Linezolid
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2000
- First approval year
- 2000
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Linezolid
- Molecular weight
- 337.35
- Structure (SMILES)
- CC(=O)NC[C@H]1CN(c2ccc(N3CCOCC3)c(F)c2)C(=O)O1
- linezolid
- Linezolid
- zyvox
- Zyvox
- 600 mg linezolid
- Intravenous linezolid
- linezolid
- Linezolid
- LINEZOLID
- Linezolid (LZD)
- linezolid (Zyvox)
- Linezolid [HSDB]
- Linezolid [INN]
- Linezolid [JAN]
- Linezolid [MART.]
- Linezolid [MI]
- Linezolid [ORANGE BOOK]
- Linezolid [USAN]
- Linezolid [USP MONOGRAPH]
- Linezolid [USP-RS]
- Linezolid [VANDF]
- Linezolid [WHO-DD]
- Linezolid 1200 mg
- Linezolid 1200 mg (QD)
- Linezolid 1200 mg (TIW)
- linezolid 600 mg
- Linezolid 600 mg
- Linezolid 600 mg (post-interim)
- Linezolid 900 mg
And 25 more, listed on the interactive page.
- ATC classification codes
- J01XX08
Sources for recorded values
- CAS registry numbers
- 165800-03-3
- ChEMBL ID
- CHEMBL126
- InChIKey
- TYZROVQLWOKYKF-ZDUSSCGKSA-N
- PubChem compound IDs
- 441401
- RxNorm IDs (RxCUI)
- 190376
- FDA ingredient codes (UNII)
- ISQ9I6J12J
- Applicant
- PFIZER
- Approval date
- 18 Apr 2000
- Application number
- NDA021130
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- linezolid
- Type
- Synthetic organic
- Drug name stem
- -zolid
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Monoamine oxidase A
- Gene symbol
- MAOA
- Protein identifier
- P21397
- Median affinity
- 4.34
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Monoamine oxidase B
- Gene symbol
- MAOB
- Protein identifier
- P27338
- Median affinity
- 5.68
- Affinity units
- pIC50
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P02358
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P02359
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P02413
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7J3
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7J7
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7K2
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7K6
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7L0
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7L3
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7L8
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7M2
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7M6
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7M9
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7N1
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7N4
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7N9
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7P5
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7Q1
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7Q6
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7R5
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7R9
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Protein identifier
- P0A7S3
And 33 more, listed on the interactive page.
Open Targets mechanisms
- Mechanism
- Bacterial 70S ribosome inhibitor
- Action type
- Inhibitor
- Target
- Bacterial 70S ribosome
- Condition
- Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000544
- Subject identifier
- D007239
- Condition
- Skin Diseases
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000701
- Subject identifier
- D012871
- Condition
- Bacterial Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000771
- Subject identifier
- D001424
- Condition
- Abscess
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003030
- Subject identifier
- D000038
- Condition
- Bacteremia
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003033
- Subject identifier
- D016470
- Condition
- Cellulitis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003035
- Subject identifier
- D002481
- Condition
- Osteomyelitis
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003102
- Subject identifier
- D010019
- Condition
- Pneumonia
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003106
- Subject identifier
- D011014
- Condition
- Lung Diseases
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003818
- Subject identifier
- D008171
- Condition
- Staphylococcal Infections
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005681
- Subject identifier
- D013203
- Condition
- Tuberculosis, Multidrug-Resistant
- Highest recorded phase
- 2
- Condition identifier
- EFO:0007381
- Subject identifier
- D018088
- Condition
- Syphilis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0007504
- Subject identifier
- D013587
- Condition
- Burns
- Highest recorded phase
- 1
- Condition identifier
- EFO:0009516
- Subject identifier
- D002056
- Condition
- Tuberculosis, Pulmonary
- Highest recorded phase
- 3
- Condition identifier
- EFO:1000049
- Subject identifier
- D014397
- Condition
- Pneumonia, Bacterial
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001272
- Subject identifier
- D018410
- Condition
- Optic Nerve Diseases
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001330
- Subject identifier
- D009901
- Condition
- Pneumonia, Pneumococcal
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001474
- Subject identifier
- D011018
- Condition
- Cystic Fibrosis
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0009061
- Subject identifier
- D003550
- Condition
- Tuberculosis
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0018076
- Subject identifier
- D014376
- Condition
- Meningitis
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0021108
- Subject identifier
- D008581
- Condition
- Gram-Positive Bacterial Infections
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0021679
- Subject identifier
- D016908
- Condition
- Tuberculosis, Multidrug-Resistant
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0041806
- Subject identifier
- D018088
- Condition
- Hematologic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0044881
- Subject identifier
- D019337
- Condition identifier
- EFO_0000544
- Condition identifier
- EFO_0000544
- Highest recorded phase
- 4
- Condition identifier
- EFO_0000701
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000771
- Condition identifier
- EFO_0003033
- Condition identifier
- EFO_0003102
- Condition identifier
- EFO_0003106
- Condition identifier
- EFO_0005681
- Condition identifier
- EFO_0006834
- Highest recorded phase
- 3
- Condition identifier
- EFO_0007381
- Highest recorded phase
- 2
- Condition identifier
- EFO_0007504
- Highest recorded phase
- 3
- Condition identifier
- EFO_0008556
- Condition identifier
- EFO_0009516
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000039
- Condition identifier
- EFO_1000049
- Highest recorded phase
- 3
- Condition identifier
- EFO_1000714
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001272
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001330
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001474
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001849
- Condition identifier
- EFO_1001865
- Condition identifier
- EFO_1001865
- Highest recorded phase
- 2
- Condition identifier
- HP_0001873
- Condition identifier
- HP_0001945
- Highest recorded phase
- 3
- Condition identifier
- HP_0100806
And 20 more, listed on the interactive page.
