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KETOCONAZOLE Drug Record

  • Summary
  • Interactions
  • Claims
  • KETOCONAZOLE chembl:CHEMBL157101 Approved

    Alternate Names:

    J02AB02
    DANDRAZOL
    KETOSIDIN
    KETOCONAZOLE
    KETOZOLE
    NIZORAL A-D
    DAKTARIN INTENSIV
    NIZORELLE
    XOLEGEL
    DAKTARIN GOLD
    DANDRID
    EXTINA
    NIZORAL
    KETOPINE
    PANFUNGOL
    LEVOKETOCONAZOLE
    NSC-317629
    R-41400
    SID456469
    1-[4-[4-[[2-(2,4-DICHLOROPHENYL)-2-(1H-IMIDAZOL-1-YLMETHYL)-1,3-DIOXOLAN-4-YL]METHOXY]PHENYL]-1-PIPERAZINYL]ETHANONE
    KETOCONAZOL
    KETOCONAZOLUM
    NSC 317629
    chemidplus:79156-75-5
    chembl:CHEMBL157101
    rxcui:6135
    chemidplus:65277-42-1
    pubchem.compound:3823
    drugbank:01026

    Drug Info:

    Drug Categories hormone antagonists
    Drug Categories agents causing hyperkalemia
    Drug Categories antifungals for dermatological use
    Drug Categories antifungals for topical use
    Drug Categories azole antifungals
    Drug Categories bsep/abcb11 substrates
    Drug Categories cytochrome p-450 cyp1a2 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp2a6 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp2b6 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp2c19 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (strong)
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a5 inhibitors
    Drug Categories cytochrome p-450 cyp3a5 inhibitors (strong)
    Drug Categories cytochrome p-450 cyp3a7 inhibitors
    Drug Categories cytochrome p-450 cyp3a7 inhibitors (strong)
    Drug Categories cytochrome p-450 substrates
    Drug Categories dermatologicals
    Drug Categories drugs causing inadvertant photosensitivity
    Drug Categories gynecological antiinfectives and antiseptics
    Drug Categories hepatotoxic agents
    Drug Categories imidazole and triazole derivatives
    Drug Categories oatp1b1/slco1b1 inhibitors
    Drug Categories p-glycoprotein inhibitors
    Drug Categories p-glycoprotein substrates
    Drug Categories photosensitizing agents
    Drug Categories potential qtc-prolonging agents
    Drug Categories qtc prolonging agents
    Drug Categories ugt1a1 inhibitors
    Drug Categories ugt2b7 inhibitors
    (3 More Sources)

    Publications:

    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Parker RS et al., 2004, Discovery, characterization, and significance of the cytochrome P450 omega-hydroxylase pathway of vitamin E catabolism., Ann N Y Acad Sci
    Gupta et al., 2007, Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP)., J Pharm Sci
    Reinhardt et al., 1989, Ketoconazole inhibits self-induced metabolism of 1,25-dihydroxyvitamin D3 and amplifies 1,25-dihydroxyvitamin D3 receptor up-regulation in rat osteosarcoma cells., Arch. Biochem. Biophys.
    Kamiński K et al., 2015, Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides., J Med Chem
    Łażewska D et al., 2014, Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands., Eur J Med Chem
    Kamińska K et al., 2015, (2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands., Eur J Med Chem
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Eil, 1992, Ketoconazole binds to the human androgen receptor., Horm. Metab. Res.
    Trachtenberg et al., 1988, Steroid synthesis inhibition by ketoconazole: sites of action., Clin Invest Med
    Tripathi et al., 2005, Mefloquine resistance reversal action of ketoconazole - a cytochrome P450 inhibitor, against mefloquine-resistant malaria., Parasitology
    Svecova L et al., 2008, Azole antimycotics differentially affect rifampicin-induced pregnane X receptor-mediated CYP3A4 gene expression., Drug Metab Dispos
    Li H et al., 2013, Novel yeast-based strategy unveils antagonist binding regions on the nuclear xenobiotic receptor PXR., J Biol Chem
    Dring AM et al., 2010, Rational quantitative structure-activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands., Chem Biol Interact
    Chiu et al., 2004, Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels., J. Pharmacol. Sci.
  • KETOCONAZOLE   CYP21A2

