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AMR Drug RepurposingSmart Screeningresearch prototype

Ketoconazole

FDA-approved product (tablet, oral), marketed as Extina, Ketoconazole, Ketozole and 3 more.

Registered studies
50+
Lab records
1
Pathogens at ≥40%
2 of 4

Chemical structure

Chemical structure of Ketoconazole
A drawing shows what the molecule is, not what it does.

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Adrenal gland disease
  • Blastomycosis
  • Cushing syndrome
  • Seborrheic dermatitis
  • Tinea
  • Tinea pedis

Indications ChEMBL records as approved, from FDA and DailyMed labels. Label ↗

WHO therapeutic group
Imidazole and triazole derivatives; Imidazole derivatives; Anticorticosteroids
FDA pharmacologic class
Azole Antifungal FDA label ↗
Anti-infective classification
Classified as another kind of anti-infective (for example an antifungal, antiviral or antiparasitic medicine).WHO ATC D01AC08; WHO ATC G01AF11; WHO ATC J02AB02; FDA class Azole Antifungal

Repurposing investigation

This medicine is being investigated here for AI-predicted antimicrobial activity against MRSA and M. tuberculosis. It was surfaced computationally for further investigation; it is not an established treatment for these infections.

AI-predicted activity

AI prediction · nothing measured
  • MRSA63.6% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • E. coli33.4% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • K. pneumoniae27.2% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • M. tuberculosis81.2% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates. This medicine was in the model's training data, so this is recall, not a new prediction.

A model’s estimate of laboratory activity against each pathogen species. It is not clinical effectiveness.

Evidence

Clinical and experimental

Documented evidence

Clinical

50+registered studies name this medicine, for any condition. The registry search keeps the first 50, so there may be more. See them below.

Experimental

  • M. tuberculosis: measured active in 1 of 1 lab record
Open Ketoconazole in ChEMBL Registered studies below
Show the 1 laboratory record, with sources

Loading records…

“Active” means the measured value reached this project’s laboratory cutoff (10 µM or stronger). A laboratory result does not show an effect in patients.

Docking

Computational · nothing measured

Dihydrofolate reductase ↗ (E. coli)

-8.6 kcal/mol

0better fit →-12

KPC-2 carbapenemase ↗ (K. pneumoniae)

-5.9 kcal/mol

0better fit →-12

Enoyl-ACP reductase (InhA) ↗ (M. tuberculosis)

-8.9 kcal/mol

0better fit →-12

Dihydrofolate reductase ↗ (MRSA)

-7.5 kcal/mol

0better fit →-12

AutoDock Vina, one experimentally solved protein per pathogen. This project’s screening target is -7.0 kcal/mol, its own mark rather than a universal cutoff. A docking score is a structural hypothesis, not proof of binding, and requires experimental validation.

Other medicines to investigate

AI prediction · nothing measured

Other repurposing candidates: approved medicines besides Ketoconazole with AI-predicted activity ≥40% against the chosen pathogen, leaving out existing antimicrobials. They are computational candidates for further investigation, not alternatives and not recommendations.

Sorted by AI-predicted activity, high to low. The order is not a ranking of which medicine is better.

Registered studies

A registration describes a study; it does not establish a positive result.

  • Study To Determine The Effect Of Food And Strong CYP3A4 Enzyme Inhibitor On PF-04449913 Drug Levels

    NCT01749085 · start 2012-12

    Registered record
    Registry ID
    NCT01749085
    Conditions
    Healthy Volunteers
    Interventions
    PF-04449913, ketoconazole; PF-04449913, ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2012-12
    Completion
    2013-02
    Enrolment
    14

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Volunteers
    InterventionPF-04449913, ketoconazole; PF-04449913, ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • Effect of Ketoconazole on Sufentanil NanoTab Pharmacokinetics

