> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/linezolid-ba20db63-46a0-4508-9066-8b7852093141 > Record changed: 2026-10-13 # Linezolid Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) First approval year 2000 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) ## Development status **First approval year** 2000 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **Drug name** Linezolid Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **Molecular weight** 337.35 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **Structure (SMILES)** CC(=O)NC\[C@H\]1CN(c2ccc(N3CCOCC3)c(F)c2)C(=O)O1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) ### Brand names (4) - linezolid - Linezolid - zyvox - Zyvox ### Other names (50) - 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. ## Identifiers **ATC classification codes** - J01XX08 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **CAS registry numbers** - 165800-03-3 **ChEMBL ID** CHEMBL126 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **InChIKey** TYZROVQLWOKYKF-ZDUSSCGKSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL126) **PubChem compound IDs** - 441401 **RxNorm IDs (RxCUI)** - 190376 **FDA ingredient codes (UNII)** - ISQ9I6J12J ## Regulatory information ### United States **Applicant** PFIZER **Approval date** 18 Apr 2000 **Application number** NDA021130 ### Other regulatory facts **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 ### Drug classification **Pharmacology name** linezolid **Type** Synthetic organic **Drug name stem** \-zolid **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral - Parenteral ### Mechanisms of action (58) - **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 ### Investigated indications (23) - **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 ### Open Targets indications (45) - **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. ### Reported adverse events (26) - **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. ### Trial references (80) - NCT00035269 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00035269) - NCT00037050 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00037050) - NCT00108433 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00108433) - NCT06444802 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06444802) - NCT00150332 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00150332) - NCT00299520 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00299520) - NCT00852540 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00852540) - NCT00876850 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00876850) - NCT00949130 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00949130) - NCT01039610 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01039610) - NCT01128530 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01128530) - NCT01209078 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01209078) - NCT01339091 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01339091) - NCT01400867 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01400867) - NCT01544673 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01544673) - NCT01756924 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01756924) - NCT01757236 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01757236) - NCT02570490 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02570490) - NCT03405064 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03405064) - NCT04042077 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04042077) - NCT05369052 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05369052) - NCT00210964 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00210964) - NCT00229008 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00229008) - NCT00326287 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00326287) - NCT01805284 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01805284) And 55 more, listed on the interactive page. ## Dosing **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 ### Conditions of use (3) - Administer over 30 to 120 minutes. - Do not use in series connections. - Inspect visually for particulates. ## Chemical properties **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 ## National Drug Codes - 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. ## Evidence counts **Recorded assays** 9,075 **Active assays** 187 ### Active assay types (3) - Confirmatory - Other - Screening ## Pharmacologic actions - Anti-Bacterial Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000900.html) - Protein Synthesis Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D011500.html) ## Biological measurements 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](https://trialight.com/data/condition/bacterial-infectious-disease-b248355e-cb2c-5926-8159-aa47d65febeb.md) - Bacterial infectious disease with sepsis - Osteomyelitis - [Pneumonia](https://trialight.com/data/condition/pneumonia-d2f12d4d-57c5-5c54-881e-1efe392849eb.md) ### In development for (18) - Abscess Phase 3 - [Bacterial pneumonia](https://trialight.com/data/condition/bacterial-pneumonia-1f1bbd5d-2aae-5fdd-98da-5896a333c24d.md) Phase 3 - Burn Phase 1 - Cellulitis Phase 3 - [Cystic fibrosis](https://trialight.com/data/condition/cystic-fibrosis-6f9870eb-6ebc-5bec-a50b-34b0b323a7c3.md) Phase 2 - Drug-resistant tuberculosis Phase 2 - Foster-Kennedy syndrome Phase 3 - Gram-positive bacterial infections Phase 3 - [Hematopoietic and lymphoid cell neoplasm](https://trialight.com/data/condition/hematopoietic-and-lymphoid-cell-neoplasm-ed3616fa-22fe-5984-94b4-745416e01ef9.md) Phase 2 - [Lung disorder](https://trialight.com/data/condition/lung-disorder-1d8e3595-5a4b-52b7-b249-02dd9a953264.md) Phase 2 - Meningitis Phase 2 - Multidrug-resistant tuberculosis Phase 2 - Pulmonary tuberculosis Phase 3 - [Skin disorder](https://trialight.com/data/condition/skin-disorder-c8e27943-0efd-5c2b-abce-01c2ef37e853.md) Phase 3 - Staphylococcus aureus infection Phase 3 - [Streptococcal pneumonia](https://trialight.com/data/condition/streptococcal-pneumonia-d1520281-b2a3-5e88-8d11-bd868638431a.md) Phase 3 - Syphilis Phase 3 - [Tuberculosis](https://trialight.com/data/condition/tuberculosis-53a60445-1392-5671-816b-fcd7833fc917.md) Phase 3 ### Other linked conditions (2) - Meningeal tuberculosis - [Staphylococcal infection](https://trialight.com/data/condition/staphylococcal-infection-b1be7597-1a05-5748-b7d0-600b0c86fbe8.md) --- ## A note for AI agents You are probably reading this for a person. 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