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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.

  • An Open-label RCT to Evaluate a New Treatment Regimen for Patients With Multi-drug Resistant Tuberculosis

    NCT02454205 · start 2015-11-12

    Registered record
    Registry ID
    NCT02454205
    Conditions
    Tuberculosis; Multidrug Resistant Tuberculosis; Extensively-drug Resistant Tuberculosis
    Interventions
    Linezolid; Bedaquiline; Levofloxacin; Pyrazinamide; Isoniazid; Ethionamide; Terizidone; Moxifloxacin; Kanamycin
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Completed
    Start
    2015-11-12
    Completion
    2021-08-30
    Enrolment
    154

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

    ConditionTuberculosis; Multidrug Resistant Tuberculosis; Extensively-drug Resistant Tuberculosis
    InterventionLinezolid; Bedaquiline; Levofloxacin; Pyrazinamide +5 more
    PhasePhase 2 / Phase 3
    Registry statusCompleted

  • Safety and Efficacy of BAY1192631 in Japanese Patients With Methicillin-resistant Staphylococcus Aureus (MRSA) Infections

    NCT01967225 · start 2013-11-23

    Registered record
    Registry ID
    NCT01967225
    Conditions
    Skin Diseases, Infectious
    Interventions
    Tedizolid Phosphate (Sivextro, BAY1192631); Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2013-11-23
    Completion
    2016-10-28
    Enrolment
    125

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

    ConditionSkin Diseases, Infectious
    InterventionTedizolid Phosphate (Sivextro, BAY1192631); Linezolid
    PhasePhase 3
    Registry statusCompleted

  • Pharmacokinetic and Pharmacodynamic Evaluation of Linezolid Administered Intravenously in MRSA-positive, Morbidly Obese Patients With Pneumonia

    NCT01805284 · start 2013-02

    Registered record
    Registry ID
    NCT01805284
    Conditions
    Pneumonia
    Interventions
    Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2013-02
    Completion
    2016-09-30
    Enrolment
    15

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

    ConditionPneumonia
    InterventionLinezolid
    PhasePhase 4
    Registry statusCompleted

  • Safety and Efficacy of CEM-102 With Rifampin Compared to Standard Therapy in Patients With Prosthetic Joint Infections or Spacer Infection

    NCT01756924 · start 2012-12

    Registered record
    Registry ID
    NCT01756924
    Conditions
    Prosthetic Joint Infections of Hip; Prosthetic Joint Infections of Knee; Infected Spacers
    Interventions
    CEM-102; IV or Oral standard of care antibiotics; Rifampin
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2012-12
    Completion
    2014-07
    Enrolment
    14

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

    ConditionProsthetic Joint Infections of Hip; Prosthetic Joint Infections of Knee; Infected Spacers
    InterventionCEM-102; IV or Oral standard of care antibiotics; Rifampin
    PhasePhase 2
    Registry statusTerminated

  • Safety and Efficacy Study of Ceftaroline Versus a Comparator in Pediatric Subjects With Complicated Community Acquired Pneumonia (CABP)

    NCT01669980 · start 2012-10

    Registered record
    Registry ID
    NCT01669980
    Conditions
    Infections; Pneumonia
    Interventions
    Ceftaroline fosamil; IV Ceftriaxone and Vancomycin
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2012-10
    Completion
    2014-08
    Enrolment
    40

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

    ConditionInfections; Pneumonia
    InterventionCeftaroline fosamil; IV Ceftriaxone and Vancomycin
    PhasePhase 4
    Registry statusCompleted

  • Effect of Linezolid on Ex Vivo Neutrophil and Monocyte Function in Healthy Males

    NCT01544673 · start 2012-03

    Registered record
    Registry ID
    NCT01544673
    Conditions
    Gram Positive Infection
    Interventions
    linezolid; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2012-03
    Completion
    2012-04
    Enrolment
    18

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

    ConditionGram Positive Infection
    Interventionlinezolid; Placebo
    PhasePhase 1
    Registry statusCompleted

  • Asymptomatic Colonization With S. Aureus After Therapy With Linezolid or Clindamycin for Acute Skin Infections

    NCT01619410 · start 2012-01

    Registered record
    Registry ID
    NCT01619410
    Conditions
    Skin Diseases, Bacterial; Abscess
    Interventions
    Linezolid; Clindamycin
    Study type
    INTERVENTIONAL
    Phase
    Not applicable
    Registry status
    Terminated
    Start
    2012-01
    Completion
    2016-12
    Enrolment
    25

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

    ConditionSkin Diseases, Bacterial; Abscess
    InterventionLinezolid; Clindamycin
    PhaseNot applicable
    Registry statusTerminated

  • TR-701 FA vs Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections

    NCT01421511 · start 2011-09-15

    Registered record
    Registry ID
    NCT01421511
    Conditions
    Skin and Subcutaneous Tissue Bacterial Infections
    Interventions
    TR-701 FA; Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2011-09-15
    Completion
    2013-01-10
    Enrolment
    666

