linezolid Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
oxazolidinone antibacterials 1584 165800-03-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • linezolid
  • linospan
  • linox
  • zyvox
  • zyvoxid
  • linezolid sodium chloride
  • linezolide
  • U-100766
  • U 100766
An oxazolidinone and acetamide derived ANTI-BACTERIAL AGENT and PROTEIN SYNTHESIS INHIBITOR that is used in the treatment of GRAM-POSITIVE BACTERIAL INFECTIONS of the skin and respiratory tract.
  • Molecular weight: 337.35
  • Formula: C16H20FN3O4
  • CLOGP: 0.17
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 71.11
  • ALOGS: -2.37
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.20 g O
1.20 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 8 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 30 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 50.82 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.58 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.69 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 18, 2000 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Serotonin syndrome 599.54 16.80 261 19204 23959 46642638
Lactic acidosis 492.40 16.80 253 19212 33656 46632941
Thrombocytopenia 482.49 16.80 408 19057 126173 46540424
Drug resistance 255.93 16.80 131 19334 17237 46649360
Anaemia 243.04 16.80 404 19061 255375 46411222
Pathogen resistance 185.36 16.80 76 19389 5984 46660613
Drug interaction 176.98 16.80 309 19156 202785 46463812
Electrocardiogram QT prolonged 160.02 16.80 148 19317 51177 46615420
Pancytopenia 148.40 16.80 180 19285 84878 46581719
Optic neuropathy 136.03 16.80 44 19421 1752 46664845
Neuropathy peripheral 132.66 16.80 176 19289 90717 46575880
Septic shock 130.59 16.80 140 19325 57753 46608844
Platelet count decreased 121.04 16.80 177 19288 99847 46566750
Multiple organ dysfunction syndrome 100.99 16.80 116 19349 51594 46615003
Mitochondrial toxicity 98.83 16.80 24 19441 323 46666274
Fatigue 97.13 16.80 68 19397 608629 46057968
Drug reaction with eosinophilia and systemic symptoms 93.57 16.80 86 19379 29462 46637135
Myelosuppression 93.29 16.80 51 19414 7652 46658945
Staphylococcal infection 92.29 16.80 93 19372 35678 46630919
Bone marrow failure 89.41 16.80 84 19381 29585 46637012
Tuberculosis 84.71 16.80 53 19412 10212 46656385
Enterococcal infection 78.42 16.80 44 19421 6943 46659654
Pain 77.67 16.80 52 19413 476896 46189701
Metabolic acidosis 72.35 16.80 85 19380 38695 46627902
Optic neuritis 71.01 16.80 41 19424 6830 46659767
Headache 65.49 16.80 62 19403 478290 46188307
Rheumatoid arthritis 65.06 16.80 11 19454 240204 46426393
Off label use 64.85 16.80 321 19144 379520 46287077
Respiratory failure 64.50 16.80 130 19335 94686 46571911
Polyneuropathy 62.34 16.80 46 19419 11598 46654999
Hypertransaminasaemia 59.27 16.80 29 19436 3459 46663138
Sepsis 58.82 16.80 156 19309 135858 46530739
Ototoxicity 52.75 16.80 19 19446 1050 46665547
Acute kidney injury 52.66 16.80 216 19249 235639 46430958
Nasopharyngitis 52.11 16.80 3 19462 153995 46512602
Hyperlactacidaemia 51.88 16.80 23 19442 2192 46664405
Hepatocellular injury 50.62 16.80 62 19403 29460 46637137
Geotrichum infection 50.21 16.80 15 19450 457 46666140
Acute generalised exanthematous pustulosis 50.00 16.80 37 19428 9368 46657229
Product use in unapproved indication 49.01 16.80 113 19352 90160 46576437
Renal failure 48.80 16.80 130 19335 113464 46553133
Arthralgia 45.58 16.80 51 19414 364552 46302045
