibacterials
- 08:12.18 — Quinolones
- 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 Anti-Biotic Resistance 1 4 Completed Basic Science Cataracts 2 4 Completed Basic Science Healthy Volunteers 1 4 Completed Basic Science Side-effect of Antibiotic 1 4 Completed Other Antibiotic Side Effect / Cataract Senile / Endophthalmitis / Safety Issues 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 Tablet Oral Injection, solution Parenteral 400 MG/250ML Tablet, film coated Oral Tablet, film coated Oral 400 MG Injection Intravenous 0.16 % Tablet, film coated Oral 436.8 Mg Tablet, coated Oral 400 mg Injection Intravenous 400 mg Solution Parenteral 400 mg/250ml Tablet, film coated Oral 400 mg/1 Solution Intravenous Solution Solution Intravenous 400 mg/250mL Solution Intravenous 160 mg Solution Ophthalmic 5 mg/ml Solution / drops Ophthalmic 0.5 % Injection, solution Ophthalmic Injection, solution Intraocular Solution Intravenous 400 mg Injection, solution Intravenous Injection Intravenous 400 mg/250ml Solution Conjunctival; Ophthalmic 1 mg Solution / drops Ophthalmic 5.5 mg Solution / drops Ophthalmic 0.5 %w/v Solution / drops Ophthalmic 5 mg/ml Injection, solution Intravenous 400 mg Tablet Oral 400 MG Solution / drops Ophthalmic 5 mg Injection, solution Intravenous 400 mg/250mL Solution / drops Ophthalmic 5 mg/1mL Solution Parenteral 400 mg Injection Intravenous 1.6 mg/ml Solution / drops Ophthalmic 5.5 mg/3ml Tablet, film coated Oral 453.8 MG Injection Intravenous 1.745 mg Tablet Oral 400 mg/1 Tablet, film coated Oral 40 MG Tablet, film coated Oral 436.3 MG Solution Intramuscular; Intravenous 400 mg/250ml Injection, solution Intraocular 5 mg/1mL Injection, solution Ophthalmic 5 mg/1mL Injection, solution 400 MG/250ML Solution Ophthalmic 5 mg Injection Intravenous Solution Ophthalmic 1 mg Solution Conjunctival; Ophthalmic 5 mg Solution Intravenous 1.6 mg Suspension Conjunctival; Ophthalmic 0.1 g Injection, suspension Ophthalmic Suspension Ophthalmic Solution / drops Ophthalmic Solution Ophthalmic 5 mg/1mL Solution / drops Ophthalmic 5.45 mg/ml Solution Ophthalmic 0.5 % Solution / drops Ophthalmic 0.5 % W/V Liquid Ophthalmic Tablet, coated Oral Solution / drops Ophthalmic - 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) Region US4990517 No 1991-02-05 2011-12-08 US CA2342211 No 2009-05-26 2019-09-29 Canada CA1340114 No 1998-11-03 2015-11-03 Canada US5849752 No 1998-12-15 2016-12-05 US US6610327 No 2003-08-26 2019-10-29 US US6548079 No 2003-04-15 2020-07-25 US US7671070 Yes 2010-03-02 2020-03-29 US US6716830 Yes 2004-04-06 2020-03-29 US US8450311 No 2013-05-28 2029-05-29 US US9114168 No 2015-08-25 2029-05-29 US
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
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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- 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. [PubMed:17139284]
- 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]
- 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]
- 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]
- 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
- 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. [PubMed:17139284]
- 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]
- 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]
- 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]
- 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
- 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. [PubMed:11752352]
- 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]
- 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]
Enzymes
- 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. [PubMed:19590965]
Drug created on June 13, 2005 13:24 / Updated on February 24, 2021 19:34