    NCT01721070 · start 2012-11

    Registered record
    Registry ID
    NCT01721070
    Conditions
    Pharmacokinetics
    Interventions
    Sufentanil NanoTab (SUF NT) 15 mcg; Ketoconazole 400 mg, sufentanil NanoTab (SUF NT) 15 mcg
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2012-11
    Completion
    2012-12
    Enrolment
    19

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPharmacokinetics
    InterventionSufentanil NanoTab (SUF NT) 15 mcg; Ketoconazole 400 mg, sufentanil NanoTab (SUF NT) 15 mcg
    PhasePhase 1
    Registry statusCompleted

  • Pharmacokinetics Study of Oral IXAZOMIB in Participants With Advanced Nonhematologic Malignancies or Lymphoma

    NCT01454076 · start 2011-11-10

    Registered record
    Registry ID
    NCT01454076
    Conditions
    Nonhematologic Malignancies; Lymphoma
    Interventions
    Ixazomib 2.5 mg; Ixazomib 4 mg Capsule A; Ixazomib 4 mg Capsule B; Ketoconazole; Rifampin; Clarithromycin; Ixazomib 4 mg Capsule B
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2011-11-10
    Completion
    2016-06-16
    Enrolment
    112

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionNonhematologic Malignancies; Lymphoma
    InterventionIxazomib 2.5 mg; Ixazomib 4 mg Capsule A; Ixazomib 4 mg Capsule B; Ketoconazole +3 more
    PhasePhase 1
    Registry statusCompleted

  • A Study To Estimate The Effect Of Ketoconazole On The Pharmacokinetics Of Pf-04937319 In Healthy Subjects

    NCT01468714 · start 2011-10

    Registered record
    Registry ID
    NCT01468714
    Conditions
    Human Volunteers
    Interventions
    PF-04937319 / ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2011-10
    Completion
    2011-10
    Enrolment
    10

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHuman Volunteers
    InterventionPF-04937319 / ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • A Drug-Drug Interaction Study of Ketoconazole, Rifampicin and Ritonavir-Boosted Atazanavir With Single-Dose RO5093151 in Healthy Volunteers

    NCT01591850 · start 2011-09

    Registered record
    Registry ID
    NCT01591850
    Conditions
    Healthy Volunteer
    Interventions
    RO5093151; atazanavir; ketoconazole; rifampicin; ritonavir
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2011-09
    Completion
    2011-11
    Enrolment
    51

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Volunteer
    InterventionRO5093151; atazanavir; ketoconazole; rifampicin +1 more
    PhasePhase 1
    Registry statusCompleted

  • A Phase 1 Study to Evaluate The Effect of Ketoconazole on the Pharmacokinetics of Tivozanib in Healthy Subjects

    NCT01363778 · start 2011-05

    Registered record
    Registry ID
    NCT01363778
    Conditions
    Healthy
    Interventions
    tivozanib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2011-05
    Completion
    2011-07
    Enrolment
    30

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy
    Interventiontivozanib
    PhasePhase 1
    Registry statusCompleted

  • A Pharmacokinetic Study to Assess the Influence of Simultaneous CYP3A4 and P-glycoprotein Inhibition on E7080 Pharmacokinetics Following Single Dose Oral Administration of 5 mg E7080 to Healthy Volunteers

    NCT02198170 · start 2011-02

    Registered record
    Registry ID
    NCT02198170
    Conditions
    Healthy Volunteers
    Interventions
    ketoconazole-placebo; placebo-ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2011-02
    Completion
    2011-06
    Enrolment
    18

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Volunteers
    Interventionketoconazole-placebo; placebo-ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • ITT4 Intratesticular Hormonal Milieu in Man (ITT4)

    NCT01215292 · start 2011-01

    Registered record
    Registry ID
    NCT01215292
    Conditions
    Healthy Males
    Interventions
    Acyline; Testosterone gel; ketoconazole 400; Ketoconazole 800; Dutasteride; Anastrozole; Placebo ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1 / Phase 2
    Registry status
    Completed
    Start
    2011-01
    Completion
    2012-03
    Enrolment
    46