Brain abscess 44.04 16.80 19 19446 1696 46664901
Product dose omission issue 42.86 16.80 9 19456 168511 46498086
Drug level decreased 42.52 16.80 28 19437 5884 46660713
Eosinophilia 42.44 16.80 46 19419 19171 46647426
Tongue discolouration 42.31 16.80 22 19443 2982 46663615
Pneumothorax 41.36 16.80 40 19425 14589 46652008
Hepatotoxicity 37.29 16.80 49 19416 24960 46641637
Sinusitis 37.26 16.80 5 19460 129763 46536834
Fall 36.93 16.80 50 19415 329047 46337550
Clostridium difficile colitis 36.82 16.80 42 19423 18511 46648086
Aspergillus infection 36.38 16.80 27 19438 6863 46659734
Pain in extremity 35.92 16.80 33 19432 258647 46407950
Kussmaul respiration 35.27 16.80 9 19456 150 46666447
Rash maculo-papular 34.62 16.80 50 19415 27824 46638773
Blood lactic acid increased 34.05 16.80 24 19441 5633 46660964
Weight increased 34.04 16.80 13 19452 164460 46502137
Enterovesical fistula 32.71 16.80 11 19454 495 46666102
Nocardiosis 32.21 16.80 15 19450 1602 46664995
Urinary tract infection enterococcal 32.04 16.80 17 19448 2401 46664196
Transaminases abnormal 31.87 16.80 11 19454 536 46666061
Infective pulmonary exacerbation of cystic fibrosis 31.40 16.80 30 19435 10777 46655820
Diabetic macroangiopathy 31.31 16.80 8 19457 134 46666463
Rash morbilliform 31.21 16.80 18 19447 2991 46663606
Leukopenia 31.15 16.80 80 19385 68263 46598334
Respiratory distress 30.86 16.80 51 19414 31865 46634732
Toxic epidermal necrolysis 30.69 16.80 42 19423 22236 46644361
Pulmonary tuberculosis 30.65 16.80 21 19444 4710 46661887
Toxic optic neuropathy 30.36 16.80 8 19457 152 46666445
Cholecystitis acute 30.00 16.80 25 19440 7513 46659084
Posterior reversible encephalopathy syndrome 29.58 16.80 34 19431 15107 46651490
Back pain 28.90 16.80 27 19438 210012 46456585
Multiple-drug resistance 28.36 16.80 16 19449 2549 46664048
Bronchitis 28.33 16.80 5 19460 105974 46560623
Acute respiratory distress syndrome 28.21 16.80 40 19425 21882 46644715
Staphylococcal sepsis 27.96 16.80 24 19441 7508 46659089
Tooth discolouration 27.63 16.80 11 19454 801 46665796
Mycobacterial peritonitis 27.58 16.80 7 19458 114 46666483
Cholestasis 27.40 16.80 44 19421 26849 46639748
Hyperoxaluria 27.30 16.80 7 19458 119 46666478
Alopecia 27.29 16.80 17 19448 162397 46504200
Infusion related reaction 26.57 16.80 5 19460 101203 46565394
Hallucination 26.51 16.80 62 19403 49889 46616708
Leuconostoc infection 26.29 16.80 5 19460 18 46666579
Pancreatitis acute 25.76 16.80 41 19424 24831 46641766
Joint swelling 25.74 16.80 19 19446 166054 46500543
Vomiting 25.31 16.80 294 19171 452500 46214097
Aplasia pure red cell 24.85 16.80 18 19447 4407 46662190
Gait disturbance 24.68 16.80 15 19450 145248 46521349
Pseudomonas infection 24.47 16.80 25 19440 9733 46656864
Klebsiella infection 24.27 16.80 21 19444 6641 46659956
Herbal toxicity 24.06 16.80 5 19460 31 46666566
Eosinophilic pneumonia acute 23.85 16.80 8 19457 357 46666240
Meningitis tuberculous 23.81 16.80 9 19456 570 46666027
Epstein-Barr virus test positive 23.80 16.80 9 19456 571 46666026
Aplasia 23.47 16.80 16 19449 3560 46663037
Peripheral swelling 23.33 16.80 19 19446 158052 46508545
Mycobacterium abscessus infection 23.13 16.80 9 19456 617 46665980
Blood disorder 23.10 16.80 19 19446 5608 46660989
Hyperbilirubinaemia 23.07 16.80 25 19440 10413 46656184
Bacteraemia 23.05 16.80 29 19436 14150 46652447
Exfoliative rash 22.93 16.80 14 19451 2581 46664016
Malaise 22.77 16.80 67 19398 331165 46335432
Sideroblastic anaemia 22.74 16.80 4 19461 8 46666589
