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Drug

Linezolid

Established medicine
ClassBacterial 70S ribosome inhibitorResearchOngoing clinical research

Also known as N-(((S)-3-(3-Fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide, Zyvox, Linezolide, Linezolidum.

RxNorm190376ChEMBLCHEMBL126ATCJ01XX08UNIIISQ9I6J12J
26
Active clinical trials
55
Protein targets
123
Regulatory events
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Comprehensive Ambulatory Antibiotics for the Treatment of Congenital Syphilis

Clinical trial2026-09-10Results expected Q1 2027 · ClinicalTrials.gov

Daptomycin, Linezolid Use Safe From Resistance Rise

Industry2026-08-27Medscape Medical News

A Phase 2 Randomized, Adaptive, Dose-Ranging, Open-Label Trial of Novel Regimens for the Treatment of Pulmonary Tuberculosis

Clinical trial2026-08-18Results expected Q4 2026 · ClinicalTrials.gov

Label change: LINEZOLID (ANDA206097)

Regulatory2026-07-28FDA

Label change: LINEZOLID (ANDA206097)

Regulatory2026-07-28FDA

Program for Rifampicin-Resistant Disease With Stratified Medicine for Tuberculosis (PRISM-TB)

Clinical trial2026-07-24Results expected Q3 2031 · ClinicalTrials.gov

Prospective, Randomized, Partially Blinded, Phase 2 Study of the Efficacy and Tolerability of Bedaquiline, Delamanid, Levofloxacin, Linezolid, and Clofazimine for Treatment of Patients With MDR-TB

Clinical trial2026-07-08Results expected Q2 2027 · ClinicalTrials.gov

Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis

Clinical trial2026-07-07Results expected Q4 2026 · ClinicalTrials.gov

TBTC Study 30: A Phase I/II Pilot Study for Evaluation of Low Dose, Once Daily, Linezolid Plus Optimized Background Therapy (OBT) Versus Placebo Plus OBT for the Treatment of Multi-drug Resistant Tuberculosis

Clinical trial2026-07-06Results posted · ClinicalTrials.gov

A Phase 2b, Randomised, Multi-center, Partially Blinded Trial Assessing the Safety and Efficacy of Regimens Containing Sorfequiline, Pretomanid and Linezolid in Adults With Newly Diagnosed, Drug-sensitive, Smear Positive Pulmonary Tuberculosis

Clinical trial2026-06-30Results expected Q2 2027 · ClinicalTrials.gov

Label change: LINEZOLID (NDA021130)

Regulatory2026-06-09FDA

Label change: LINEZOLID (NDA021131)

Regulatory2026-06-09FDA

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Linezolid
Aliases & brands
N-(((S)-3-(3-Fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl)methyl)acetamideZyvoxLinezolideLinezolidum
RxNorm CUI
190376
ChEMBL ID
CHEMBL126
ATC codes
J01XX08
UNII
ISQ9I6J12J
Primary mechanism
Bacterial 70S ribosome inhibitor
Regulatory jurisdictions
mhrafda

Pharmacology & targets

55 targets

Known molecular targets and mechanisms supported by curated pharmacology databases.

Large ribosomal subunit protein bL36A
rpmJ1 · P0A7Q6
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL3
rplC · P60438
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS2
rpsB · P0A7V0
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL4
rplD · P60723
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein bS1
rpsA · P0AG67
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS10
rpsJ · P0A7R5
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS11
rpsK · P0A7R9
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS12
rpsL · P0A7S3
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS13
rpsM · P0A7S9
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS14
rpsN · P0AG59
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS15
rpsO · P0ADZ4
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein bS16
rpsP · P0A7T3
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS17
rpsQ · P0AG63
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein bS18
rpsR · P0A7T7
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS19
rpsS · P0A7U3
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein bS20
rpsT · P0A7U7
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein bS21
rpsU · P68679
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS3
rpsC · P0A7V3
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS4
rpsD · P0A7V8
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS5
rpsE · P0A7W1
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein bS6
rpsF · P02358
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS7
rpsG · P02359
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS8
rpsH · P0A7W7
INHIBITORBacterial 70S ribosome inhibitor
Small ribosomal subunit protein uS9
rpsI · P0A7X3
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL10
rplJ · P0A7J3
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL11
rplK · P0A7J7
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL13
rplM · P0AA10
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL14
rplN · P0ADY3
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL15
rplO · P02413
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL16
rplP · P0ADY7
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL17
rplQ · P0AG44
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL18
rplR · P0C018
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL19
rplS · P0A7K6
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL1
rplA · P0A7L0
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL20
rplT · P0A7L3
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL21
rplU · P0AG48
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL22
rplV · P61175
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL23
rplW · P0ADZ0
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL24
rplX · P60624
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL25
rplY · P68919
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL27
rpmA · P0A7L8
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL28
rpmB · P0A7M2
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL29
rpmC · P0A7M6
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL2
rplB · P60422
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL30
rpmD · P0AG51
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL31B
ykgM · P0A7N1
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL31
rpmE · P0A7M9
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL32
rpmF · P0A7N4
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL33
rpmG · P0A7N9
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL34
rpmH · P0A7P5
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL35
rpmI · P0A7Q1
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL36B
rpmJ2 · Q2EEQ2
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL5
rplE · P62399
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein uL6
rplF · P0AG55
INHIBITORBacterial 70S ribosome inhibitor
Large ribosomal subunit protein bL12
rplL · P0A7K2
INHIBITORBacterial 70S ribosome inhibitor