    Interaction Score: 4.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    2966691


    Sources:
    DrugBank

  • KETOCONAZOLE   CYP3A43

    Interaction Score: 0.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15991489


    Sources:
    NCI

  • KETOCONAZOLE   CYP4F2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15753130


    Sources:
    PharmGKB

  • KETOCONAZOLE   CYP17A1

    Interaction Score: 0.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    2966691


    Sources:
    DrugBank

  • KETOCONAZOLE   KCNA10

    Interaction Score: 0.31

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand None

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • KETOCONAZOLE   NR1I3

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20869355


    Sources:
    DrugBank

  • KETOCONAZOLE   ABCG2

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17518356


    Sources:
    NCI

  • KETOCONAZOLE   SNCA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   NR1I2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17998298 23525103


    Sources:
    DrugBank

  • KETOCONAZOLE   NR1H4

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   CYP3A4

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition
    Direct Interaction? False

    PMIDs:
    26052884 22931300 24996140 26360048 9187528


    Sources:
    DTC GuideToPharmacology PharmGKB

  • KETOCONAZOLE   MPHOSPH8

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   VDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2546501


    Sources:
    DTC NCI

  • KETOCONAZOLE   HSP90AA1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   KCNH2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    15272206


    Sources:
    DrugBank

  • KETOCONAZOLE   CBX1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • KETOCONAZOLE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • KETOCONAZOLE   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • KETOCONAZOLE   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • KETOCONAZOLE   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • KETOCONAZOLE   BAZ2B

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   KDM4A

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    1526623


    Sources:
    DrugBank

  • KETOCONAZOLE   NFE2L2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KETOCONAZOLE   EHMT2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB01026

    • Version: 5.1.7

    Alternate Names:
    KETOCONAZOLE DrugBank Drug Name
    65277-42-1 CAS Number
    Apo-ketoconazole Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Trachtenberg et al., 1988, Steroid synthesis inhibition by ketoconazole: sites of action., Clin Invest Med
    Li H et al., 2013, Novel yeast-based strategy unveils antagonist binding regions on the nuclear xenobiotic receptor PXR., J Biol Chem
    Svecova L et al., 2008, Azole antimycotics differentially affect rifampicin-induced pregnane X receptor-mediated CYP3A4 gene expression., Drug Metab Dispos

  • NCI: KETOCONAZOLE

    • Version: 14-September-2017

    Alternate Names:
    C605 NCI drug code

    Drug Info:

    Publications:
    Reinhardt et al., 1989, Ketoconazole inhibits self-induced metabolism of 1,25-dihydroxyvitamin D3 and amplifies 1,25-dihydroxyvitamin D3 receptor up-regulation in rat osteosarcoma cells., Arch. Biochem. Biophys.
    Tripathi et al., 2005, Mefloquine resistance reversal action of ketoconazole - a cytochrome P450 inhibitor, against mefloquine-resistant malaria., Parasitology
    Gupta et al., 2007, Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP)., J Pharm Sci

  • DTC: KETOCONAZOLE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL295698 ChEMBL Drug ID

    Drug Info:

    Publications:
    Kamińska K et al., 2015, (2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands., Eur J Med Chem
    Łażewska D et al., 2014, Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands., Eur J Med Chem
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

  • PharmGKB: ketoconazole

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Parker RS et al., 2004, Discovery, characterization, and significance of the cytochrome P450 omega-hydroxylase pathway of vitamin E catabolism., Ann N Y Acad Sci
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

  • TTD: Ketoconazole

    • Version: 2020.06.01

    Alternate Names:
    D0B4IF TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 135650454

    • Version: 29-September-2020

    Alternate Names:
    KETOCONAZOLE GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL157101

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21