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

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 4713 477600-75-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tasocitinib
  • xeljanz
  • CP 690550
  • tofacitinib citrate
  • tofacitinib
  • CP-690550
Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
  • Molecular weight: 312.38
  • Formula: C16H20N6O
  • CLOGP: 1.55
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 88.91
  • ALOGS: -3.02
  • ROTB: 3

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.24 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.88 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.60 % Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 6, 2012 FDA PF PRISM CV

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
Drug ineffective 8646.93 16.16 12734 199389 665104 45808835
Rheumatoid arthritis 4000.82 16.16 5169 206954 235046 46238893
Joint swelling 2925.94 16.16 3680 208443 162393 46311546
Drug intolerance 2488.01 16.16 3195 208928 143854 46330085
Synovitis 2354.58 16.16 2060 210063 59015 46414924
Arthralgia 2317.43 16.16 5098 207025 359505 46114434
Treatment failure 2302.24 16.16 2459 209664 90628 46383311
Therapeutic product effect incomplete 2236.29 16.16 2233 209890 75920 46398019
Musculoskeletal stiffness 1958.23 16.16 2317 209806 95676 46378263
Condition aggravated 1837.59 16.16 3671 208452 241381 46232558
Therapeutic product effect decreased 1707.74 16.16 1988 210135 80613 46393326
Contraindicated product administered 1669.24 16.16 1934 210189 78013 46395926
Pain 1170.26 16.16 4762 207361 472186 46001753
Arthropathy 903.89 16.16 1482 210641 83218 46390721
Loss of personal independence in daily activities 888.83 16.16 1194 210929 55989 46417950
Acute kidney injury 763.46 16.16 89 212034 235766 46238173
Abdominal discomfort 739.01 16.16 1915 210208 149250 46324689
C-reactive protein abnormal 738.32 16.16 677 211446 20593 46453346
Peripheral swelling 737.67 16.16 1968 210155 156103 46317836
Hypotension 693.28 16.16 113 212010 232476 46241463
Hand deformity 678.31 16.16 811 211312 33763 46440176
Herpes zoster 667.07 16.16 1145 210978 66727 46407212
Swelling 595.52 16.16 1565 210558 122946 46350993
Joint range of motion decreased 587.45 16.16 513 211610 14611 46459328
Drug interaction 584.66 16.16 108 212015 202986 46270953
Joint stiffness 578.52 16.16 664 211459 26444 46447495
Toxicity to various agents 571.60 16.16 131 211992 211635 46262304
Drug hypersensitivity 551.64 16.16 2380 209743 241445 46232494
Blood cholesterol increased 525.54 16.16 771 211352 39242 46434697
Death 511.29 16.16 464 211659 335084 46138855
Infection 493.51 16.16 1530 210593 132062 46341877
Hepatic enzyme increased 481.94 16.16 1114 211009 80673 46393266
Rheumatoid factor positive 466.90 16.16 519 211604 19942 46453997
Pain in extremity 447.10 16.16 2336 209787 256344 46217595
Sensitivity to weather change 433.09 16.16 285 211838 5231 46468708
Alopecia 420.85 16.16 1654 210469 160760 46313179
Anti-cyclic citrullinated peptide antibody positive 416.98 16.16 474 211649 18671 46455268
Dyspnoea 415.41 16.16 1099 211024 514449 45959490
Liver function test increased 406.43 16.16 510 211613 22316 46451623
Red blood cell sedimentation rate abnormal 400.47 16.16 396 211727 13253 46460686