- Event
- anaemia
- Reports
- 774
- Reporting signal score
- 719.051
- Event
- bone marrow failure
- Reports
- 183
- Reporting signal score
- 251.916
- Event
- choroiditis
- Reports
- 42
- Reporting signal score
- 156.362
- Event
- drug interaction
- Reports
- 469
- Reporting signal score
- 280.427
- Event
- drug reaction with eosinophilia and systemic symptoms
- Reports
- 141
- Reporting signal score
- 138.011
- Event
- drug resistance
- Reports
- 267
- Reporting signal score
- 460.098
- Event
- electrocardiogram qt prolonged
- Reports
- 222
- Reporting signal score
- 250.176
- Event
- enterococcal infection
- Reports
- 62
- Reporting signal score
- 130.916
- Event
- fatigue
- Reports
- 72
- Reporting signal score
- 167.613
- Event
- hepatotoxicity
- Reports
- 134
- Reporting signal score
- 170.035
- Event
- lactic acidosis
- Reports
- 375
- Reporting signal score
- 674.412
- Event
- mitochondrial toxicity
- Reports
- 43
- Reporting signal score
- 137.546
- Event
- myelosuppression
- Reports
- 83
- Reporting signal score
- 114.429
- Event
- neuropathy peripheral
- Reports
- 416
- Reporting signal score
- 447.309
- Event
- optic neuritis
- Reports
- 91
- Reporting signal score
- 162.013
- Event
- optic neuropathy
- Reports
- 157
- Reporting signal score
- 533.553
- Event
- ototoxicity
- Reports
- 45
- Reporting signal score
- 107.919
- Event
- pain
- Reports
- 45
- Reporting signal score
- 115.482
- Event
- pancytopenia
- Reports
- 403
- Reporting signal score
- 574.367
- Event
- pathogen resistance
- Reports
- 114
- Reporting signal score
- 215.256
- Event
- platelet count decreased
- Reports
- 347
- Reporting signal score
- 279.936
- Event
- polyneuropathy
- Reports
- 100
- Reporting signal score
- 146.499
- Event
- serotonin syndrome
- Reports
- 486
- Reporting signal score
- 1,232.7
- Event
- thrombocytopenia
- Reports
- 944
- Reporting signal score
- 1,377.32
- Event
- tongue discolouration
- Reports
- 53
- Reporting signal score
- 123.189
And 1 more, listed on the interactive page.
- NCT00035269
- NCT00037050
- NCT00108433
- NCT06444802
- NCT00150332
- NCT00299520
- NCT00852540
- NCT00876850
- NCT00949130
- NCT01039610
- NCT01128530
- NCT01209078
- NCT01339091
- NCT01400867
- NCT01544673
- NCT01756924
- NCT01757236
- NCT02570490
- NCT03405064
- NCT04042077
- NCT05369052
- NCT00210964
- NCT00229008
- NCT00326287
- NCT01805284
And 55 more, listed on the interactive page.
- Dose
- 10 mg/kg, 600 mg, 10 mg/kg, 600 mg, 10 mg/kg, 600 mg, 400 mg, 600 mg
- Route
- Intravenous, oral
- How often
- Every 8 hours, every 12 hours, every 8 hours, every 12 hours, every 12 hours
- Administer over 30 to 120 minutes.
- Do not use in series connections.
- Inspect visually for particulates.
