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

Early Bactericidal Activity of Linezolid, Gatifloxacin, Levofloxacin, Isoniazid (INH) and Moxifloxacin in HIV Negative Adults With Initial Episodes of Sputum Smear-Positive Pulmonary Tuberculosis

Phase 1

Completed

Conditions: Tuberculosis

Interventions: Drug: Moxifloxacin
Drug: Gatifloxacin
Drug: Levofloxacin
Drug: Isoniazid
Drug: Linezolid

First Posted Date: 2006-11-06

Last Posted Date: 2018-11-08

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

Target Recruit Count: 70

Registration Number: NCT00396084

Locations: 🇺🇸
San Francisco General Hospital - Pulmonary and Critical Care Medicine, San Francisco, California, United States
🇧🇷
Universidade Federal do Espirito Santo - Duke Hubert-Yeargan Center, Vitória, Espírito Santo, Brazil

Study to Evaluate Eye Function in Patients Taking Linezolid for Six Weeks or Greater

Phase 3

Terminated

Conditions: Optic Nerve Diseases

Interventions: Drug: Zyvox - linezolid
Drug: Matched control

First Posted Date: 2006-08-02

Last Posted Date: 2015-06-26

Lead Sponsor: Pfizer

Target Recruit Count: 34

Registration Number: NCT00359632

Locations: 🇺🇸
Ochsner Clinic Foundation, New Orleans, Louisiana, United States
🇺🇸
Triple O Research Institute, PA, West Palm Beach, Florida, United States
🇺🇸
Henry Ford Health System, Detroit, Michigan, United States

and more 9 locations

Study of Intravenous (I.V.) Iclaprim Versus Linezolid in Complicated Skin and Skin Structure Infections [cSSSI] (ASSIST-2)

Phase 3

Completed

Conditions: Skin Diseases, Bacterial

First Posted Date: 2006-03-17

Last Posted Date: 2007-03-27

Lead Sponsor: Arpida AG

Registration Number: NCT00303550

Locations: 🇺🇸
Edward Hospital & Health Services, Naperville, Illinois, United States
🇺🇸
Wyoming Medical Center, Casper, Wyoming, United States

Phase 3 Safety and Efficacy Study of I.V. Iclaprim v Linezolid in cSSSI (ASSIST-1)

Phase 3

Completed

Conditions: Complicated Skin and Skin Structure Infection

First Posted Date: 2006-03-07

Last Posted Date: 2008-04-04

Lead Sponsor: Arpida AG

Registration Number: NCT00299520

Locations: 🇺🇸
Infectious Disease of Indiana, Indianapolis, Indiana, United States
🇺🇸
VA Medical Center, Boise, Idaho, United States
🇺🇸
e-Study Site, National City, California, United States

and more 2 locations