This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Generic Name
- Garenoxacin
- DrugBank Accession Number
- DB06160
- Background
Garenoxacin, a quinolone antibiotic, is being investigated for the treatment of gram-positive and gram-negative bacterial infections.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for Garenoxacin (DB06160)
- Weight
- Average: 426.42
Monoisotopic: 426.139113458 - Chemical Formula
- C23H20F2N2O4
- Synonyms
- Garenoxacin
- Garénoxacine
- Garenoxacino
- Garenoxacinum
- External IDs
- BMS 284756
- BMS-284756
- BMS284756
- T 3811
- T-3811
Pharmacology
- Indication
Investigated for use/treatment in bacterial infection.
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Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Not Available
- Mechanism of action
- Not Available
- Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- 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 Garenoxacin. Aceclofenac Aceclofenac may increase the neuroexcitatory activities of Garenoxacin. Acemetacin Acemetacin may increase the neuroexcitatory activities of Garenoxacin. Acenocoumarol The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Garenoxacin. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Garenoxacin. Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Garenoxacin. Acetylsalicylic acid Acetylsalicylic acid may increase the neuroexcitatory activities of Garenoxacin. Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Garenoxacin. Acyclovir The metabolism of Acyclovir can be decreased when combined with Garenoxacin. Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Garenoxacin. 
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- Not Available
Products
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Ingredient UNII CAS InChI Key Garenoxacin mesylate OXI6EF55FR 223652-90-2 IGTHEWGRXUAFKF-NVJADKKVSA-N
Categories
- ATC Codes
- J01MA19 — Garenoxacin
- Drug Categories
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antiinfectives for Systemic Use
- Antineoplastic Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Enzyme Inhibitors
- Fluoroquinolones
- Heterocyclic Compounds, Fused-Ring
- Moderate Risk QTc-Prolonging Agents
- QTc Prolonging Agents
- Quinolines
- Quinolones
- 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
- Hydroquinolones / Hydroquinolines / Pyridinecarboxylic acids / Isoindolines / Isoindoles / Aralkylamines / Benzenoids / Vinylogous amides / Heteroaromatic compounds / Amino acids show 10 more
- Substituents
- Alkyl fluoride / Alkyl halide / Amine / Amino acid / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carboxylic acid show 24 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- V72H9867WB
- CAS number
- 194804-75-6
- InChI Key
- NJDRXTDGYFKORP-LLVKDONJSA-N
- InChI
- InChI=1S/C23H20F2N2O4/c1-11-15-5-2-12(8-13(15)9-26-11)16-6-7-17-19(21(16)31-23(24)25)27(14-3-4-14)10-18(20(17)28)22(29)30/h2,5-8,10-11,14,23,26H,3-4,9H2,1H3,(H,29,30)/t11-/m1/s1
- IUPAC Name
- 1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
- SMILES
- C[C@H]1NCC2=CC(=CC=C12)C1=CC=C2C(=O)C(=CN(C3CC3)C2=C1OC(F)F)C(O)=O
References
- General References
- Not Available
- External Links
- ChemSpider
- 110579
- ChEBI
- 131716
- ChEMBL
- CHEMBL215303
- ZINC
- ZINC000003585048
- Wikipedia
- Garenoxacin
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0232 mg/mL ALOGPS logP 1.71 ALOGPS logP 1.62 Chemaxon logS -4.3 ALOGPS pKa (Strongest Acidic) 6.05 Chemaxon pKa (Strongest Basic) 8.88 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 78.87 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 110.37 m3·mol-1 Chemaxon Polarizability 42.39 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key 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
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- This drug is a fluoroquinolone, and these agents are known to inhibit CYP1A2.
- 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
- Rodighiero V: Effects of liver disease on pharmacokinetics. An update. Clin Pharmacokinet. 1999 Nov;37(5):399-431. [Article]
- Bril F, Gonzalez CD, Di Girolamo G: Antimicrobial agents-associated with QT interval prolongation. Curr Drug Saf. 2010 Jan;5(1):85-92. [Article]
- Zhang L, Wei MJ, Zhao CY, Qi HM: Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes. Acta Pharmacol Sin. 2008 Dec;29(12):1507-14. doi: 10.1111/j.1745-7254.2008.00908.x. [Article]
Drug created at March 19, 2008 16:14 / Updated at February 21, 2021 18:52