Dehydration 386.34 16.16 122 212001 159418 46314521
Febrile neutropenia 382.75 16.16 10 212113 94617 46379322
Hyponatraemia 378.14 16.16 20 212103 101312 46372627
Tuberculin test positive 369.58 16.16 207 211916 2797 46471142
Vomiting 362.34 16.16 968 211155 451826 46022113
Confusional state 339.06 16.16 151 211972 159741 46314198
Anaemia 325.28 16.16 411 211712 255368 46218571
Nasopharyngitis 321.63 16.16 1469 210654 152529 46321410
Overdose 316.18 16.16 44 212079 101935 46372004
Red blood cell sedimentation rate increased 314.94 16.16 451 211672 22438 46451501
Rash 311.46 16.16 2718 209405 353794 46120145
Cardiac arrest 307.88 16.16 28 212095 90371 46383568
Seizure 307.08 16.16 89 212034 122965 46350974
Product use issue 306.71 16.16 1037 211086 93607 46380332
Musculoskeletal pain 306.27 16.16 853 211270 69275 46404664
Mobility decreased 299.88 16.16 772 211351 59822 46414117
Bone erosion 282.65 16.16 277 211846 9166 46464773
Hypokalaemia 280.00 16.16 35 212088 87989 46385950
Tachycardia 277.91 16.16 57 212066 99565 46374374
Tenderness 276.62 16.16 362 211761 16519 46457420
Intentional overdose 274.08 16.16 4 212119 64940 46408999
Drug abuse 271.60 16.16 3 212120 63405 46410534
Neutropenia 271.02 16.16 157 211966 143047 46330892
Rheumatoid nodule 265.16 16.16 262 211861 8758 46465181
Grip strength decreased 264.24 16.16 256 211867 8350 46465589
Bradycardia 260.84 16.16 9 212114 66289 46407650
Glossodynia 254.15 16.16 598 211525 43775 46430164
Pyrexia 250.55 16.16 784 211339 348018 46125921
Somnolence 246.83 16.16 209 211914 156312 46317627
Mycobacterium tuberculosis complex test positive 242.37 16.16 126 211997 1452 46472487
Drug effective for unapproved indication 242.23 16.16 125 211998 1417 46472522
Oedema peripheral 237.77 16.16 225 211898 159481 46314458
Pancytopenia 232.45 16.16 51 212072 85007 46388932
Suicide attempt 229.66 16.16 4 212119 55032 46418907
Respiratory failure 228.52 16.16 73 212050 94743 46379196
Pemphigus 226.21 16.16 579 211544 44695 46429244
Exposure during pregnancy 224.92 16.16 105 212018 108107 46365832
Decreased appetite 224.55 16.16 333 211790 193503 46280436
Haemoglobin decreased 221.26 16.16 158 211965 128791 46345148
Inflammation 220.50 16.16 601 211522 48180 46425759
Pleural effusion 218.23 16.16 54 212069 82898 46391041
Asthenia 210.26 16.16 718 211405 310357 46163582
Therapy interrupted 208.01 16.16 251 211872 10540 46463399
Thrombocytopenia 207.02 16.16 163 211960 126418 46347521
Arthritis 206.87 16.16 796 211327 76520 46397419
Hyperkalaemia 206.37 16.16 5 212118 50704 46423235
Foot deformity 200.64 16.16 296 211827 15129 46458810
Tremor 199.29 16.16 141 211982 115498 46358441
Upper respiratory tract infection 196.70 16.16 686 211437 62870 46411069
Platelet count decreased 195.92 16.16 105 212018 99919 46374020
Renal failure 195.11 16.16 139 211984 113455 46360484
Headache 193.90 16.16 3148 208975 475204 45998735
Coma 193.57 16.16 20 212103 58329 46415610
Cardiac failure congestive 192.25 16.16 88 212035 91662 46382277
Injection site pain 192.21 16.16 125 211998 107027 46366912
Oxygen saturation decreased 189.93 16.16 41 212082 69123 46404816
International normalised ratio increased 189.36 16.16 5 212118 46878 46427061
Wound 188.13 16.16 522 211601 42280 46431659
Adverse drug reaction 187.12 16.16 533 211590 43829 46430110
Depressed level of consciousness 185.23 16.16 7 212116 47562 46426377
Hypoglycaemia 184.57 16.16 17 212106 54332 46419607
Cardiac failure 183.20 16.16 67 212056 79881 46394058
Systemic lupus erythematosus 182.56 16.16 681 211442 64499 46409440
Pericarditis 181.12 16.16 361 211762 23566 46450373
Osteoporosis 180.22 16.16 497 211626 40111 46433828
Fibromyalgia 178.71 16.16 463 211660 36000 46437939
Dry eye 178.36 16.16 413 211710 29909 46444030
Gastrointestinal haemorrhage 177.03 16.16 65 212058 77308 46396631
Hypoxia 176.62 16.16 16 212107 51822 46422117
Atrial fibrillation 174.98 16.16 129 211994 103461 46370478
Multiple sclerosis relapse 168.26 16.16 5 212118 42120 46431819
Osteoarthritis 166.23 16.16 639 211484 61386 46412553
Fatigue 165.37 16.16 3768 208355 604929 45869010
Dizziness 162.55 16.16 896 211227 339518 46134421
C-reactive protein increased 162.29 16.16 610 211513 57980 46415959
Metabolic acidosis 161.05 16.16 3 212120 38777 46435162
Disease progression 160.37 16.16 109 212014 91191 46382748
Sepsis 160.03 16.16 231 211892 135783 46338156
Plasma cell myeloma 159.16 16.16 11 212112 44467 46429472
Rhabdomyolysis 157.14 16.16 8 212115 41901 46432038
Syncope 156.66 16.16 147 211976 104656 46369283
Multiple organ dysfunction syndrome 156.30 16.16 24 212099 51686 46422253
Hallucination 156.07 16.16 21 212102 49930 46424009
Illness 155.29 16.16 232 211891 11992 46461947
Agitation 153.89 16.16 32 212091 55383 46418556
Discomfort 153.36 16.16 514 211609 46156 46427783
Product dose omission in error 152.55 16.16 64 212059 431 46473508
Hypersensitivity 149.33 16.16 1181 210942 149140 46324799
Weight decreased 148.23 16.16 478 211645 210371 46263568
Chest discomfort 145.34 16.16 118 212005 90151 46383788
Nodule 143.65 16.16 256 211867 15349 46458590
Therapeutic response unexpected 143.52 16.16 256 211867 15360 46458579
Osteonecrosis of jaw 141.51 16.16 3 212120 34399 46439540
Product quality issue 139.64 16.16 5 212118 35643 46438296
Lactic acidosis 139.31 16.16 3 212120 33906 46440033
Suicidal ideation 138.34 16.16 42 212081 56340 46417599
Encephalopathy 137.88 16.16 3 212120 33586 46440353
Blood parathyroid hormone decreased 137.65 16.16 132 211991 4249 46469690
Sinusitis 136.90 16.16 1034 211089 128734 46345205
Ascites 134.01 16.16 8 212115 36576 46437363
Fear of injection 132.29 16.16 126 211997 4021 46469918
Joint noise 131.62 16.16 112 212011 3075 46470864
Respiratory arrest 131.57 16.16 5 212118 33811 46440128
Granuloma skin 131.29 16.16 116 212007 3354 46470585
Helicobacter infection 129.87 16.16 209 211914 11527 46462412
Chest pain 129.35 16.16 392 211731 175932 46298007
Rhinorrhoea 129.29 16.16 493 211630 47172 46426767
Gastrointestinal disorder 128.36 16.16 574 211549 59002 46414937
Abortion spontaneous 128.01 16.16 22 212101 43624 46430315
Pruritus 127.90 16.16 616 211507 241736 46232203
Unresponsive to stimuli 127.84 16.16 4 212119 32170 46441769
Gastric disorder 127.68 16.16 336 211787 26369 46447570
Hyperglycaemia 127.47 16.16 8 212115 35063 46438876
Wrong technique in product usage process 127.41 16.16 44 212079 54378 46419561
Flushing 124.78 16.16 69 212054 64545 46409394
Blood pressure decreased 124.18 16.16 52 212071 57107 46416832
