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AMR Drug RepurposingSmart Screeningresearch prototype

Tolbutamide

FDA-approved product (tablet, oral), marketed as Orinase, Tolbutamide, Orinase Diagnostic.

Registered studies
34
Lab records
0
Pathogens at ≥40%
1 of 4

Chemical structure

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

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Diabetes mellitus
  • Type 2 diabetes mellitus

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

WHO therapeutic group
Sulfonylureas; Tests for diabetes
Anti-infective classification
Not classified as an anti-infective.

Repurposing investigation

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

AI-predicted activity

AI prediction · nothing measured
  • MRSA31.9% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • E. coli20.5% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • K. pneumoniae8.8% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • M. tuberculosis49.3% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.

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

Evidence

Clinical and experimental

Documented evidence

Clinical

34registered studies name this medicine, for any condition. See them below.

Experimental

No evidence found

No laboratory measurement against the four pathogens in the ChEMBL records loaded here.

Open Tolbutamide in ChEMBL Registered studies below

Docking

Computational · nothing measured

Dihydrofolate reductase ↗ (E. coli)

-7.0 kcal/mol

0better fit →-12

KPC-2 carbapenemase ↗ (K. pneumoniae)

-7.0 kcal/mol

0better fit →-12

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

-7.2 kcal/mol

0better fit →-12

Dihydrofolate reductase ↗ (MRSA)

-7.0 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 Tolbutamide 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.

  • A PHASE 1, OPEN-LABEL, CROSS-OVER, FIXED SEQUENCE STUDY TO EVALUATE THE EFFECT OF MULTIPLE DOSES OF DS-1971A ON THE SINGLE DOSE PHARMACOKINETICS OF PROBE SUBSTRATES FOR CYP2B6, CYP2C8, CYP2C9, CYP2C19 AND CYP3A4 ENZYMES IN HEALTHY MALE AND FEMALE SUBJECTS

    NCT02473627 · start 2015-05

    Registered record
    Registry ID
    NCT02473627
    Conditions
    Healthy
    Interventions
    DS-1971a; midazolam hydrochloride; Omeprazole; Pioglitazone hydrochloride; Buproprion; Tolbutamide
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2015-05
    Completion
    2015-07
    Enrolment
    18

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

    ConditionHealthy
    InterventionDS-1971a; midazolam hydrochloride; Omeprazole; Pioglitazone hydrochloride +2 more
    PhasePhase 1
    Registry statusCompleted

  • Evaluation of CYP450 Activities in Diabetic Patients vs. Non-diabetic Subjects

    NCT02291666 · start 2015-04

    Registered record
    Registry ID
    NCT02291666
    Conditions
    Type 2 Diabetes
    Interventions
    CRCHUM-MT cocktail
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2015-04
    Completion
    2019-07
    Enrolment
    73

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

    ConditionType 2 Diabetes
    InterventionCRCHUM-MT cocktail
    PhasePhase 4
    Registry statusCompleted

  • A Study to Assess Effect of JNJ-54861911 on Pharmacokinetics of Cocktail Representatives for Cytochrome P450 (CYP) 3A4, CYP2B6, CYP2C9, and CYP1A2 Substrates

    NCT02211079 · start 2014-09

    Registered record
    Registry ID
    NCT02211079
    Conditions
    Healthy
    Interventions
    JNJ-54861911; Caffeine; Midazolam; Tolbutamide
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2014-09
    Completion
    2014-11
    Enrolment
    16

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

    ConditionHealthy
    InterventionJNJ-54861911; Caffeine; Midazolam; Tolbutamide
    PhasePhase 1
    Registry statusCompleted

  • Incretin-based Drugs and the Risk of Heart Failure

    NCT02456428 · start 2014-03

    Registered record
    Registry ID
    NCT02456428
    Conditions
    Type 2 Diabetes Mellitus
    Interventions
    DPP-4 inhibitors; GLP-1 analogs; Insulins; Biguanides; Sulfonylureas; Thiazolidinediones; Alpha-glucosidase inhibitors; Meglitinides
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2014-03
    Completion
    2015-05
    Enrolment
    1,499,650