Procalcitonin increased 22.48 16.80 9 19456 665 46665932
Systemic candida 22.29 16.80 14 19451 2713 46663884
Depression 22.08 16.80 23 19442 170081 46496516
Acid base balance abnormal 22.02 16.80 7 19458 263 46666334
Muscle spasms 21.93 16.80 12 19453 123101 46543496
Tuberculoma of central nervous system 21.23 16.80 7 19458 296 46666301
Toxic skin eruption 21.20 16.80 26 19439 12361 46654236
SJS-TEN overlap 21.18 16.80 6 19459 151 46666446
Hyponatraemia 21.13 16.80 91 19374 101241 46565356
Pyrexia 21.05 16.80 230 19235 348572 46318025
Drug level below therapeutic 20.50 16.80 14 19451 3123 46663474
Psoriasis 20.38 16.80 4 19461 78600 46587997
Pyelonephritis chronic 20.30 16.80 6 19459 176 46666421
Intentional product use issue 20.25 16.80 58 19407 52722 46613875
Electrolyte imbalance 20.08 16.80 30 19435 17196 46649401
Septal panniculitis 20.02 16.80 5 19460 76 46666521
Wound infection staphylococcal 19.98 16.80 13 19452 2676 46663921
Hepatic infarction 19.92 16.80 8 19457 596 46666001
Hyperpyrexia 19.65 16.80 13 19452 2753 46663844
Metabolic encephalopathy 19.62 16.80 17 19448 5386 46661211
Swelling 19.60 16.80 14 19451 124497 46542100
Encephalopathy 19.27 16.80 43 19422 33546 46633051
Neutropenia 18.87 16.80 113 19352 143091 46523506
Antibiotic level above therapeutic 18.66 16.80 6 19459 234 46666363
Haemoglobin decreased 18.45 16.80 104 19361 128845 46537752
Hepatitis cholestatic 18.39 16.80 18 19447 6659 46659938
Hyperalbuminaemia 17.94 16.80 4 19461 36 46666561
Systemic lupus erythematosus 17.58 16.80 3 19462 65177 46601420
Escherichia infection 17.38 16.80 22 19443 10795 46655802
Hyperthermia 17.37 16.80 19 19446 7995 46658602
Balance disorder 17.34 16.80 3 19462 64518 46602079
Migraine 17.26 16.80 4 19461 70022 46596575
Gastrooesophageal reflux disease 16.89 16.80 5 19460 74339 46592258

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Thrombocytopenia 700.15 16.07 705 24230 136339 29791204
Serotonin syndrome 508.26 16.07 263 24672 17628 29909915
Optic neuropathy 309.07 16.07 95 24840 1554 29925989
Lactic acidosis 255.48 16.07 210 24725 31003 29896540
Anaemia 240.92 16.07 532 24403 207460 29720083
Electrocardiogram QT prolonged 228.35 16.07 209 24726 35626 29891917
Pancytopenia 212.33 16.07 305 24630 84747 29842796
Drug resistance 198.06 16.07 151 24784 19982 29907561
Enterococcal infection 177.86 16.07 101 24834 8123 29919420
Platelet count decreased 152.32 16.07 297 24638 105832 29821711
Bone marrow failure 150.55 16.07 153 24782 29632 29897911
Pathogen resistance 144.42 16.07 89 24846 8321 29919222
Fatigue 125.98 16.07 55 24880 320618 29606925
Neuropathy peripheral 122.08 16.07 214 24721 70261 29857282
Off label use 119.02 16.07 465 24470 248825 29678718
Septic shock 115.19 16.07 197 24738 63410 29864133
Drug interaction 115.17 16.07 396 24539 199172 29728371
Product use in unapproved indication 105.30 16.07 206 24729 73487 29854056
Choroiditis 98.98 16.07 34 24901 801 29926742
Tuberculosis 96.14 16.07 68 24867 8009 29919534
Optic neuritis 87.29 16.07 46 24889 3188 29924355
Polyneuropathy 87.24 16.07 75 24860 11748 29915795
Multiple organ dysfunction syndrome 78.25 16.07 167 24768 63320 29864223
Trichoglossia 76.69 16.07 15 24920 25 29927518
Drug reaction with eosinophilia and systemic symptoms 72.11 16.07 103 24832 28385 29899158
Endophthalmitis 70.57 16.07 41 24894 3439 29924104
Myelosuppression 69.94 16.07 54 24881 7268 29920275
Hypersensitivity vasculitis 68.01 16.07 41 24894 3682 29923861