Panniculitis 122.09 16.16 140 211983 5564 46468375
Lethargy 120.44 16.16 41 212082 51130 46422809
Drug reaction with eosinophilia and systemic symptoms 119.89 16.16 3 212120 29545 46444394
Adverse reaction 119.56 16.16 165 211958 7925 46466014
Disorientation 119.03 16.16 14 212109 36904 46437035
Mental status changes 119.02 16.16 16 212107 38072 46435867
Neutrophil count decreased 118.69 16.16 26 212097 43400 46430539
Blood bilirubin increased 117.94 16.16 10 212113 34174 46439765
Coronary artery disease 116.10 16.16 10 212113 33742 46440197
Pulmonary hypertension 115.18 16.16 14 212109 35979 46437960
Joint effusion 114.57 16.16 200 211923 11795 46462144
COVID-19 113.65 16.16 257 211866 18318 46455621
Hepatocellular injury 112.73 16.16 5 212118 29517 46444422
Gamma-glutamyltransferase increased 110.29 16.16 9 212114 31731 46442208
Pulmonary oedema 110.20 16.16 47 212076 51058 46422881
Dysarthria 109.75 16.16 19 212104 37479 46436460
Rheumatic fever 109.49 16.16 96 212027 2747 46471192
Respiratory distress 108.31 16.16 10 212113 31906 46442033
Cerebrovascular accident 107.95 16.16 183 211940 100856 46373083
Duodenal ulcer perforation 107.47 16.16 161 211962 8341 46465598
Delirium 106.50 16.16 20 212103 37208 46436731
Product dose omission issue 106.20 16.16 1202 210921 167318 46306621
Anxiety 105.83 16.16 446 211677 181511 46292428
Neuropathy peripheral 104.29 16.16 157 211966 90736 46383203
Influenza 103.67 16.16 728 211395 88542 46385397
Loss of consciousness 103.28 16.16 210 211913 108028 46365911
Joint laxity 101.93 16.16 81 212042 2015 46471924
Immune system disorder 101.92 16.16 152 211971 7843 46466096
Blood alkaline phosphatase increased 101.81 16.16 27 212096 39582 46434357
Hepatic function abnormal 101.72 16.16 17 212106 34404 46439535
Abdominal pain 101.30 16.16 621 211502 229410 46244529
Haematoma 100.52 16.16 13 212110 31859 46442080
Pulmonary embolism 99.97 16.16 215 211908 108370 46365569
Hypophagia 99.94 16.16 9 212114 29297 46444642
Neck pain 99.61 16.16 506 211617 54800 46419139
Myocardial infarction 99.34 16.16 182 211941 97346 46376593
Malaise 95.59 16.16 2070 210053 329162 46144777
Fluid overload 93.65 16.16 8 212115 27177 46446762
Angioedema 93.49 16.16 31 212092 39311 46434628
Finger deformity 92.91 16.16 116 212007 5046 46468893
Jaundice 92.84 16.16 11 212112 28834 46445105
Onychomycosis 92.60 16.16 104 212019 4039 46469900
Stevens-Johnson syndrome 92.19 16.16 3 212120 23294 46450645
Medication error 91.93 16.16 15 212108 30896 46443043
Acute respiratory failure 91.62 16.16 12 212111 29126 46444813
Neoplasm progression 91.52 16.16 8 212115 26675 46447264
Cognitive disorder 91.34 16.16 27 212096 36856 46437083
Hepatic failure 91.33 16.16 20 212103 33396 46440543
Vision blurred 90.17 16.16 139 211984 79569 46394370
Injection site erythema 88.87 16.16 125 211998 74302 46399637
Pulmonary arterial hypertension 88.32 16.16 8 212115 25920 46448019
Agranulocytosis 87.28 16.16 3 212120 22182 46451757
Therapy cessation 87.21 16.16 293 211830 26336 46447603
Bone marrow failure 86.90 16.16 15 212108 29654 46444285
White blood cell count decreased 86.25 16.16 244 211879 111987 46361952
Septic shock 85.54 16.16 82 212041 57811 46416128
Oral mucosal exfoliation 84.18 16.16 64 212059 1489 46472450
Accidental exposure to product 82.41 16.16 3 212120 21078 46452861
Ulcer 82.29 16.16 218 211905 17174 46456765
Deep vein thrombosis 82.00 16.16 148 211975 79625 46394314
Pre-existing condition improved 81.86 16.16 124 211999 6488 46467451
Incorrect dose administered 81.82 16.16 53 212070 45497 46428442
Epilepsy 81.74 16.16 7 212116 23731 46450208
Palpitations 81.68 16.16 196 211927 95063 46378876
Intentional dose omission 81.19 16.16 87 212036 3203 46470736
Joint injury 81.16 16.16 231 211892 18978 46454961
Spinal stenosis 80.61 16.16 177 211946 12366 46461573
Oropharyngeal pain 80.41 16.16 595 211528 73573 46400366
Pneumonia aspiration 80.36 16.16 22 212101 31583 46442356
Off label use 80.34 16.16 2276 209847 377565 46096374
Injection site pruritus 80.33 16.16 40 212083 39703 46434236
Arrhythmia 80.12 16.16 29 212094 34812 46439127
Psychotic disorder 79.76 16.16 6 212117 22615 46451324
Dyskinesia 79.69 16.16 17 212106 28908 46445031
Injection site reaction 78.74 16.16 427 211696 47422 46426517
Sinus tachycardia 78.49 16.16 5 212118 21644 46452295
Circulatory collapse 78.38 16.16 5 212118 21619 46452320
Knee arthroplasty 78.04 16.16 261 211862 23404 46450535
Device issue 77.57 16.16 3 212120 19977 46453962
Injection site haemorrhage 77.48 16.16 4 212119 20705 46453234
Hypocalcaemia 77.45 16.16 14 212109 26771 46447168
Pericardial effusion 76.85 16.16 12 212111 25531 46448408
Balance disorder 76.40 16.16 109 212014 64412 46409527
Impaired work ability 75.27 16.16 173 211950 12463 46461476
Melaena 75.14 16.16 17 212106 27755 46446184
Emotional distress 75.09 16.16 23 212100 30684 46443255
Altered state of consciousness 74.90 16.16 9 212114 23339 46450600
Hemiparesis 74.70 16.16 4 212119 20065 46453874
Dyspnoea exertional 74.57 16.16 71 212052 50218 46423721
Nail disorder 73.27 16.16 130 211993 7766 46466173
Joint dislocation 73.20 16.16 159 211964 11027 46462912
Acute myocardial infarction 72.69 16.16 27 212096 31897 46442042
Urinary retention 72.44 16.16 15 212108 26046 46447893
Aphasia 72.42 16.16 20 212103 28547 46445392
Therapeutic product effect delayed 72.42 16.16 64 212059 1851 46472088
Cholelithiasis 72.25 16.16 43 212080 38638 46435301
Synovial cyst 72.14 16.16 124 211999 7222 46466717
Gait inability 71.94 16.16 334 211789 34869 46439070
Pallor 71.74 16.16 10 212113 23156 46450783
Cerebral haemorrhage 71.67 16.16 20 212103 28351 46445588
Sleep disorder 71.28 16.16 409 211714 46386 46427553
Dysphagia 71.21 16.16 153 211970 77159 46396780
Shock 71.13 16.16 8 212115 21837 46452102
Blood glucose increased 70.15 16.16 138 211985 71875 46402064
Mitral valve incompetence 69.42 16.16 4 212119 18848 46455091
Drug tolerance decreased 68.73 16.16 77 212046 2982 46470957
Musculoskeletal disorder 68.68 16.16 190 211933 15355 46458584
Vaginal haemorrhage 68.62 16.16 16 212107 25588 46448351
Ejection fraction decreased 68.61 16.16 3 212120 17934 46456005
Hepatitis B virus test positive 67.96 16.16 28 212095 179 46473760
Face oedema 67.76 16.16 5 212118 19148 46454791
Constipation 67.53 16.16 488 211635 173609 46300330
Mouth ulceration 67.44 16.16 271 211852 26561 46447378
Asthma 67.42 16.16 203 211920 91339 46382600
Tenosynovitis 66.25 16.16 121 212002 7394 46466545
Haematemesis 66.20 16.16 24 212099 28782 46445157
