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AMR Drug RepurposingSmart Screeningresearch prototype

Linezolid

FDA-approved product (tablet, oral), marketed as Linezolid, Linezolid In Sodium Chloride 0.9% In Plastic Container, Zyvox.

Registered studies
50+
Lab records
63
Pathogens at ≥40%
2 of 4

Chemical structure

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

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Bacterial disease
  • Bacteriemia
  • Infection
  • Osteomyelitis
  • Pneumonia

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

WHO therapeutic group
Other antibacterials
FDA pharmacologic class
Oxazolidinone Antibacterial FDA label ↗
Anti-infective classification
Classified as an existing antimicrobial.WHO ATC J01XX08; FDA class Oxazolidinone Antibacterial

Repurposing investigation

Linezolid is already an antimicrobial, so it is not counted among the repurposing candidates. Its AI-predicted activity is shown below for reference.

AI-predicted activity

AI prediction · nothing measured
  • MRSA89.6% 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.
  • E. coli1.0% AI-predicted activityBelow 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.
  • K. pneumoniae27.4% AI-predicted activityBelow 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.
  • M. tuberculosis82.4% 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

  • MRSA: measured active in 39 of 44 lab records
  • E. coli: measured active in 1 of 4 lab records
  • K. pneumoniae: measured active in 2 of 8 lab records
  • M. tuberculosis: measured active in 5 of 7 lab records
Open Linezolid in ChEMBL Registered studies below
Show the 63 laboratory records, 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)

-7.0 kcal/mol

0better fit →-12

KPC-2 carbapenemase ↗ (K. pneumoniae)

-7.5 kcal/mol

0better fit →-12

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

-7.7 kcal/mol

0better fit →-12

Dihydrofolate reductase ↗ (MRSA)

-7.4 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 Linezolid 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.

  • Susceptibility Testing of Biofilm to Guide Treatment of Periprosthetic Joint Infections

    NCT04488458 · start 2021-08-15

    Registered record
    Registry ID
    NCT04488458
    Conditions
    Prosthetic Joint Infection; Prosthetic Infection; Hip Prosthesis Infection; Knee Prosthesis Infection
    Interventions
    MIC or MBEC+MIC based treatment algorithm
    Study type
    INTERVENTIONAL
    Phase
    Not applicable
    Registry status
    Unknown
    Start
    2021-08-15
    Completion
    2023-12-31
    Enrolment
    40

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

    ConditionProsthetic Joint Infection; Prosthetic Infection; Hip Prosthesis Infection; Knee Prosthesis Infection
    InterventionMIC or MBEC+MIC based treatment algorithm
    PhaseNot applicable
    Registry statusUnknown

  • Intensified Tuberculosis Treatment to Reduce the Mortality of Patients With Tuberculous Meningitis

    NCT04145258 · start 2021-02-07

    Registered record
    Registry ID
    NCT04145258
    Conditions
    Tuberculous Meningitis
    Interventions
    Aspirin; Placebo of aspirin; WHO TBM treatment; Intensified TBM treatment
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Recruiting
    Start
    2021-02-07
    Completion
    2026-09-26
    Enrolment
    768

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

    ConditionTuberculous Meningitis
    InterventionAspirin; Placebo of aspirin; WHO TBM treatment; Intensified TBM treatment
    PhasePhase 3
    Registry statusRecruiting

  • Economic Evaluation of New MDR TB Regimens

    NCT04207112 · start 2020-10-20

    Registered record
    Registry ID
    NCT04207112
    Conditions
    Multi-drug Resistant Tuberculosis; Extensively Drug-Resistant Tuberculosis; Pulmonary Tuberculoses
    Interventions
    Bedaquiline; Pretomanid; Moxifloxacin; Linezolid; Clofazimine; Standard Drugs
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Completed
    Start
    2020-10-20
    Completion
    2022-08-25
    Enrolment
    73

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

    ConditionMulti-drug Resistant Tuberculosis; Extensively Drug-Resistant Tuberculosis; Pulmonary Tuberculoses
    InterventionBedaquiline; Pretomanid; Moxifloxacin; Linezolid +2 more
    PhasePhase 2 / Phase 3
    Registry statusCompleted

  • Building Evidence for Advancing New Treatment for Rifampicin Resistant Tuberculosis (RR-TB) Comparing a Short Course of Treatment (Containing Bedaquiline, Delamanid and Linezolid) With the Current South African Standard of Care