Pain 66.98 16.07 30 24905 172611 29754932
Fall 65.42 16.07 35 24900 181837 29745706
Staphylococcal infection 64.65 16.07 101 24834 30123 29897420
Hypertransaminasaemia 63.87 16.07 40 24895 3845 29923698
Hepatotoxicity 63.60 16.07 77 24858 18068 29909475
Intentional product use issue 63.46 16.07 111 24824 36329 29891214
Alveolar lung disease 62.55 16.07 20 24915 374 29927169
Antimicrobial susceptibility test resistant 61.67 16.07 16 24919 135 29927408
Visual acuity reduced 60.08 16.07 70 24865 15776 29911767
Rash maculo-papular 58.67 16.07 88 24847 25330 29902213
Ototoxicity 55.98 16.07 26 24909 1370 29926173
Toxic optic neuropathy 55.40 16.07 21 24914 661 29926882
Tooth discolouration 55.17 16.07 17 24918 280 29927263
Tongue discolouration 55 16.07 24 24911 1091 29926452
Candida infection 53.52 16.07 65 24870 15297 29912246
Cardiac valve vegetation 51.50 16.07 18 24917 447 29927096
Geotrichum infection 50.94 16.07 18 24917 462 29927081
Enterococcus test positive 50.87 16.07 21 24914 831 29926712
Nocardiosis 50.42 16.07 33 24902 3422 29924121
Respiratory failure 50.41 16.07 191 24744 100451 29827092
Bicytopenia 50.23 16.07 26 24909 1736 29925807
Eosinophilic pneumonia 49.89 16.07 30 24905 2681 29924862
Klebsiella infection 49.40 16.07 43 24892 6844 29920699
Eosinophilia 48.70 16.07 75 24860 22085 29905458
Uveitis 47.16 16.07 38 24897 5439 29922104
Systemic candida 46.80 16.07 29 24906 2735 29924808
Renal impairment 46.55 16.07 165 24770 84019 29843524
Arthralgia 43.39 16.07 30 24905 135761 29791782
Dizziness 42.78 16.07 60 24875 194849 29732694
Sepsis 41.44 16.07 235 24700 146160 29781383
Bronchopulmonary aspergillosis 41.21 16.07 51 24884 12233 29915310
Back pain 41.06 16.07 17 24918 102579 29824964
Intraocular pressure increased 40.88 16.07 34 24901 5086 29922457
Hepatitis cholestatic 40.76 16.07 41 24894 7831 29919712
Disseminated intravascular coagulation 40.50 16.07 69 24866 22102 29905441
Myocardial infarction 39.80 16.07 28 24907 125597 29801946
Completed suicide 38.99 16.07 17 24918 99475 29828068
Differentiation syndrome 38.58 16.07 19 24916 1141 29926402
Pulmonary interstitial emphysema syndrome 38.51 16.07 14 24921 391 29927152
Hyperlactacidaemia 38.29 16.07 25 24910 2581 29924962
Malaise 37.02 16.07 51 24884 166911 29760632
Product dose omission issue 36.96 16.07 15 24920 91616 29835927
Mitochondrial toxicity 36.65 16.07 24 24911 2490 29925053
Headache 36.26 16.07 60 24875 182246 29745297
Constipation 35.98 16.07 25 24910 112881 29814662
Incorrect product administration duration 35.45 16.07 28 24907 3894 29923649
Death 34.97 16.07 166 24769 357117 29570426
Deafness 34.85 16.07 43 24892 10282 29917261
Staphylococcal bacteraemia 34.58 16.07 35 24900 6733 29920810
Product use issue 33.38 16.07 99 24836 45917 29881626
Reticulocytopenia 32.27 16.07 8 24927 55 29927488
Eye pain 31.85 16.07 44 24891 11745 29915798
Normocytic anaemia 31.69 16.07 18 24917 1446 29926097
Respiratory gas exchange disorder 30.73 16.07 12 24923 410 29927133
Nasopharyngitis 30.43 16.07 6 24929 58843 29868700
Leukopenia 30.10 16.07 109 24826 56050 29871493
Treatment failure 29.45 16.07 79 24856 34600 29892943
Toxic epidermal necrolysis 29.09 16.07 53 24882 17887 29909656
Aplastic anaemia 28.87 16.07 29 24906 5527 29922016
Dehydration 28.11 16.07 37 24898 123502 29804041
Chest pain 28.04 16.07 34 24901 117593 29809950
Hepatic failure 27.36 16.07 76 24859 33967 29893576
Drug ineffective for unapproved indication 27.01 16.07 39 24896 10841 29916702