Toothache 65.74 16.16 195 211928 16397 46457542
Heart rate decreased 65.53 16.16 31 212092 31692 46442247
Electrolyte imbalance 65.50 16.16 3 212120 17223 46456716
Hallucination, visual 65.18 16.16 4 212119 17869 46456070
Acne 65.07 16.16 219 211904 19700 46454239
Transient ischaemic attack 64.91 16.16 39 212084 34864 46439075
Synovial disorder 64.87 16.16 43 212080 799 46473140
Drug level increased 64.71 16.16 5 212118 18436 46455503
Metastases to liver 64.20 16.16 7 212116 19578 46454361
Skin necrosis 64.12 16.16 129 211994 8475 46465464
Swollen joint count increased 63.74 16.16 66 212057 2334 46471605
Aggression 63.41 16.16 13 212110 22731 46451208
Tuberculosis 62.76 16.16 142 211981 10123 46463816
Product administration error 62.13 16.16 8 212115 19673 46454266
Dry mouth 62.03 16.16 445 211678 54481 46419458
Blood urea increased 61.97 16.16 19 212104 25333 46448606
Pancreatitis acute 61.96 16.16 18 212105 24854 46449085
Contrast media allergy 61.88 16.16 57 212066 1742 46472197
Cardiogenic shock 61.82 16.16 3 212120 16381 46457558
Chronic kidney disease 61.42 16.16 57 212066 40814 46433125
Soft tissue disorder 61.29 16.16 85 212038 4101 46469838
Blood potassium decreased 60.93 16.16 50 212073 38013 46435926
Abnormal behaviour 60.90 16.16 11 212112 21047 46452892
Heart rate increased 60.90 16.16 158 211965 74633 46399306
Injection site swelling 60.89 16.16 56 212067 40271 46433668
Nasal congestion 60.36 16.16 400 211723 47713 46426226
Cerebral infarction 59.91 16.16 16 212107 23350 46450589
Orthostatic hypotension 59.34 16.16 19 212104 24639 46449300
Diverticulitis 59.27 16.16 302 211821 32737 46441202
Rheumatoid lung 58.74 16.16 54 212069 1646 46472293
Injury 58.71 16.16 68 212055 43959 46429980
Blood lactate dehydrogenase increased 58.66 16.16 11 212112 20489 46453450
Acute respiratory distress syndrome 58.15 16.16 14 212109 21908 46452031
Pulmonary toxicity 58.08 16.16 88 212035 4605 46469334
Cardiomegaly 57.95 16.16 6 212117 17476 46456463
Inappropriate schedule of product administration 57.94 16.16 131 211992 64882 46409057
Dysgeusia 57.91 16.16 59 212064 40432 46433507
Intestinal obstruction 57.79 16.16 23 212100 26052 46447887
Upper gastrointestinal haemorrhage 57.45 16.16 5 212118 16733 46457206
Restlessness 57.42 16.16 22 212101 25502 46448437
Angina pectoris 57.12 16.16 25 212098 26750 46447189
Deformity 56.72 16.16 111 212012 7146 46466793
Oedema 56.69 16.16 139 211984 66932 46407007
Coagulopathy 54.96 16.16 9 212114 18490 46455449
Disseminated intravascular coagulation 54.81 16.16 10 212113 18995 46454944
Neck deformity 54.76 16.16 54 212069 1800 46472139
Cyanosis 54.20 16.16 5 212118 15966 46457973
Chronic obstructive pulmonary disease 53.95 16.16 113 212010 57520 46416419
Disability 53.86 16.16 133 211990 10034 46463905
Hyperhidrosis 53.67 16.16 216 211907 89092 46384847
Full blood count decreased 53.66 16.16 17 212106 22194 46451745
Crepitations 53.59 16.16 98 212025 5994 46467945
Visual acuity reduced 53.29 16.16 17 212106 22096 46451843
Peptic ulcer haemorrhage 53.27 16.16 41 212082 972 46472967
Vertigo 53.09 16.16 97 212026 51951 46421988
Bronchospasm 53.09 16.16 5 212118 15702 46458237
Tachypnoea 52.98 16.16 3 212120 14348 46459591
Product substitution issue 52.96 16.16 4 212119 15027 46458912