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

    ConditionType 2 Diabetes Mellitus
    InterventionDPP-4 inhibitors; GLP-1 analogs; Insulins; Biguanides +4 more
    PhaseNot recorded
    Registry statusCompleted

  • Incretin-based Drugs and Pancreatic Cancer

    NCT02475499 · start 2014-03

    Registered record
    Registry ID
    NCT02475499
    Conditions
    Diabetes Mellitus, Type 2
    Interventions
    DPP-4 inhibitors; GLP-1 analogs; Sulfonylureas; Biguanides; Thiazolidinediones; Alpha-glucosidase inhibitors; Meglitinides
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2014-03
    Completion
    2015-04
    Enrolment
    886,172

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

    ConditionDiabetes Mellitus, Type 2
    InterventionDPP-4 inhibitors; GLP-1 analogs; Sulfonylureas; Biguanides +3 more
    PhaseNot recorded
    Registry statusCompleted

  • Incretin-based Drugs and Acute Pancreatitis

    NCT02476760 · start 2014-03

    Registered record
    Registry ID
    NCT02476760
    Conditions
    Diabetes Mellitus, Type 2
    Interventions
    DPP-4 inhibitors; GLP-1 analogs; Insulins; Biguanides; Sulfonylureas; Thiazolidinediones; Alpha-glucosidase inhibitors; Meglitinides
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2014-03
    Completion
    2015-04
    Enrolment
    1,417,914

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

    ConditionDiabetes Mellitus, Type 2
    InterventionDPP-4 inhibitors; GLP-1 analogs; Insulins; Biguanides +4 more
    PhaseNot recorded
    Registry statusCompleted

  • Drug Drug Interaction Study Between BI 201335 and BI 207127 in Chronic Hepatitis C Infected Patients

    NCT01525628 · start 2012-04

    Registered record
    Registry ID
    NCT01525628
    Conditions
    Hepatitis C, Chronic
    Interventions
    midazolam; BI 201335; tenofovir; caffeine; tolbutamide; tolbutamide; midazolam; caffeine; pegylated interferon; BI 201335; BI 201335; BI 207127; BI 207127; BI 201335; BI 207127; ribavirin; ribavirin; ribavirin; pegylated interferon; ribavirin; caffeine; tolbutamide; BI 207127; midazolam; BI 201335; BI 207127; ribavirin
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2012-04
    Completion
    2014-10
    Enrolment
    72

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

    ConditionHepatitis C, Chronic
    Interventionmidazolam; BI 201335; tenofovir; caffeine +23 more
    PhasePhase 1
    Registry statusCompleted

  • Open Label, Single Dose, Non-randomized Study to Assess the Drug to Drug Interaction of Briakinumab on CYP Substrates.

    NCT01260844 · start 2011-04

    Registered record
    Registry ID
    NCT01260844
    Conditions
    Moderate to Severe Plaque Psoriasis
    Interventions
    briakinumab
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Withdrawn
    Start
    2011-04
    Completion
    Not recorded
    Enrolment
    12

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

    ConditionModerate to Severe Plaque Psoriasis
    Interventionbriakinumab
    PhasePhase 1
    Registry statusWithdrawn

  • Gamma-Secretase/Notch Signalling Pathway Inhibitor RO4929097 in Treating Patients With Advanced Solid Tumors

    NCT01218620 · start 2010-09

    Registered record
    Registry ID
    NCT01218620
    Conditions
    Adult Solid Neoplasm
    Interventions
    Gamma-Secretase Inhibitor RO4929097; Ketoconazole; Rifampin; Midazolam Hydrochloride; Omeprazole; Tolbutamide; Dextromethorphan Hydrobromide; Pharmacological Study; Laboratory Biomarker Analysis
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-09
    Completion
    2014-12
    Enrolment
    17