Regulatory timeline

123 events

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval
2000-04-18
Latest approval
2017-02-22
Authorities
FDA · MHRA
Total events
123
fdaU.S. Food and Drug Administration· 122 events
2026-07-28Label change
Label change: LINEZOLID (ANDA206097)
Evidence ↗
2026-07-28Label change
Label change: LINEZOLID (ANDA206097)
Evidence ↗
2026-06-09Label change
Label change: LINEZOLID (NDA021130)
Evidence ↗
mhraMedicines and Healthcare products Regulatory Agency· 1 event
2014-12-11Safety communicationSafety
Drug Safety Update: Linezolid: restricted indication
Evidence ↗

Data from the U.S. Food and Drug Administration (U.S. Food and Drug Administration), public domain (CC0).

Contains public sector information from the Medicines and Healthcare products Regulatory Agency (MHRA) licensed under the Open Government Licence (OGL v3).

Clinical trials

114 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
114
registered trials across all phases
LATEST COMPLETION 2026
26
Active studies
22
Recruiting
68
Late-stage (III+)
69
Completed
19
Discontinued
PHASE DISTRIBUTIONn = 114
Phase 110Phase 1 / 24Phase 232Phase 2 / 37Phase 338Phase 414Phase N / A9

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

Linezolid or Vancomycin Surgical Site Infection Prophylaxis

RecruitingPH IVKey trialAssistance Publique Hopitaux De Marseillen=1,1602029

Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis

RecruitingPH IVFundacion Clinic per a la Recerca Biomédican=3602027

REINFORCE - Reducing Infection-related Readmissions Following Cystectomy. a Multicentre Randomised Clinical Trial Testing Superiority of Individualised Targeted Antibiotic Prophylaxis Over Empiric Prophylaxis At Ureteral Stent Removal to Reduce Infection-related Readmissions Following Cystectomy.

RecruitingPH IVRigshospitalet, Denmarkn=2482027

Microbiological Characteristics of Biofilm on Double J Ureteral Stents After Lithotripsy: A Randomized Controlled Trial

Not yet recruitingPH IVMenoufia Universityn=1002026

A Pragmatic Randomized Controlled Trial to Evaluate the Efficacy and Safety of an Oral Short-course Regimen Including Bedaquiline for the Treatment of Patients With Multidrug-resistant Tuberculosis in China

Unknown statusPH IVBeijing Chest Hospitaln=2122025

Recent completions

Trials that read out recently, adding to the completed evidence base.

Oral and Neuro-Penetrative Alternative Antibiotics for Patients With Syphilis

CompletedPH IIIFundación FLS de Lucha Contra el Sida, las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencian=2242026

A Phase II, Prospective, Randomized, Multicenter Trial to Evaluate the Efficacy and Safety/Tolerability of Two Linezolid Dosing Strategies in Combination With a Short Course Regimen for the Treatment of Drug-Resistant Pulmonary Tuberculosis

CompletedPH IINational Institute of Allergy and Infectious Diseases (NIAID)n=1382026

A Parallel Group, Phase 2A, Randomised, Open Label Treatment Study to Assess the Early Bactericidal Activity, Safety and Tolerability of GSK3036656 Administered as a Two Drug Combination With Novel and Established Antitubercular Agents, or Standard of Care in Adults With Rifampicin-susceptible Pulmonary Tuberculosis

CompletedPH IIGlaxoSmithKlinen=1272025

Evaluating Newly Approved Drugs in Combination Regimens for Multidrug-Resistant TB With Fluoroquinolone Resistance (endTB-Q)

CompletedPH IIIMédecins Sans Frontières, Francen=3232024

Repurposing Clinically Approved Drugs for Yaws With an Insight Into the Cutaneous Ulcer Disease Syndrome (Trep-AByaws)

CompletedPH IIIFundación FLS de Lucha Contra el Sida, las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencian=3842024

Refining MDR-TB Treatment (T) Regimens (R) for Ultra(U) Short(S) Therapy(T) (TB-TRUST)-PLUS

CompletedN/AHuashan Hospitaln=892024
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • ClinicalTrials.gov — clinical trials
  • Regulatory event sources are credited in the Regulatory Timeline above.