    NCT04062201 · start 2019-08-22

    Registered record
    Registry ID
    NCT04062201
    Conditions
    Tuberculosis; Pre-XDR-TB; Extensively Drug-Resistant Tuberculosis; Multi Drug Resistant Tuberculosis; Rifampicin Resistant Tuberculosis
    Interventions
    Bedaquiline Oral Tablet; Linezolid Oral Tablet; Delamanid in Oral Dosage Form; Clofazimine Oral Product; Levofloxacin Oral Tablet; Isoniazid Oral Product; Ethambutol Oral Product; Pyrazinamide Oral Product; Linezolid Oral Tablet; Clofazimine Oral Product; Levofloxacin Oral Tablet
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2019-08-22
    Completion
    2024-04-15
    Enrolment
    402

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

    ConditionTuberculosis; Pre-XDR-TB; Extensively Drug-Resistant Tuberculosis; Multi Drug Resistant Tuberculosis +1 more
    InterventionBedaquiline Oral Tablet; Linezolid Oral Tablet; Delamanid in Oral Dosage Form; Clofazimine Oral Product +7 more
    PhasePhase 3
    Registry statusCompleted

  • The Effect of 18-month Regimen Containing 6 Anti-tuberculosis Drugs for Patients With MDR-TB

    NCT03830671 · start 2019-03-08

    Registered record
    Registry ID
    NCT03830671
    Conditions
    Multi-drug Resistant Tuberculosis
    Interventions
    18-month regimen containing 6 anti-TB drugs
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2019-03-08
    Completion
    2022-06-08
    Enrolment
    515

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

    ConditionMulti-drug Resistant Tuberculosis
    Intervention18-month regimen containing 6 anti-TB drugs
    PhasePhase 4
    Registry statusCompleted

  • Study to Assess Safety, Tolerability and Efficacy of Afabicin in The Treatment of Participants With Bone or Joint Infection Due to Staphylococcus

    NCT03723551 · start 2019-02-20

    Registered record
    Registry ID
    NCT03723551
    Conditions
    Bone or Joint Infection
    Interventions
    Afabicin; Cefazolin; Vancomycin; Linezolid; Clindamycin
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2019-02-20
    Completion
    2025-04-23
    Enrolment
    67

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

    ConditionBone or Joint Infection
    InterventionAfabicin; Cefazolin; Vancomycin; Linezolid +1 more
    PhasePhase 2
    Registry statusTerminated

  • Population Pharmacokinetics of Meropenem and Linezolid in Children With Severe Infectious Diseases

    NCT03643497 · start 2018-07-01

    Registered record
    Registry ID
    NCT03643497
    Conditions
    Children；Infection
    Interventions
    anti-infective drugs
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Unknown
    Start
    2018-07-01
    Completion
    2021-12-31
    Enrolment
    800

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

    ConditionChildren；Infection
    Interventionanti-infective drugs
    PhaseNot recorded
    Registry statusUnknown

  • Comparative Study To Determine The Efficacy, Safety, And Tolerability Of Ceftolozane-Tazobactam

    NCT03485950 · start 2018-05-16

    Registered record
    Registry ID
    NCT03485950
    Conditions
    Other Infectious Diseases
    Interventions
    Cefepime; Ceftolozane; Laboratory Biomarker Analysis; Meropenem; Piperacillin-Tazobactam; Tazobactam
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2018-05-16
    Completion
    2022-02-16
    Enrolment
    100

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

    ConditionOther Infectious Diseases
    InterventionCefepime; Ceftolozane; Laboratory Biomarker Analysis; Meropenem +2 more
    PhasePhase 2
    Registry statusCompleted

  • Linezolid in Healthy Volunteers

    NCT03841721 · start 2018-05-01

    Registered record
    Registry ID
    NCT03841721
    Conditions
    Healthy
    Interventions
    Linezolid oral tablet 300 mg/day for 5 day
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Unknown
    Start
    2018-05-01
    Completion
    2019-12-31
    Enrolment
    30

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

    ConditionHealthy
    InterventionLinezolid oral tablet 300 mg/day for 5 day
    PhasePhase 1
    Registry statusUnknown

  • Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis

    NCT03474198 · start 2018-03-21

    Registered record
    Registry ID
    NCT03474198
    Conditions
    Tuberculosis, Pulmonary
    Interventions
    Rifampicin; Isoniazid; Pyrazinamide; Ethambutol; Linezolid; Clofazimine; Rifapentine; Levofloxacin; Bedaquiline; Rifampicin
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Completed
    Start
    2018-03-21
    Completion
    2022-01-20
    Enrolment
    675

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

    ConditionTuberculosis, Pulmonary
    InterventionRifampicin; Isoniazid; Pyrazinamide; Ethambutol +6 more
    PhasePhase 2 / Phase 3
    Registry statusCompleted

  • Clinical Study of Cefiderocol (S-649266) for the Treatment of Nosocomial Pneumonia Caused by Gram-negative Pathogens

    NCT03032380 · start 2017-10-24

    Registered record
    Registry ID
    NCT03032380
    Conditions
    Healthcare-associated Pneumonia (HCAP); Hospital Acquired Pneumonia (HAP); Ventilator Associated Pneumonia (VAP)
    Interventions
    Cefiderocol; Meropenem; Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2017-10-24
    Completion
    2019-04-01
    Enrolment
    300

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

    ConditionHealthcare-associated Pneumonia (HCAP); Hospital Acquired Pneumonia (HAP); Ventilator Associated Pneumonia (VAP)
    InterventionCefiderocol; Meropenem; Linezolid
    PhasePhase 3
    Registry statusCompleted

  • Plasma and Lung Tissue Concentrations of Linezolid in Septic Shock Patients

    NCT03308227 · start 2017-10-20

    Registered record
    Registry ID
    NCT03308227
    Conditions
    Septic Shock
    Interventions
    Not recorded
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Unknown
    Start
    2017-10-20
    Completion
    2018-04-30
    Enrolment
    46

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

    ConditionSeptic Shock
    InterventionNot recorded
    PhaseNot recorded
    Registry statusUnknown

  • Comparative Study of Levonadifloxacin (IV and Oral) With Linezolid (IV and Oral) in Acute Bacterial Skin and Skin Structure Infections (ABSSSI)

    NCT03405064 · start 2017-08-25

    Registered record
    Registry ID
    NCT03405064
    Conditions
    Acute Bacterial Skin and Skin Structure Infections
    Interventions
    Oral Levonadifloxacin/Linezolid Tablet; Intravenous Levonadifloxacin/Linezolid Infusion
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2017-08-25
    Completion
    2018-11-30
    Enrolment
    501

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

    ConditionAcute Bacterial Skin and Skin Structure Infections
    InterventionOral Levonadifloxacin/Linezolid Tablet; Intravenous Levonadifloxacin/Linezolid Infusion
    PhasePhase 3
    Registry statusCompleted

  • Pragmatic Clinical Trial for a More Effective Concise and Less Toxic MDR-TB Treatment Regimen(s)

    NCT02589782 · start 2017-01

    Registered record
    Registry ID
    NCT02589782
    Conditions
    Tuberculosis, Multidrug-Resistant; Extensively Drug-Resistant Tuberculosis; Tuberculosis, Pulmonary
    Interventions
    Bedaquiline; Pretomanid; Moxifloxacin; Linezolid; Clofazimine; Locally accepted standard of care which is consistent with the WHO recommendations for the treatment of M/XDR-TB.
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Completed
    Start
    2017-01
    Completion
    2022-08-05
    Enrolment
    552

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

    ConditionTuberculosis, Multidrug-Resistant; Extensively Drug-Resistant Tuberculosis; Tuberculosis, Pulmonary
    InterventionBedaquiline; Pretomanid; Moxifloxacin; Linezolid +2 more
    PhasePhase 2 / Phase 3
    Registry statusCompleted

  • Treatment Shortening of MDR-TB Using Existing and New Drugs

    NCT02619994 · start 2016-01

    Registered record
    Registry ID
    NCT02619994
    Conditions
    Tuberculosis, Multidrug-Resistant
    Interventions
    Linezolid; Delamanid; Levofloxacin; Pyrazinamide; Locally-used WHO-approved MDR-TB regimen in Korea
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2016-01
    Completion
    2021-06
    Enrolment
    214

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

    ConditionTuberculosis, Multidrug-Resistant
    InterventionLinezolid; Delamanid; Levofloxacin; Pyrazinamide +1 more
    PhasePhase 2
    Registry statusCompleted