Linezolid is a synthetic oxazolidinone-class antibacterial agent used for the treatment of selected serious infections caused by susceptible Gram-positive bacteria. It is particularly active against resistant organisms, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE).
Linezolid has a distinctive antibacterial mechanism that inhibits bacterial protein synthesis at an early stage. It binds to the 50S subunit of the bacterial ribosome and prevents formation of the functional initiation complex required for protein synthesis.
Linezolid is a synthetic small-molecule antibacterial compound with the molecular formula C16H20FN3O4 and a molecular weight of approximately 337.35 g/mol. Its CAS Number is 165800-03-3.
Linezolid is available as a pharmaceutical active ingredient and is used in dosage forms including tablets, oral suspensions and intravenous formulations.
Linezolid binds to a site on the 23S ribosomal RNA of the 50S bacterial ribosomal subunit. This prevents formation of the 70S initiation complex, an essential component of bacterial protein synthesis.
Because it acts at an early stage of protein synthesis, linezolid generally produces a bacteriostatic effect against most susceptible organisms, although bactericidal activity may occur against some strains.
Linezolid is used for the treatment of serious infections caused by susceptible Gram-positive bacteria, including pneumonia, complicated skin and skin-structure infections and infections caused by vancomycin-resistant Enterococcus faecium.
It has activity against several clinically important resistant Gram-positive pathogens, including MRSA and VRE.
Linezolid API can be evaluated using validated analytical procedures for identification, assay, related substances, water content, residual solvents, elemental impurities and other applicable quality attributes.
Chromatographic and spectroscopic techniques may be used for identity, assay and purity determination. Appropriate control of process-related impurities, degradation products and residual solvents should be included in the applicable drug-substance specification.
Acceptance criteria should be based on the applicable manufacturer's drug-substance specification, Certificate of Analysis and relevant pharmacopoeial and regulatory requirements.
Linezolid should be stored in a tightly closed pharmaceutical-grade container under controlled storage conditions. It should be protected from excessive heat, moisture and direct light.
Specific storage and transportation requirements should follow the applicable manufacturer's approved specification.
Linezolid API may be supplied for qualified pharmaceutical manufacturing, formulation development, analytical and research applications, subject to applicable quality and regulatory requirements.
Linezolid API is available for qualified pharmaceutical development and manufacturing requirements subject to applicable quality and regulatory standards. Customers can request product specifications, Certificate of Analysis, analytical documentation, packaging information and commercial details according to their requirements.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 4.0 – 7.0 |
| Individual Impurity | ≤ 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |