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linezolid (Zyvox)
Linezolid inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing peptide bond formation.
Linezolid inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing peptide bond formation. Used for Vancomycin-resistant Enterococcus faecium (VRE) infections, Nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus (MRSA), Complicated skin and soft tissue infections caused by susceptible gram-positive bacteria.
At a glance
| Generic name | linezolid (Zyvox) |
|---|---|
| Also known as | Zyvox, linezolid |
| Sponsor | Pfizer |
| Drug class | Oxazolidinone antibiotic |
| Target | Bacterial 50S ribosomal subunit |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease |
| Phase | FDA-approved |
Mechanism of action
Linezolid is an oxazolidinone antibiotic that binds to the bacterial 50S ribosomal subunit and blocks the initiation of protein synthesis. This mechanism is bacteriostatic, halting bacterial growth and allowing the immune system to clear the infection. It is effective against both gram-positive and some gram-negative bacteria, including resistant strains such as MRSA and VRE.
Approved indications
- Vancomycin-resistant Enterococcus faecium (VRE) infections
- Nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus (MRSA)
- Complicated skin and soft tissue infections caused by susceptible gram-positive bacteria
- Community-acquired pneumonia caused by susceptible pathogens
Common side effects
- Thrombocytopenia
- Nausea
- Diarrhea
- Headache
- Peripheral neuropathy (with prolonged use)
- Optic neuropathy (with prolonged use)
- Serotonin syndrome (drug interaction risk)
Key clinical trials
- Linezolid Plus Standard of Care (NA)
- Testing a Novel Combination Treatment (Arm D) Versus Standard of Care for Intensive Phase Treatment for Mycobacterium Abscessus Pulmonary Disease in People With or Without Cystic Fibrosis in the Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) Adaptive Platform Trial (PHASE2)
- Trial of Novel Regimens for the Treatment of Pulmonary Tuberculosis (PHASE2)
- Linezolid Tolerance During the BPaL Regimen With Dosage Personalization Based on Therapeutic Drug Monitoring (TDM) During Multidrug-Resistant Tuberculosis Treatment (PHASE4)
- Linezolid for Syphilis Pilot Study (PHASE2)
- Prospective, Randomized, Multicenter Clinical Trial of Bisphosphonates Combined With Vancomycin for the Treatment of Cierny-Mader Type I and III Osteomyelitis (PHASE3)
- Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis (PHASE4)
- A Study of Quabodepistat-containing Regimens for the Treatment of Drug-resistant Pulmonary Tuberculosis (PHASE3)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |