Linezolid

Generic Name: Linezolid

Brand Names: Zyvox, Zyvoxam

Drug Type: Small Molecule

Chemical Formula: C_₁₆H_₂₀FN_₃O_₄

CAS Number: 165800-03-3

Unique Ingredient Identifier: ISQ9I6J12J

Background: Linezolid is a synthetic antibiotic which is used for the treatment of infections caused by aerobic Gram-positive bacteria. Its effects are bacteriostatic against both enterococci and staphylococci and bactericidal against most isolates of streptococci. Linezolid exerts its antibacterial activity by inhibiting the initiation of bacterial protein synthesis - more specifically, it binds to the 23S ribosomal RNA of the 50S subunit and, in doing so, prevents the formation of the 70S initiation complex which is essential for bacterial reproduction.

Linezolid was initially approved in 2000 and was the first member of the oxazolidinone antibiotic class. A second member of this class, tedizolid, was approved by the FDA in 2014 and is considered generally more effective and tolerable than its predecessor.

Indication: Linezolid is indicated in adults and children for the treatment of infections caused by susceptible Gram-positive bacteria, including nosocomial pneumonia, community-acquired pneumonia, skin and skin structure infections, and vancomycin-resistant Enterococcus faecium infections. Examples of susceptible bacteria include Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae.

Linezolid is not indicated for the treatment of Gram-negative infections, nor has it been evaluated for use longer than 28 days.

Associated Conditions: Community Acquired Pneumonia (CAP) caused by Staphylococcus Aureus Infections, Community acquired pneumonia caused by Susceptible strains of Streptococcus pneumoniae, Complicated Skin and Skin Structure Infection caused by Staphylococcus Aureus Infections, Complicated Skin and Skin Structure Infection caused by Streptococcus Agalactiae Infection, Complicated Skin and Skin Structure Infection caused by Streptococcus Pyogenes Infection, Nosocomial Pneumonia caused by Staphylococcus Aureus Infections, Nosocomial Pneumonia caused by Streptococcus Pneumoniae Infections, Uncomplicated Skin and Skin Structure Infections caused by Staphylococcus Aureus Infections, Uncomplicated Skin and Skin Structure Infections caused by Streptococcus Pyogenes Infection, Vancomycin-resistant Enterococcus faecium infection

Clinical Trials

Evaluation of the Early Bactericidal Activity of Tedizolid and Linezolide Against Mycobacterium Tuberculosis (TEDITUB)

Phase 2

Recruiting

Conditions: Tuberculosis
Multidrug Resistant Tuberculosis

Interventions: Drug: Tedizolid arm (SIVEXTRO®)
Drug: Standard quadruple therapy arm
Drug: Linezolid arm (ZYVOXID®)

First Posted Date: 2022-09-09

Last Posted Date: 2025-02-03

Lead Sponsor: Assistance Publique - Hôpitaux de Paris

Target Recruit Count: 60

Registration Number: NCT05534750

Locations: 🇫🇷
Bacteriology department- Hôpital Saint-Antoine, Paris, France

Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis

Phase 4

Recruiting

Conditions: Endocarditis Infective

First Posted Date: 2022-06-01

Last Posted Date: 2025-03-11

Lead Sponsor: Fundacion Clinic per a la Recerca Biomédica

Target Recruit Count: 360

Registration Number: NCT05398679

Locations: 🇪🇸
Hospital Virgen de la Macarena, Sevilla, Andalucía, Spain
🇪🇸
Hospital Virgen del Rocío, Sevilla, Andalucía, Spain
🇪🇸
Parc Taulí Hospital Universitari, Sabadell, Barcelona, Spain

and more 17 locations

Trial of a Six-Month Regimen of High-Dose Rifampicin, High-Dose Isoniazid, Linezolid, and Pyrazinamide Versus a Standard Nine-Month Regimen for the Treatment of Adults and Adolescents With Tuberculous Meningitis

Phase 2

Suspended

Conditions: Tuberculous Meningitis

Interventions: Drug: Rifampicin (RIF)
Drug: ethambutol (EMB)
Drug: Isoniazid (INH)
Drug: Linezolid (LZD)
Drug: Rifampicin
Drug: Pyrazinamide (PZA)
Drug: Isoniazid

First Posted Date: 2022-05-20

Last Posted Date: 2025-04-23

Lead Sponsor: National Institute of Allergy and Infectious Diseases (NIAID)

Target Recruit Count: 330

Registration Number: NCT05383742

Locations: 🇵🇪
Socios en Salud Sucursal Peru CRS (Site ID: 31985), Lima, Peru
🇵🇪
Barranco CRS (Site ID:11301), Lima, Peru
🇵🇭
TB HIV Innovations and Clinical Research Foundation Corp (Site ID: 31981), Cavite, Philippines

and more 15 locations

Safety and Efficacy Study of Contezolid Acefosamil and Contezolid Compared to Linezolid Administered Intravenously and Orally to Adults With Moderate or Severe Diabetic Foot Infections (DFI)

Phase 3

Recruiting

Conditions: Diabetic Foot Infection

Interventions: Drug: contezolid acefosamil (IV)/contezolid (PO)
Drug: Linezolid (IV and PO)

First Posted Date: 2022-05-11

Last Posted Date: 2025-05-18

Lead Sponsor: MicuRx

Target Recruit Count: 865

Registration Number: NCT05369052

Locations: 🇺🇸
New Hope Research Development, Corona, California, United States
🇺🇸
Clemente Clinical Research, Los Angeles, California, United States
🇺🇸
VA Greater Los Angeles Healthcare System, Los Angeles, California, United States

and more 52 locations

A Study of an Oral Short-course Regimen Including Bedaquiline for the Treatment of Participants With Multidrug-resistant Tuberculosis in China