Gastrointestinal disorder 26.88 16.07 67 24868 28070 29899473
Pulmonary mucormycosis 26.82 16.07 11 24924 428 29927115
Syncope 26.77 16.07 19 24916 84884 29842659
Vascular pseudoaneurysm thrombosis 26.68 16.07 7 24928 62 29927481
Pseudomonas infection 26.65 16.07 38 24897 10444 29917099
Nosocomial infection 26.65 16.07 15 24920 1184 29926359
Botulism 26.65 16.07 9 24926 201 29927342
Pneumonia staphylococcal 26.52 16.07 21 24914 2930 29924613
Mucormycosis 26.47 16.07 27 24908 5241 29922302
Sideroblastic anaemia 26.35 16.07 8 24927 125 29927418
Drug ineffective 26.29 16.07 413 24522 339974 29587569
Clostridium test positive 26.07 16.07 18 24917 2038 29925505
Cholangiolitis 25.83 16.07 6 24929 30 29927513
Hypoacusis 25.81 16.07 44 24891 14095 29913448
Condition aggravated 25.44 16.07 199 24736 137667 29789876
CNS ventriculitis 25.43 16.07 9 24926 232 29927311
Hyperleukocytosis 25.03 16.07 16 24919 1593 29925950
Intentional overdose 24.22 16.07 3 24932 41478 29886065
Acute kidney injury 24.13 16.07 340 24595 273502 29654041
Cardiac failure congestive 23.95 16.07 21 24914 84386 29843157
Coronary artery disease 23.82 16.07 6 24929 49706 29877837
Myoclonus 23.74 16.07 41 24894 13271 29914272
Deafness neurosensory 23.62 16.07 18 24917 2375 29925168
Splenic necrosis 23.52 16.07 6 24929 47 29927496
Mycobacterium chelonae infection 23.43 16.07 11 24924 594 29926949
Weight increased 23.31 16.07 17 24918 74896 29852647
Malignant neoplasm progression 23.02 16.07 16 24919 72271 29855272
Cardiac disorder 23.02 16.07 3 24932 39890 29887653
Nutritional condition abnormal 23.01 16.07 10 24925 450 29927093
Drug-induced liver injury 22.83 16.07 53 24882 21221 29906322
Organ failure 22.78 16.07 17 24918 2174 29925369
Metastases to muscle 22.65 16.07 8 24927 205 29927338
Muscle spasms 22.50 16.07 13 24922 64825 29862718
Metastases to retroperitoneum 22.47 16.07 8 24927 210 29927333
Diffuse alveolar damage 22.19 16.07 16 24919 1940 29925603
Brain abscess 21.81 16.07 18 24917 2663 29924880
Aplasia pure red cell 21.56 16.07 25 24910 5601 29921942
Toxic neuropathy 21.43 16.07 9 24926 372 29927171
Acute myocardial infarction 20.80 16.07 9 24926 52930 29874613
Mycobacterium abscessus infection 20.66 16.07 10 24925 578 29926965
Splenic infection fungal 20.64 16.07 6 24929 80 29927463
Renal failure 20.48 16.07 180 24755 128786 29798757
Wound dehiscence 20.30 16.07 19 24916 3322 29924221
Hypofibrinogenaemia 19.92 16.07 14 24921 1631 29925912
Asthenia 19.76 16.07 106 24829 221184 29706359
Rheumatoid arthritis 19.69 16.07 5 24930 41192 29886351
Status epilepticus 19.61 16.07 34 24901 11038 29916505
Dyspnoea 19.33 16.07 181 24754 333114 29594429
Peripheral sensory neuropathy 18.99 16.07 24 24911 5877 29921666
Metastases to spleen 18.95 16.07 8 24927 335 29927208
Metastases to bone marrow 18.93 16.07 9 24926 500 29927043
Haematological malignancy 18.87 16.07 6 24929 110 29927433
Memory impairment 18.78 16.07 4 24931 37170 29890373
Hepatocellular injury 18.65 16.07 55 24880 25416 29902127
Spontaneous haematoma 18.58 16.07 9 24926 521 29927022
Tubulointerstitial nephritis 18.57 16.07 44 24891 17847 29909696
Haemophagocytic lymphohistiocytosis 18.57 16.07 31 24904 9760 29917783
Cough 18.50 16.07 49 24886 125593 29801950
Acute respiratory distress syndrome 18.46 16.07 52 24883 23420 29904123
Joint swelling 18.41 16.07 8 24927 46938 29880605
Shock haemorrhagic 18.40 16.07 31 24904 9834 29917709
Bronchitis 18.22 16.07 5 24930 39120 29888423
