Overview
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.
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
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/05/06 | Not Applicable | Not yet recruiting | University Hospital, Basel, Switzerland | ||
2025/04/10 | Phase 2 | Not yet recruiting | |||
2025/04/01 | Phase 3 | Not yet recruiting | Shenzhen Third People's Hospital | ||
2025/02/06 | Phase 1 | ENROLLING_BY_INVITATION | Beijing Chest Hospital | ||
2025/02/06 | Phase 1 | ENROLLING_BY_INVITATION | Beijing Chest Hospital | ||
2025/01/07 | N/A | Active, not recruiting | |||
2024/11/29 | Phase 4 | Recruiting | |||
2024/10/21 | Phase 3 | Recruiting | |||
2024/06/06 | Phase 3 | Not yet recruiting | University of Hamburg-Eppendorf | ||
2024/06/04 | Not Applicable | Not yet recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Fresenius Kabi Norge As | 66298-5140 | INTRAVENOUS | 600 mg in 300 mL | 9/3/2018 | |
| Ascend Laboratories, LLC | 67877-419 | ORAL | 600 mg in 1 1 | 10/12/2023 | |
| Hospira, Inc. | 0409-4883 | INTRAVENOUS | 2 mg in 1 mL | 1/10/2023 | |
| Sandoz Inc | 0781-3431 | INTRAVENOUS | 200 mg in 100 mL | 8/3/2023 | |
| American Health Packaging | 60687-754 | ORAL | 100 mg in 5 mL | 8/18/2023 | |
| Hikma Pharmaceuticals USA Inc. | 0143-9534 | INTRAVENOUS | 600 mg in 300 mL | 2/16/2024 | |
| Sun Pharmaceutical Industries, Inc. | 57664-683 | INTRAVENOUS | 600 mg in 300 mL | 8/8/2023 | |
| Chartwell RX, LLC | 62135-442 | ORAL | 600 mg in 1 1 | 2/22/2023 | |
| Mylan Institutional LLC | 67457-324 | INTRAVENOUS | 200 mg in 100 mL | 11/15/2023 | |
| Amneal Pharmaceuticals LLC | 65162-777 | ORAL | 600 mg in 1 1 | 11/17/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| LINEZOLID SANDOZ FILM COATED TABLET 600MG | SIN14946P | TABLET, FILM COATED | 600mg | 2/10/2016 | |
| HETERO-LINEZOLID FILM COATED TABLETS 600 MG | SIN15762P | TABLET, FILM COATED | 600.00 mg | 8/5/2019 | |
| LINEZAN SOLUTION FOR INFUSION 2MG/ML | SIN16950P | INFUSION, SOLUTION | 2 mg/ml | 2/16/2024 | |
| LINEZOLID KABI SOLUTION FOR INFUSION 2MG/ML | SIN15849P | INFUSION, SOLUTION | 2mg/ml | 11/2/2019 | |
| ZYVOX SOLUTION FOR INFUSION 2 mg/ml | SIN11407P | INJECTION | 2 mg/ml | 10/19/2000 | |
| ZYVOX GRANULES FOR ORAL SUSPENSION 20 mg/ml | SIN11408P | GRANULE, FOR SUSPENSION | 20 mg/ml | 10/19/2000 | |
| ZYVOX TABLET 600 mg | SIN11405P | TABLET, FILM COATED | 600 mg | 10/19/2000 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Linezolid for Oral Suspension | 国药准字H20253003 | 化学药品 | 口服混悬剂 | 1/2/2025 | |
| Linezolid for Oral Suspension | 国药准字H20243512 | 化学药品 | 口服混悬剂 | 4/17/2024 | |
| Linezolid for Oral Suspension | 国药准字H20249523 | 化学药品 | 口服混悬剂 | 12/1/2024 | |
| Linezolid for Oral Suspension | 国药准字HJ20170247 | 化学药品 | 口服混悬剂 | 9/2/2021 | |
| Linezolid and Glucose Injection | 国药准字H20249784 | 化学药品 | 注射剂 | 12/25/2024 | |
| Linezolid and Glucose Injection | 国药准字HC20240008 | 化学药品 | 注射剂 | 11/5/2024 | |
| Linezolid and Glucose Injection | 国药准字H20203278 | 化学药品 | 注射剂 | 6/29/2020 | |
| Linezolid and Glucose Injection | 国药准字H20243447 | 化学药品 | 注射剂 | 4/7/2024 | |
| Linezolid and Glucose Injection | 国药准字H20227018 | 化学药品 | 注射剂 | 2/15/2022 | |
| Linezolid and Glucose Injection | 国药准字H20193018 | 化学药品 | 注射剂 | 11/8/2023 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| LINEZOLID SOLUTION FOR INFUSION 600MG/300ML | N/A | N/A | N/A | 11/22/2023 | |
| LINOSPAN TABLETS 600MG | N/A | N/A | N/A | 11/7/2017 | |
| ZYVOX GRANULES FOR SUSPENSION 20MG/ML | N/A | N/A | N/A | 6/18/2001 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| APO-LINEZOLID linezolid 600 mg tablet blister pack | 207476 | Medicine | A | 1/31/2014 | |
| LINEZOLID CA linezolid 600 mg film-coated tablet blister pack | 272901 | Medicine | A | 1/24/2017 | |
| LINEZOLID KP linezolid 600 mg tablet bottle | 247240 | Medicine | A | 6/1/2016 | |
| LINEZOLID AN linezolid 600 mg tablet blister pack | 235018 | Medicine | A | 1/28/2016 | |
| LINEZOID linezolid 600 mg/300 mL injection solution | 235013 | Medicine | A | 1/28/2016 | |
| ZOLID linezolid 600 mg tablet blister pack | 235011 | Medicine | A | 1/28/2016 | |
| ZOLID linezolid 600 mg/300 mL injection solution | 235015 | Medicine | A | 1/28/2016 | |
| LINEZOLID RM linezolid 600 mg tablet bottle | 247233 | Medicine | A | 6/1/2016 | |
| ZYVOX linezolid 600mg/300mL injection infusion bag | 79690 | Medicine | A | 9/24/2001 | |
| LINEZOLID PANPHARMA INJECTION linezolid 200 mg in 100 mL solution for injection infusion bag | 255932 | Panpharma Australia Pty Ltd | Medicine | A | 9/30/2016 |