Phase 4

Recruiting

Conditions: Tuberculosis, Multidrug-Resistant

Interventions: Drug: Bedaquiline
Drug: Levofloxacin
Drug: Linezolid
Drug: Cycloserine
Drug: Clofazimine
Drug: Pyrazinamide
Drug: Protionamide

First Posted Date: 2022-04-01

Last Posted Date: 2023-01-18

Lead Sponsor: Beijing Chest Hospital

Target Recruit Count: 212

Registration Number: NCT05306223

Locations: 🇨🇳
Beijing Chest Hospital, Beijing, China
🇨🇳
The Pulmonary Hospital of Fuzhou in Fujian Province（The tuberculosis control and prevention Hospital of Fuzhou in Fujian Province）, Fuzhou, China
🇨🇳
The Eighth Medical Center of PLA General Hospital, Beijing, China

and more 14 locations

Alternative Antibiotics for Syphilis

Phase 3

Recruiting

Conditions: Early Latent Syphilis
Primary Syphilis
Secondary Syphilis

Interventions: Drug: Linezolid 600 mg
Drug: Benzathine Penicilllin G

First Posted Date: 2021-10-06

Last Posted Date: 2024-05-10

Lead Sponsor: Fundación FLS de Lucha Contra el Sida, las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia

Target Recruit Count: 224

Registration Number: NCT05069974

Locations: 🇪🇸
CAP Drassanes-Hospital Universitari Vall d'Hebron, Barcelona, Spain
🇪🇸
Hospital Clínic de Barcelona, Barcelona, Spain
🇪🇸
Barcelona Checkpoint, Barcelona, Spain

and more 3 locations

Modified BPaL Regimen for Managing Pre-XDR TB and MDR (TI/NR) TB in India

Phase 3

Active, not recruiting

Conditions: Treatment Intolerant Multidrug-Resistant Pulmonary TB
Non-responsive Multidrug-Resistant Pulmonary TB
Pre-Extensively Drug-Resistant Pulmonary TB

Interventions: Drug: Linezolid
Drug: Bedaquiline
Drug: Pretomanid

First Posted Date: 2021-09-10

Last Posted Date: 2024-01-03

Lead Sponsor: Tuberculosis Research Centre, India

Target Recruit Count: 400

Registration Number: NCT05040126

Locations: 🇮🇳
S N Medical College, Agra, Uttarpradesh, India

Linezolid Dosing Strategies in Drug-Resistant TB

Phase 2

Active, not recruiting

Conditions: Tuberculosis, Multidrug-Resistant
Tuberculosis
Tuberculosis, Pulmonary

Interventions: Drug: Linezolid 600 mg
Drug: Linezolid 1200 mg (QD)
Drug: Bedaquiline 200 mg
Drug: Linezolid 1200 mg (TIW)
Drug: Bedaquiline 100 mg
Drug: Clofazimine 300 mg
Drug: Delamanid 300 mg
Drug: Clofazimine 100 mg

First Posted Date: 2021-08-16

Last Posted Date: 2025-03-24

Lead Sponsor: National Institute of Allergy and Infectious Diseases (NIAID)

Target Recruit Count: 132

Registration Number: NCT05007821

Locations: 🇧🇼
Gaborone CRS (Site ID: 12701), Gaborone, South-East District, Botswana
🇧🇷
Instituto de Pesquisa Clinica Evandro Chagas (IPEC) CRS (Site ID: 12101), Rio De Janeiro, Brazil
🇭🇹
GHESKIO Institute of Infectious Diseases and Reproductive Health (GHESKIO - IMIS) CRS (Site ID: 31730), Port-au-Prince, Haiti

and more 10 locations

PHASE II SINGLE-CENTER, RANDOMIZED, OPEN-LABEL, PROSPECTIVE, STUDY TO DETERMINE THE IMPACT OF SERIAL PROCALCITONIN

Phase 2

Completed

Conditions: Hematopoietic and Lymphoid Cell Neoplasm
Malignant Solid Neoplasm

Interventions: Drug: Imipenem/Cilastatin/Relebactam
Drug: Cefepime
Drug: Vancomycin
Drug: Meropenem
Drug: Daptomycin
Drug: Piperacillin-Tazobactam
Drug: Linezolid

First Posted Date: 2021-07-30

Last Posted Date: 2024-11-04

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 100

Registration Number: NCT04983901

Locations: 🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States

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

Not Applicable

Completed

Conditions: Multidrug Resistant Tuberculosis

Interventions: Drug: Bedaquiline
Drug: Pyrazinamide
Drug: Linezolid
Drug: Cycloserine
Drug: Clofazimine

First Posted Date: 2021-01-22

Last Posted Date: 2024-11-11

Lead Sponsor: Huashan Hospital

Target Recruit Count: 89

Registration Number: NCT04717908

Locations: 🇨🇳
The Third People's Hospital of Shenzhen City, Shenzhen, Guangzhou, China
🇨🇳
The Central Hospital of Wenzhou City, Wenzhou, Zhejiang, China
🇨🇳
Hwa Mei Hosptal,University of Chinese Academy of Sciences(Ningbo No.2 Hospital), Ningbo, Zhejiang, China

and more 12 locations

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