Linezolid

Oxazolidinone Antibacterial — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Linezolid is an ofp drug in the Oxazolidinone Antibacterial class catalogued in DrugCentral. It was first approved by the FDA in 2000. DrugCentral lists 5 molecular targets, including MAOA, SDHA and CALML3. Recorded indications include Complicated Skin and Skin Structure Staphylococcus Aureus Infection, Complicated Skin and Skin Structure Streptococcus Agalactiae Infection, Complicated Skin and Skin Structure Streptococcus Pyogenes Infection and Diabetic Foot Infection Due to Gram-Positive Bacteria.

• Approval status: ofp (first approved 2000 by the FDA).
• Drug class: Oxazolidinone Antibacterial.
• Molecular targets: MAOA, SDHA, CALML3 and Maob (5 listed in DrugCentral).
• Indications: Complicated Skin and Skin Structure Staphylococcus Aureus Infection, Complicated Skin and Skin Structure Streptococcus Agalactiae Infection, Complicated Skin and Skin Structure Streptococcus Pyogenes Infection, Diabetic Foot Infection Due to Gram-Positive Bacteria and Infection due to Staphylococcus aureus and others.
• ATC code: J01XX08 (Other antibacterials).
• Molecular formula: C16H20FN3O4; molecular weight 337.35 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (10)

• Complicated Skin and Skin Structure Staphylococcus Aureus Infection
• Complicated Skin and Skin Structure Streptococcus Agalactiae Infection
• Complicated Skin and Skin Structure Streptococcus Pyogenes Infection
• Diabetic Foot Infection Due to Gram-Positive Bacteria
• Infection due to Staphylococcus aureus
• Pneumonia due to Streptococcus
• Staphylococcal pneumonia
• Streptococcus pyogenes infection
• Vancomycin resistant enterococcus
• Vancomycin-Resistant Enterococcus Faecium Infection

Off-label uses (2)

• Infection of bone
• Pyrexia of unknown origin

Contraindications (16)

• Anemia
• Bone marrow depression
• Carcinoid syndrome
• Disorder of optic nerve
• Hypertensive disorder
• Lactic acidosis
• Leukopenia
• Pancytopenia
• Peripheral nerve disease
• Pheochromocytoma
• Pseudomembranous enterocolitis
• Seizure disorder
• Serotonin syndrome
• Thrombocytopenic disorder
• Thyrotoxicosis
• Visual impairment

Mechanism & targets

• Established pharmacologic class: Oxazolidinone Antibacterial

Molecular targets (5)

Target	Gene	Action	Activity
Amine oxidase [flavin-containing] A	MAOA	unknown	Ki 5.10
Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial	SDHA	unknown	IC50 5.09
Calmodulin-like protein 3	CALML3	unknown	IC50 5.03
Amine oxidase [flavin-containing] B	Maob	unknown	IC50 4.77
Amine oxidase [flavin-containing] B	MAOB	unknown	Ki 4.50

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2000-04-18	FDA	—	PHARMACIA AND UPJOHN

ATC classification

ATC code	Therapeutic hierarchy
J01XX08	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIBACTERIALS FOR SYSTEMIC USE › OTHER ANTIBACTERIALS › Other antibacterials

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Thrombocytopenia	2893.3
Lactic acidosis	1918.5
Serotonin syndrome	1758.6
Drug resistance	1343.2
Anaemia	1154.3
Pancytopenia	928.0
Electrocardiogram QT prolonged	906.0
Neuropathy peripheral	888.5
Drug interaction	845.8
Optic neuropathy	717.1
Platelet count decreased	714.0
Pathogen resistance	633.5

Chemical structure

• Molecular formula: C₁₆H₂₀FN₃O₄
• Molecular weight: 337.35 g/mol
• CAS number: 165800-03-3
• InChIKey: TYZROVQLWOKYKF-ZDUSSCGKSA-N
• PubChem CID: 441401

CC(=O)NC[C@H]1CN(C(=O)O1)C1=CC(F)=C(C=C1)N1CCOCC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Linezolid used for?

DrugCentral lists the following indications for Linezolid: Complicated Skin and Skin Structure Staphylococcus Aureus Infection, Complicated Skin and Skin Structure Streptococcus Agalactiae Infection, Complicated Skin and Skin Structure Streptococcus Pyogenes Infection, Diabetic Foot Infection Due to Gram-Positive Bacteria, Infection due to Staphylococcus aureus, Pneumonia due to Streptococcus, Staphylococcal pneumonia and Streptococcus pyogenes infection and others.

How does Linezolid work?

Its molecular targets in DrugCentral include MAOA, SDHA, CALML3 and Maob.

When was Linezolid first approved?

Linezolid was first approved by the FDA in 2000.

What drug class does Linezolid belong to?

Linezolid is in the Oxazolidinone Antibacterial class.

What is the chemical formula of Linezolid?

Linezolid has the molecular formula C16H20FN3O4 and a molecular weight of 337.35 g/mol.

Sources

• DrugCentral drug card 1584 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL126 — compound record and bioactivity
• PubChem CID 441401 — chemical identifiers
• DrugBank DB00601 — drug record
• FDA UNII ISQ9I6J12J — substance identity
• DailyMed: FDA labels for Linezolid — current prescribing information (label search)
• UniProt P21397 (MAOA) — target protein
• UniProt P31040 (SDHA) — target protein
• UniProt P27482 (CALML3) — target protein
• UniProt P27338 (MAOB) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.