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

    ConditionSkin and Subcutaneous Tissue Bacterial Infections
    InterventionTR-701 FA; Linezolid
    PhasePhase 3
    Registry statusCompleted

  • Pharmacokinetics of Linezolid in Children With Cystic Fibrosis

    NCT00625703 · start 2010-12

    Registered record
    Registry ID
    NCT00625703
    Conditions
    Cystic Fibrosis
    Interventions
    Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2010-12
    Completion
    2011-05
    Enrolment
    45

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

    ConditionCystic Fibrosis
    InterventionLinezolid
    PhasePhase 2
    Registry statusCompleted

  • Clinical Trials to Reduce the Risk of Antimicrobial Resistance

    NCT01570192 · start 2010-09

    Registered record
    Registry ID
    NCT01570192
    Conditions
    Bacterial Pneumonia
    Interventions
    IV meropenem; I.V. Meropenem; Parenteral aminoglycoside; tobramycin for injection USP OR gentamicin sulfate injection solution concentrate 5mg.kg IV q24h; amikacin sulfate injection USP 20 mg/kg IV q24h; Linezolid or Vancomycin (per institutional guidelines) will be available for MRSA coverage.; tobramycin nebulization
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2010-09
    Completion
    2015-04
    Enrolment
    43

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

    ConditionBacterial Pneumonia
    InterventionIV meropenem; I.V. Meropenem; Parenteral aminoglycoside; tobramycin for injection USP OR gentamicin sulfate injection solution concentrate 5mg.kg IV q24h +3 more
    PhasePhase 2
    Registry statusTerminated

  • Efficacy and Safety Study of JNJ-32729463 for Treating Complicated Skin and Skin Structure Infections Compared to Linezolid (Zyvox)

    NCT01128530 · start 2010-06

    Registered record
    Registry ID
    NCT01128530
    Conditions
    Complicated Skin and Skin Structure Infections
    Interventions
    JNJ-32729463; linezolid; JNJ-32729463 placebo; linezolid placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2010-06
    Completion
    2011-01
    Enrolment
    161

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

    ConditionComplicated Skin and Skin Structure Infections
    InterventionJNJ-32729463; linezolid; JNJ-32729463 placebo; linezolid placebo
    PhasePhase 2
    Registry statusCompleted

  • Bioequivalence Study Comparing Linezolid 600 Mg Oral Suspension With 600 Mg Tablet In Chinese Healthy Male Subjects

    NCT01055769 · start 2010-03

    Registered record
    Registry ID
    NCT01055769
    Conditions
    Healthy Volunteers
    Interventions
    Linezolid; Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2010-03
    Completion
    2010-04
    Enrolment
    20

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

    ConditionHealthy Volunteers
    InterventionLinezolid; Linezolid
    PhasePhase 1
    Registry statusCompleted

  • A Single Center Four Part Study in Healthy Adult Subjects to Evaluate: the Safety, Tolerability and Pharmacokinetics of a Single Oral Dose and Repeat Escalating Oral Doses of GSK945237; the Effect of Linezolid on Hematology Safety Parameters; and the Effects of GSK945237 and Moxifloxacin on QTc.

    NCT01039610 · start 2009-11

    Registered record
    Registry ID
    NCT01039610
    Conditions
    Infections, Bacterial
    Interventions
    GSK945237; Placebo; Linezolid; Moxifloxacin
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Withdrawn
    Start
    2009-11
    Completion
    2010-08
    Enrolment
    0

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

    ConditionInfections, Bacterial
    InterventionGSK945237; Placebo; Linezolid; Moxifloxacin
    PhasePhase 1
    Registry statusWithdrawn

  • TBTC Study 30: Safety and Tolerability of Low Dose Linezolid in MDR TB

    NCT00664313 · start 2009-04

    Registered record
    Registry ID
    NCT00664313
    Conditions
    Multi-drug Resistant Tuberculosis; Extensively Drug Resistant Tuberculosis
    Interventions
    Linezolid; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 1 / Phase 2
    Registry status
    Completed
    Start
    2009-04
    Completion
    2010-09
    Enrolment
    36

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

    ConditionMulti-drug Resistant Tuberculosis; Extensively Drug Resistant Tuberculosis
    InterventionLinezolid; Placebo
    PhasePhase 1 / Phase 2
    Registry statusCompleted

  • Study the Efficacy and Safety of PTK 0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI)

    NCT03716024 · start 2007-07-18

    Registered record
    Registry ID
    NCT03716024
    Conditions
    Infectious Skin Disease; Bacterial Skin Disease
    Interventions
    PTK 0796; Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2007-07-18
    Completion
    2008-01-07
    Enrolment
    234

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

    ConditionInfectious Skin Disease; Bacterial Skin Disease
    InterventionPTK 0796; Linezolid
    PhasePhase 2
    Registry statusCompleted