Cytopenia 18.21 16.07 28 24907 8228 29919315
Staphylococcus test positive 17.98 16.07 17 24918 3010 29924533
Blood disorder 17.73 16.07 17 24918 3062 29924481
Peripheral swelling 17.56 16.07 15 24920 61059 29866484
Corynebacterium infection 17.50 16.07 8 24927 406 29927137
Haemodynamic instability 17.42 16.07 27 24908 7988 29919555
Insomnia 17.36 16.07 32 24903 93304 29834239
Retinopathy hypertensive 17.10 16.07 7 24928 271 29927272
Chondritis 17.09 16.07 6 24929 151 29927392
Allodynia 17.07 16.07 9 24926 624 29926919
Intentional product misuse 16.97 16.07 4 24931 34663 29892880
Bacteraemia 16.95 16.07 39 24896 15521 29912022
Extradural abscess 16.87 16.07 9 24926 639 29926904
Inappropriate schedule of product administration 16.85 16.07 6 24929 39722 29887821
Acute generalised exanthematous pustulosis 16.83 16.07 23 24912 6075 29921468
Depression 16.82 16.07 31 24904 90406 29837137
Meningitis staphylococcal 16.60 16.07 5 24930 76 29927467
Neurotoxicity 16.58 16.07 35 24900 13147 29914396
Wrong technique in product usage process 16.48 16.07 3 24932 31152 29896391
Aspergillus infection 16.34 16.07 30 24905 10184 29917359
Rhodococcus infection 16.26 16.07 6 24929 175 29927368
Red blood cell vacuolisation 16.20 16.07 3 24932 3 29927540
Pulmonary valve disease 16.08 16.07 5 24930 85 29927458

Pharmacologic Action:

SourceCodeDescription
ATC J01XX08 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER ANTIBACTERIALS
Other antibacterials
FDA CS M0361132 Oxazolidinones
FDA EPC N0000175495 Oxazolidinone Antibacterial
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011500 Protein Synthesis Inhibitors
CHEBI has role CHEBI:36047 antibacterial drugs
CHEBI has role CHEBI:48001 protein synthesis inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Staphylococcal pneumonia indication 22754005
Pneumonia due to Streptococcus indication 34020007
Vancomycin resistant enterococcus indication 113727004
Streptococcus pyogenes infection indication 302809008
Infection due to Staphylococcus aureus indication 406602003
Complicated Skin and Skin Structure Staphylococcus Aureus Infection indication
Diabetic Foot Infection Due to Gram-Positive Bacteria indication
Complicated Skin and Skin Structure Streptococcus Agalactiae Infection indication
Complicated Skin and Skin Structure Streptococcus Pyogenes Infection indication
Vancomycin-Resistant Enterococcus Faecium Infection indication
Pyrexia of unknown origin off-label use 7520000
Infection of bone off-label use 111253001
Carcinoid syndrome contraindication 35868009
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of optic nerve contraindication 77157004 DOID:1891
Leukopenia contraindication 84828003 DOID:615
Thyrotoxicosis contraindication 90739004 DOID:7997
Lactic acidosis contraindication 91273001 DOID:3650
Pancytopenia contraindication 127034005 DOID:12450
Seizure disorder contraindication 128613002
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Peripheral nerve disease contraindication 302226006
Pheochromocytoma contraindication 302835009
Bone marrow depression contraindication 307762000
Serotonin syndrome contraindication 371089000
Visual impairment contraindication 397540003
Pseudomembranous enterocolitis contraindication 397683000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.4 acidic
pKa2 1.59 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Amine oxidase [flavin-containing] B Enzyme Ki 4.50 WOMBAT-PK
Amine oxidase [flavin-containing] A Enzyme Ki 5.10 CHEMBL