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

    ConditionAdult Solid Neoplasm
    InterventionGamma-Secretase Inhibitor RO4929097; Ketoconazole; Rifampin; Midazolam Hydrochloride +5 more
    PhasePhase 1
    Registry statusCompleted

  • Pharmacokinetic Study to Characterize Individual Metabolic Profile

    NCT01188525 · start 2010-08

    Registered record
    Registry ID
    NCT01188525
    Conditions
    Healthy Volunteers
    Interventions
    10 parents drugs adminstration
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-08
    Completion
    2011-07
    Enrolment
    10

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

    ConditionHealthy Volunteers
    Intervention10 parents drugs adminstration
    PhasePhase 1
    Registry statusCompleted

  • A Pharmacokinetic Evaluation of Metformin in Relation to the Polymorphism A270S in Healthy Caucasian Volunteers

    NCT01237522 · start 2010-08

    Registered record
    Registry ID
    NCT01237522
    Conditions
    Metformin; Organic Cation Transporter 2; Polymorphism,Single Nucleotide
    Interventions
    Metformin
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2010-08
    Completion
    2010-12
    Enrolment
    50

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

    ConditionMetformin; Organic Cation Transporter 2; Polymorphism,Single Nucleotide
    InterventionMetformin
    PhasePhase 4
    Registry statusCompleted

  • A Drug Interaction Study of Tasisulam in Patients With Advanced Cancer or Lymphoma

    NCT01185548 · start 2010-07

    Registered record
    Registry ID
    NCT01185548
    Conditions
    Lymphoma; Advanced Cancer
    Interventions
    Tolbutamide; Tasisulam
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Terminated
    Start
    2010-07
    Completion
    2010-12
    Enrolment
    4

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

    ConditionLymphoma; Advanced Cancer
    InterventionTolbutamide; Tasisulam
    PhasePhase 1
    Registry statusTerminated

  • A Pharmacokinetic and Drug Interaction Study of JNJ-26489112 in Healthy Volunteers

    NCT01147887 · start 2010-06

    Registered record
    Registry ID
    NCT01147887
    Conditions
    Healthy
    Interventions
    Drug combination/ 26489112
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-06
    Completion
    2010-08
    Enrolment
    20

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

    ConditionHealthy
    InterventionDrug combination/ 26489112
    PhasePhase 1
    Registry statusCompleted

  • To Compare the Effect of a Subcutaneous Canakinumab Administration to Placebo in Patients With Impaired Glucose Tolerance or Patients With Type 2 Diabetes With Differing Baseline Diabetes Therapies

    NCT01068860 · start 2010-02

    Registered record
    Registry ID
    NCT01068860
    Conditions
    Type 2 Diabetes Mellitus; Impaired Glucose Tolerance
    Interventions
    Canakinumab 150 mg; Placebo to Canakinumab
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2010-02
    Completion
    2010-08
    Enrolment
    246

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

    ConditionType 2 Diabetes Mellitus; Impaired Glucose Tolerance
    InterventionCanakinumab 150 mg; Placebo to Canakinumab
    PhasePhase 2
    Registry statusCompleted

  • Effects of Genotype on CYP2C9 Drug Interactions

    NCT01061112 · start 2009-12

    Registered record
    Registry ID
    NCT01061112
    Conditions
    Healthy
    Interventions
    Flurbiprofen Control - Flurbiprofen Only; Flurbiprofen Inhibition - Flurbiprofen & Fluconazole; Ketoprofen Control - Ketoprofen Only; Ketoprofen Inhibition - Ketoprofen & Fluconazole; Tolbutamide Control - Tolbutamide Only; Tolbutamide Inhibition - Tolbutamide & Fluconazole
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2009-12
    Completion
    2014-06
    Enrolment
    23

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

    ConditionHealthy
    InterventionFlurbiprofen Control - Flurbiprofen Only; Flurbiprofen Inhibition - Flurbiprofen & Fluconazole; Ketoprofen Control - Ketoprofen Only; Ketoprofen Inhibition - Ketoprofen & Fluconazole +2 more
    PhaseNot recorded
    Registry statusCompleted