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

Trial of Novel Regimens for the Treatment of Pulmonary Tuberculosis

Phase 2

Suspended

Conditions: Pulmonary Tuberculosis

Interventions: Drug: Isoniazid
Drug: Rifampicin
Drug: Bedaquiline
Drug: Pyrazinamide
Drug: Pretomanid
Drug: Ethambutol
Drug: Linezolid
Drug: TBI-223
Drug: Sutezolid

First Posted Date: 2024-01-05

Last Posted Date: 2025-04-23

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

Target Recruit Count: 315

Registration Number: NCT06192160

Locations: 🇧🇼
12701, Gaborone CRS, Gaborone, Botswana
🇧🇷
12201, Hospital Nossa Senhora da Conceicao CRS, Porto Alegre, Brazil
🇧🇷
12101, Instituto de Pesquisa Clinica Evandro Chagas (IPEC) CRS, Rio De Janeiro, Brazil

and more 22 locations

Adjunctive Clindamycin Versus Linezolid for β-lactam Treated Patients With Invasive Group A Streptococcal Infections

Active, not recruiting

Conditions: Streptococcal Sepsis
Infection, Bacterial
Necrotizing Soft Tissue Infection
Infection, Bloodstream
Invasive Group A Beta-Haemolytic Streptococcal Disease
Streptococcal Toxic Shock Syndrome

First Posted Date: 2023-11-13

Last Posted Date: 2023-11-13

Lead Sponsor: National Institutes of Health Clinical Center (CC)

Target Recruit Count: 1000

Registration Number: NCT06126263

Locations: 🇺🇸
National Institutes of Health Clinical Center (primary center conducting large database study), Bethesda, Maryland, United States

Platform Assessing Regimens and Durations In a Global Multisite Consortium for TB

Phase 2

Recruiting

Conditions: Pulmonary Tuberculosis

Interventions: Drug: GSK3036656
Drug: BTZ-043
Drug: Bedaquiline (B)
Drug: Rifampicin (R)
Drug: Delamanid (D)
Drug: Isoniazid (H)
Drug: Pretomanid (Pa)
Drug: Linezolid (L)
Drug: Moxifloxacin (M)
Drug: Pyrazinamide (Z)
Drug: Ethambutol (E)

First Posted Date: 2023-11-02

Last Posted Date: 2024-10-16

Lead Sponsor: University College, London

Target Recruit Count: 2500

Registration Number: NCT06114628

Locations: 🇿🇦
TASK Eden, George, South Africa
🇹🇿
NIMR Mbeya, Mbeya, Tanzania
🇿🇦
TASK Brooklyn, Cape Town, South Africa

and more 5 locations

Innovating Shorter, All- Oral, Precised, Individualized Treatment Regimen for Rifampicin Resistant Tuberculosis：Contezolid, Delamanid and Bedaquiline Cohort

Phase 3

Active, not recruiting

Conditions: Pulmonary Tuberculosis
Rifampicin-resistant Tuberculosis

Interventions: Drug: Bedaquiline
Drug: Delamanid
Drug: Contezolid
Drug: Levofloxacin
Drug: Moxifloxacin
Drug: Linezolid
Drug: Clofazimine
Drug: Cycloserine
Drug: Prothionamide
Drug: Pyrazinamide
Drug: Para-Aminosalicylic Acid
Drug: Ethambutol

First Posted Date: 2023-10-13

Last Posted Date: 2025-04-01

Lead Sponsor: Beijing Chest Hospital

Target Recruit Count: 186

Registration Number: NCT06081361

Locations: 🇨🇳
Fuzhou Pulmonary Hospital of Fujian, Fuzhou, China
🇨🇳
People's Hospital of Linyi, Linyi, China
🇨🇳
Fourth People's Hospital of Nanning, Nanning, China

and more 36 locations

Phase 2 Trial Assessing TBAJ876 or Bedaquiline, With Pretomanid and Linezolid in Adults With Drug-sensitive Pulmonary Tuberculosis

Phase 2

Active, not recruiting

Conditions: Pulmonary TB
Pulmonary Tuberculosis
Drug Sensitive Tuberculosis

Interventions: Drug: TBAJ-876
Drug: HRZE
Drug: Pretomanid
Drug: Linezolid
Drug: Bedaquiline
Drug: HR

First Posted Date: 2023-09-28

Last Posted Date: 2025-02-17

Lead Sponsor: Global Alliance for TB Drug Development

Target Recruit Count: 300

Registration Number: NCT06058299

Locations: 🇵🇭
Care Clinical Trial Group Inc., Dasmariñas, Philippines
🇬🇪
National Center for Tuberculosis and Lung Diseases, Tbilisi, Georgia
🇵🇭
Tropical Disease Foundation, Makati City, Philippines

and more 19 locations