Amine oxidase [flavin-containing] B Enzyme IC50 4.77 CHEMBL

External reference:

IDSource
4021218 VUID
N0000148664 NUI
D00947 KEGG_DRUG
4021218 VANDF
C0663241 UMLSCUI
CHEBI:63607 CHEBI
ZLD PDB_CHEM_ID
CHEMBL126 ChEMBL_ID
D000069349 MESH_DESCRIPTOR_UI
DB00601 DRUGBANK_ID
10827 IUPHAR_LIGAND_ID
7584 INN_ID
ISQ9I6J12J UNII
441401 PUBCHEM_CID
190376 RXNORM
229070 MMSL
31932 MMSL
8840 MMSL
d04534 MMSL
008223 NDDF
125695009 SNOMEDCT_US
387056004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 0009-4992 INJECTION, SOLUTION 600 mg INTRAVENOUS NDA 32 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 0009-5136 SUSPENSION 100 mg ORAL NDA 32 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 0009-5137 INJECTION, SOLUTION 200 mg INTRAVENOUS NDA 32 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 0009-5138 TABLET, FILM COATED 600 mg ORAL NDA 32 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 0009-5140 INJECTION, SOLUTION 600 mg INTRAVENOUS NDA 32 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 0009-7807 INJECTION, SOLUTION 600 mg INTRAVENOUS NDA 32 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 0054-0319 POWDER, FOR SUSPENSION 100 mg ORAL ANDA 27 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 0409-4883 INJECTION, SOLUTION 2 mg INTRAVENOUS NDA 30 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 0781-3431 INJECTION, SOLUTION 200 mg INTRAVENOUS ANDA 29 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 0781-3433 INJECTION, SOLUTION 600 mg INTRAVENOUS ANDA 29 sections
Linezolid Human Prescription Drug Label 1 0904-6553 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 21695-399 TABLET, FILM COATED 600 mg ORAL NDA 28 sections
linezolid HUMAN PRESCRIPTION DRUG LABEL 1 25021-169 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 29 sections
Linezolid Human Prescription Drug Label 1 31722-749 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 40032-022 TABLET 600 mg ORAL ANDA 26 sections
Linezolid Human Prescription Drug Label 1 46708-183 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 50268-471 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Linezolid Human Prescription Drug Label 1 55150-242 INJECTION, SOLUTION 600 mg INTRAVENOUS ANDA 28 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 55695-009 SUSPENSION 100 mg ORAL NDA 31 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 57664-682 INJECTION, SOLUTION 200 mg INTRAVENOUS ANDA 29 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 57664-683 INJECTION, SOLUTION 600 mg INTRAVENOUS ANDA 29 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 59762-1307 TABLET, FILM COATED 600 mg ORAL NDA AUTHORIZED GENERIC 32 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 59762-1308 SUSPENSION 100 mg ORAL NDA AUTHORIZED GENERIC 32 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 60687-309 TABLET, FILM COATED 600 mg ORAL ANDA 26 sections
Linezolid Human Prescription Drug Label 1 62332-183 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 63323-713 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 29 sections
Linezolid HUMAN PRESCRIPTION DRUG LABEL 1 65162-777 TABLET 600 mg ORAL ANDA 27 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 66298-4992 INJECTION, SOLUTION 600 mg INTRAVENOUS NDA 31 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 66298-5137 INJECTION, SOLUTION 200 mg INTRAVENOUS NDA 31 sections
Zyvox HUMAN PRESCRIPTION DRUG LABEL 1 66298-5140 INJECTION, SOLUTION 600 mg INTRAVENOUS NDA 31 sections