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

A Study to Assess Objective Endpoint Measurements of Response in Bacterial Skin Infections

Phase 2

Completed

Conditions: Skin and Subcutaneous Tissue Bacterial Infections

Interventions: Drug: Vancomycin
Drug: Delafloxacin
Drug: Linezolid

First Posted Date: 2011-01-26

Last Posted Date: 2019-10-16

Lead Sponsor: Melinta Therapeutics, Inc.

Target Recruit Count: 256

Registration Number: NCT01283581

Locations: 🇺🇸
University of South Alabama Medical Center, Mobile, Alabama, United States
🇺🇸
Southbay Pharma Research, Buena Park, California, United States
🇺🇸
Drug Research and Analysis Corp, Montgomery, Alabama, United States

and more 22 locations

Zyvox (Linezolid) Special Investigation For Vancomycin-Resistant Enterococci (VRE)

Completed

Conditions: Vancomycin Resistance Enterococcus Faecium

Interventions: Drug: Zyvox (linezolid)

First Posted Date: 2010-10-20

Last Posted Date: 2012-07-02

Lead Sponsor: Pfizer

Target Recruit Count: 41

Registration Number: NCT01224626

GSK1322322 Versus Linezolid in the Treatment of Acute Bacterial Skin and Skin Structure Infection

Phase 2

Completed

Conditions: Skin Infections, Bacterial

Interventions: Drug: GSK1322322
Drug: Linezolid
Drug: Linezolid placebo
Drug: GSK1322322 placebo

First Posted Date: 2010-09-24

Last Posted Date: 2017-12-04

Lead Sponsor: GlaxoSmithKline

Target Recruit Count: 84

Registration Number: NCT01209078

Locations: 🇺🇸
GSK Investigational Site, West Reading, Pennsylvania, United States

Population Pharmacokinetics of Linezolid

Phase 4

Completed

Conditions: Methicillin-Resistant Staphylococcus AureuS

Interventions: Drug: Linezolid

First Posted Date: 2010-09-13

Last Posted Date: 2012-10-23

Lead Sponsor: University Hospital, Toulouse

Target Recruit Count: 60

Registration Number: NCT01200654

TR-701 FA vs. Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections.

Phase 3

Completed

Conditions: Skin and Subcutaneous Tissue Bacterial Infections

Interventions: Drug: TR-701 FA
Drug: Linezolid

First Posted Date: 2010-07-27

Last Posted Date: 2018-08-29

Lead Sponsor: Trius Therapeutics LLC, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)

Target Recruit Count: 667

Registration Number: NCT01170221

Locations: 🇺🇸
Trius investigator site 135, Hialeah, Florida, United States
🇺🇸
Trius investigator site 133, Butte, Montana, United States
🇺🇸
Trius investigator site 120, Houston, Texas, United States

and more 81 locations