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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.

  • Ceftobiprole in the Treatment of Patients With Community-Acquired Pneumonia

    NCT00326287 · start 2006-06

    Registered record
    Registry ID
    NCT00326287
    Conditions
    Pneumonia
    Interventions
    Ceftobiprole medocaril; Ceftriaxone with or without Linezolid
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2006-06
    Completion
    2007-07
    Enrolment
    638

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

    ConditionPneumonia
    InterventionCeftobiprole medocaril; Ceftriaxone with or without Linezolid
    PhasePhase 3
    Registry statusCompleted

  • Nosocomial Pneumonia With Suspected Or Proven Methicillin-Resistant Staphylococcus Aureus (MRSA)

    NCT00084266 · start 2004-10

    Registered record
    Registry ID
    NCT00084266
    Conditions
    Methicillin Resistant Staphylococcus Aureus (MRSA)
    Interventions
    linezolid (Zyvox); vancomycin
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2004-10
    Completion
    2010-03
    Enrolment
    1,225

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

    ConditionMethicillin Resistant Staphylococcus Aureus (MRSA)
    Interventionlinezolid (Zyvox); vancomycin
    PhasePhase 4
    Registry statusCompleted

  • Skin Structure Infections With Suspected or Proven Methicillin-Resistant Staphylococcus Aureus (MRSA)

    NCT00087490 · start 2004-10

    Registered record
    Registry ID
    NCT00087490
    Conditions
    Skin/Soft Tissue Infections; Methicillin Resistant Staphylococcus Aureus (MRSA)
    Interventions
    linezolid; vancomycin
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Completed
    Start
    2004-10
    Completion
    2007-07
    Enrolment
    1,077

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

    ConditionSkin/Soft Tissue Infections; Methicillin Resistant Staphylococcus Aureus (MRSA)
    Interventionlinezolid; vancomycin
    PhasePhase 4
    Registry statusCompleted

  • New Antibiotic to Treat Patients With Community-acquired Pneumonia Due to a Specific Bacteria (S. Pneumoniae Pneumonia)

    NCT00035269 · start 2001-12

    Registered record
    Registry ID
    NCT00035269
    Conditions
    Pneumonia, Pneumococcal; Community Acquired Infections; Gram-positive Bacterial Infections
    Interventions
    Antibiotic
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2001-12
    Completion
    2003-05
    Enrolment
    230

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

    ConditionPneumonia, Pneumococcal; Community Acquired Infections; Gram-positive Bacterial Infections
    InterventionAntibiotic
    PhasePhase 3
    Registry statusCompleted

  • Treatment of Neutropenic Patients With Fever Who Are Suspected to Have A Gram Positive Infection

    NCT00035425 · start 2001-11

    Registered record
    Registry ID
    NCT00035425
    Conditions
    Febrile Neutropenia
    Interventions
    linezolid; vancomycin
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2001-11
    Completion
    2002-11
    Enrolment
    120

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

    ConditionFebrile Neutropenia
    Interventionlinezolid; vancomycin
    PhasePhase 3
    Registry statusCompleted