- Hydrogen bond acceptors
- 5
- Hydrogen bond donors
- 1
- Polar surface area
- 71.11
- Calculated partition coefficient (ALogP)
- 1.12
- Calculated partition coefficient (XLogP)
- 0.7
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 4
- Heavy atoms
- 24
- Molecular formula
- C16H20FN3O4
- Monoisotopic mass
- 337.14378429
- Natural product
- No
- 0009-5136
- 0009-5138
- 0009-5140
- 0009-7807
- 0054-0319
- 0143-9534
- 0409-4883
- 0781-3431
- 0781-3433
- 0904-6553
- 31722-749
- 31722-865
- 33342-352
- 43386-022
- 46708-183
- 55150-242
- 57664-682
- 57664-683
- 60687-309
- 60687-754
- 62135-442
- 62332-183
- 63323-713
- 64980-561
- 65145-181
And 14 more, listed on the interactive page.
- Recorded assays
- 9,075
- Active assays
- 187
- Confirmatory
- Other
- Screening
- Anti-Bacterial Agents
- Protein Synthesis Inhibitors
These details could not be displayed.
Related records
Trials (204)
- 6 Months of Bedaquiline(BDQ), Delamanid(DLM), Linezolid(LZD) and Levofloxacin(LFX) in RR-TB Patients in Hubei Province
- A Clinical Study, Randomized, Double-blind, Placebo-controlled, Single Dose Study
- A P3 Comparator Trial in Community Acquired Bacterial Pneumonia
- A PAN-USR TB Multi-Center Trial
- A Phase 2 Trial to Evaluate the Efficacy and Safety of Linezolid in Tuberculosis Patients. (LIN-CL001)
- A Phase 3 Trial Assessing Safety and Efficacy of B-Pa-L in Participants With DR-TB
- A Phase II Clinical Study of LCB01-0371 to Evaluate the EBA, Safety and PK
- A Phase II Study of Allogeneic Hematopoietic Stem Cell Transplant for Subjects With VEXAS (Vacuoles, E1 Enzyme, X-linked, Autoinflammatory, Somatic) Syndrome
- A Platform Protocol to Investigate Post-Transplant Cyclophosphamide-Based Graft-Versus-Host Disease Prophylaxis in Patients With Hematologic Malignancies Undergoing Mismatched Unrelated Donor Peripheral Blood Stem Cell Transplantation
- A Safety Study of Epoetin Alfa in Patients With Cancer Who Have Chemotherapy-Related Anemia
- A Single Center Four Part Study in Healthy Adult Subjects to Evaluate: the Safety, Tolerability and Pharmacokinetics of a Single Oral Dose and Repeat Escalating Oral Doses of GSK945237; the Effect of Linezolid on Hematology Safety Parameters; and the Effects of GSK945237 and Moxifloxacin on QTc.
- A Study of an Oral Short-course Regimen Including Bedaquiline for the Treatment of Participants With Multidrug-resistant Tuberculosis in China
- A Study Of Avelumab In Patients With Locally Advanced Or Metastatic Urothelial Cancer (JAVELIN Bladder 100)
- A Study on the Short-course Treatment Regimen Containing Pretomanid for Drug-resistant Tuberculosis
- A Study to Assess Objective Endpoint Measurements of Response in Bacterial Skin Infections
- A Study To Assess The Effect Of Linezolid On QTc Interval
- AbioKin - Antibiotic Kinetics
- Abnormal Post-partum Glucose Metabolism After Gestational Diabetes Diagnosed Before or After 24 Weeks of Gestation
- Adding Asciminib to Usual Treatment for Adults With Newly Diagnosed Philadelphia Chromosome Positive (Ph+) Acute Lymphoblastic Leukemia
- Adjunctive Clindamycin Versus Linezolid for β-lactam Treated Patients With Invasive Group A Streptococcal Infections
Approved for (4)
- Bacterial infectious disease
- Bacterial infectious disease with sepsis
- Osteomyelitis
- Pneumonia
In development for (18)
- Abscess Phase 3
- Bacterial pneumonia Phase 3
- Burn Phase 1
- Cellulitis Phase 3
- Cystic fibrosis Phase 2
- Drug-resistant tuberculosis Phase 2
- Foster-Kennedy syndrome Phase 3
- Gram-positive bacterial infections Phase 3
- Hematopoietic and lymphoid cell neoplasm Phase 2
- Lung disorder Phase 2
- Meningitis Phase 2
- Multidrug-resistant tuberculosis Phase 2
- Pulmonary tuberculosis Phase 3
- Skin disorder Phase 3
- Staphylococcus aureus infection Phase 3
- Streptococcal pneumonia Phase 3
- Syphilis Phase 3
- Tuberculosis Phase 3
Other linked conditions (2)
- Meningeal tuberculosis
- Staphylococcal infection