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

Linezolid Pharmacokinetics (PK) in Multi-Drug Resistant (MDR)/Extensively-Drug Resistant (XDR) Tuberculosis (TB)

Phase 1

Completed

Conditions: Multi-Drug Resistant Tuberculosis
Extensively Drug Resistant Tuberculosis

Interventions: Drug: Microcrystalline Methylcellulose - Placebo
Drug: Linezolid

First Posted Date: 2008-06-05

Last Posted Date: 2012-08-17

Lead Sponsor: Centers for Disease Control and Prevention

Target Recruit Count: 26

Registration Number: NCT00691392

Locations: 🇿🇦
King George V Hospital, Durban, KwaZulu Natal, South Africa

Single and Multiple Ascending Dose Pharmacokinetic Study of TR701 in Healthy Adults

Phase 1

Completed

Conditions: Healthy Subjects

Interventions: Drug: placebo
Drug: TR-701
Drug: linezolid

First Posted Date: 2008-05-05

Last Posted Date: 2017-08-31

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

Target Recruit Count: 80

Registration Number: NCT00671814

Locations: 🇺🇸
Covance Clinical Research Unit, Madison, Wisconsin, United States

Drug Use Investigation Of Zyvox (Linezolid) (Regulatory Post Marketing Commitment Plan)

Completed

Conditions: Staphylococcal Infections

Interventions: Drug: linezolid (Zyvox)

First Posted Date: 2008-04-24

Last Posted Date: 2012-07-02

Lead Sponsor: Pfizer

Target Recruit Count: 1004

Registration Number: NCT00666276

TBTC Study 30: Safety and Tolerability of Low Dose Linezolid in MDR TB

Phase 1

Completed

Conditions: Multi-drug Resistant Tuberculosis
Extensively Drug Resistant Tuberculosis

Interventions: Drug: Linezolid
Drug: Placebo

First Posted Date: 2008-04-22

Last Posted Date: 2025-04-24

Lead Sponsor: Centers for Disease Control and Prevention

Target Recruit Count: 36

Registration Number: NCT00664313

Locations: 🇿🇦
King George V Hospital, Durban, South Africa

Safety and Efficacy Study of Oxazolidinones to Treat Uncomplicated Skin Infections

Phase 2

Completed

Conditions: Infectious Skin Diseases
Bacterial Skin Diseases
Staphylococcal Skin Infections
Streptococcal Infections
Abscess

Interventions: Drug: Radezolid
Drug: Linezolid

First Posted Date: 2008-03-31

Last Posted Date: 2014-03-27

Lead Sponsor: Melinta Therapeutics, Inc.

Target Recruit Count: 150

Registration Number: NCT00646958

Locations: 🇺🇸
Jamaica Hospital Medical Center, Jamaica, New York, United States
🇺🇸
Mercury Street Medical Group, LLC, Butte, Montana, United States
🇺🇸
Healthcare Partners Medical Group, Los Angeles, California, United States

and more 16 locations