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Males
    InterventionAcyline; Testosterone gel; ketoconazole 400; Ketoconazole 800 +3 more
    PhasePhase 1 / Phase 2
    Registry statusCompleted

  • A Study to Determine the Relative Bioavailability of a Tablet Formulation of GDC-0941 and the Effect of Ketoconazole on the Pharmacokinetics of the GDC-0941 Tablet

    NCT01240226 · start 2010-11

    Registered record
    Registry ID
    NCT01240226
    Conditions
    Healthy Volunteer
    Interventions
    GDC-0941; GDC-0941; ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-11
    Completion
    2010-12
    Enrolment
    22

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Volunteer
    InterventionGDC-0941; GDC-0941; ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • A Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of Linifanib (ABT-869)

    NCT01114191 · start 2010-05

    Registered record
    Registry ID
    NCT01114191
    Conditions
    Solid Tumors
    Interventions
    ABT-869; ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-05
    Completion
    2011-02
    Enrolment
    12

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionSolid Tumors
    InterventionABT-869; ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • A Study to Evaluate the Relative Bioavailability, Food Effect and Effect of Ketoconazole on the Rate and Extent of Absorption of Solid Dosage Formulation(s) of JNJ-40411813

    NCT01932320 · start 2010-02

    Registered record
    Registry ID
    NCT01932320
    Conditions
    Healthy
    Interventions
    JNJ-40411813: Formulation A; JNJ-40411813: Formulation B; JNJ-40411813: Formulation C; Ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-02
    Completion
    2010-05
    Enrolment
    36

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy
    InterventionJNJ-40411813: Formulation A; JNJ-40411813: Formulation B; JNJ-40411813: Formulation C; Ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • Trial for Studying Pharmacokinetic Effects of Ketoconazole on CG100649

    NCT01154764 · start 2009-10

    Registered record
    Registry ID
    NCT01154764
    Conditions
    Healthy
    Interventions
    CG100649; Ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2009-10
    Completion
    2010-12
    Enrolment
    28

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy
    InterventionCG100649; Ketoconazole
    PhasePhase 1
    Registry statusCompleted

  • Validation Study of Multiple Probe Compounds for Drug Interaction Evaluation

    NCT00964106 · start 2009-08-26

    Registered record
    Registry ID
    NCT00964106
    Conditions
    Drug Interactions
    Interventions
    Caffeine; Rosiglitazone; Flurbiprofen; Omeprazole; Dextromethorphan; Midazolam; Rosuvastatin; Ketoconazole; Fluconazole; Rifampin; Rosiglitazone
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2009-08-26
    Completion
    2011-08-29
    Enrolment
    87

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionDrug Interactions
    InterventionCaffeine; Rosiglitazone; Flurbiprofen; Omeprazole +7 more
    PhasePhase 1
    Registry statusCompleted

  • Study Evaluating The Effect of Bosutinib (SKI-606) On Cardiac Repolarization (Rhythms Of The Heart)

    NCT00914121 · start 2009-06

    Registered record
    Registry ID
    NCT00914121
    Conditions
    Healthy Subjects
    Interventions
    SKI-606; Placebo; Moxifloxacin
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2009-06
    Completion
    2009-08
    Enrolment
    60

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Subjects
    InterventionSKI-606; Placebo; Moxifloxacin
    PhasePhase 1
    Registry statusCompleted

  • Relative Bioavailability of Single Doses of Dabigatran Etexilate When Administered Alone or in Combination With a Single Dose of Ketoconazole or in Combination With q.d. Ketoconazole at Steady State in Healthy Male and Female Volunteers

    NCT02170675 · start 2009-06

    Registered record
    Registry ID
    NCT02170675
    Conditions
    Healthy
    Interventions
    Dabigatran etexilate; Ketoconazole
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2009-06
    Completion
    Not recorded
    Enrolment
    24

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy
    InterventionDabigatran etexilate; Ketoconazole
    PhasePhase 1
    Registry statusCompleted