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

MRX-I Versus Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infection

Phase 2

Completed

Conditions: Bacterial Infections

Interventions: Drug: MRX-I
Drug: Linezolid

First Posted Date: 2014-10-21

Last Posted Date: 2024-11-04

Lead Sponsor: MicuRx

Target Recruit Count: 120

Registration Number: NCT02269319

A P3 Comparator Trial in Community Acquired Bacterial Pneumonia

Phase 3

Withdrawn

Conditions: Community Acquired Pneumonia

Interventions: Drug: Linezolid Placebo
Drug: Linezolid
Drug: Dalbavancin
Drug: Azithromycin

First Posted Date: 2014-10-21

Last Posted Date: 2016-01-22

Lead Sponsor: Durata Therapeutics Inc., an affiliate of Allergan plc

Registration Number: NCT02269644

Locations: 🇺🇸
Mercury Street Medical Group, Butte, Montana, United States

Linezolid Pharmacokinetics In Patients With Impaired Renal Function (PPT6)

Not Applicable

Completed

Conditions: Renal Failure
Impaired Renal Function

Interventions: Drug: 600 mg linezolid

First Posted Date: 2014-03-14

Last Posted Date: 2014-03-14

Lead Sponsor: Damanhour University

Target Recruit Count: 18

Registration Number: NCT02087566

Efficacy and Safety of Intravenous to Oral 6-Day Tedizolid Phosphate vs. Intravenous to Oral 10-Day Linezolid in Patients With Acute Bacterial Skin and Skin Structure Infection (ABSSSI)

Phase 3

Completed

Conditions: Bacterial Infections

Interventions: Drug: Placebo Tedizolid (BAY119-2631)
Drug: Tedizolid (BAY119-2631)
Drug: Linezolid
Drug: Placebo Linezolid

First Posted Date: 2014-02-19

Last Posted Date: 2017-06-07

Lead Sponsor: Bayer

Target Recruit Count: 598

Registration Number: NCT02066402

Tedizolid Phosphate (TR-701 FA, MK-1986) vs Linezolid for the Treatment of Nosocomial Pneumonia (MK-1986-002)

Phase 3

Completed

Conditions: Pneumonia

Interventions: Drug: Linezolid
Drug: Tedizolid phosphate

First Posted Date: 2013-12-24

Last Posted Date: 2019-06-27

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

Target Recruit Count: 726

Registration Number: NCT02019420

Linezolid Instead of Ethambutol in Treatment of Drug-susceptible Tuberculosis

Phase 2

Conditions: Pulmonary Tuberculosis Without Resistance to Rifampicin

Interventions: Drug: Linezolid
Drug: Ethambutol

First Posted Date: 2013-11-25

Last Posted Date: 2014-12-30

Lead Sponsor: Seoul National University Hospital

Target Recruit Count: 429

Registration Number: NCT01994460

Locations: 🇰🇷
Seoul National University Bundang Hospital, Seongnam, Kyunggi, Korea, Republic of
🇰🇷
National Medical Center, Seoul, Korea, Republic of
🇰🇷
SMG-SNU Boramae Medical Center, Seoul, Korea, Republic of