Pharyngitis 52.81 16.16 188 211935 17395 46456544
Hospitalisation 52.30 16.16 133 211990 63252 46410687
Mucosal inflammation 52.19 16.16 60 212063 38916 46435023
Haemoptysis 51.97 16.16 27 212096 26162 46447777
Complication associated with device 51.96 16.16 5 212118 15436 46458503
Pruritus allergic 51.93 16.16 41 212082 1010 46472929
Wrist deformity 51.86 16.16 48 212075 1476 46472463
Erythema 51.73 16.16 408 211715 142412 46331527
Malnutrition 51.47 16.16 3 212120 14000 46459939
Pancreatitis 51.35 16.16 74 212049 43553 46430386
Swollen tongue 51.16 16.16 35 212088 29197 46444742
Ataxia 51.15 16.16 3 212120 13927 46460012
Exostosis 50.96 16.16 131 211992 10132 46463807
Accidental overdose 50.95 16.16 14 212109 20052 46453887
Arthrodesis 50.89 16.16 57 212066 2207 46471732
Therapeutic product effect variable 50.85 16.16 41 212082 1042 46472897
Metastases to bone 50.82 16.16 9 212114 17467 46456472
Adverse event 50.25 16.16 296 211827 33888 46440051
Neurotoxicity 50.23 16.16 3 212120 13714 46460225
Tricuspid valve incompetence 50.23 16.16 3 212120 13714 46460225
Irritability 50.21 16.16 35 212088 28911 46445028
Leukocytosis 49.67 16.16 22 212101 23376 46450563
Infusion related reaction 49.57 16.16 689 211434 100519 46373420
X-ray abnormal 49.36 16.16 42 212081 1153 46472786
Gait disturbance 48.76 16.16 929 211194 144334 46329605
Disturbance in attention 48.63 16.16 43 212080 31517 46442422
Elbow deformity 48.50 16.16 44 212079 1318 46472621
Injection site hypersensitivity 48.39 16.16 46 212077 1464 46472475
Intentional product use issue 48.16 16.16 407 211716 52373 46421566
Sinus disorder 47.96 16.16 175 211948 16388 46457551
Diarrhoea 47.88 16.16 2068 210055 557534 45916405
Ischaemic stroke 47.79 16.16 9 212114 16713 46457226
Epistaxis 47.77 16.16 142 211981 64163 46409776
Injection site mass 47.75 16.16 6 212117 15034 46458905
Therapeutic response decreased 47.24 16.16 347 211776 42798 46431141
Limb deformity 47.04 16.16 69 212054 3507 46470432
Ileus 46.17 16.16 5 212118 14059 46459880
Acute myeloid leukaemia 46.16 16.16 8 212115 15770 46458169
Haematuria 45.89 16.16 33 212090 26825 46447114
Device malfunction 45.89 16.16 4 212119 13370 46460569
Pulmonary fibrosis 45.84 16.16 197 211926 19895 46454044
Haematocrit decreased 45.83 16.16 55 212068 35002 46438937
Blood calcium decreased 45.73 16.16 8 212115 15665 46458274
Diabetic ketoacidosis 45.69 16.16 13 212110 18197 46455742
Extremity contracture 45.49 16.16 40 212083 1149 46472790
Carpal tunnel syndrome 45.45 16.16 167 211956 15692 46458247
Rash maculo-papular 45.38 16.16 36 212087 27838 46446101
Right ventricular failure 45.28 16.16 9 212114 16084 46457855
Blood pressure fluctuation 45.12 16.16 43 212080 30405 46443534
Coeliac disease 44.83 16.16 100 212023 7061 46466878
Osteonecrosis 44.82 16.16 31 212092 25713 46448226
Bacteraemia 44.19 16.16 6 212117 14173 46459766
General physical health deterioration 44.14 16.16 326 211797 115443 46358496
Hip arthroplasty 43.98 16.16 181 211942 17931 46456008
Anti-cyclic citrullinated peptide antibody 43.94 16.16 23 212100 269 46473670
Fluid retention 43.76 16.16 105 212018 50941 46422998
Myelodysplastic syndrome 43.76 16.16 9 212114 15702 46458237
Nodal osteoarthritis 43.65 16.16 33 212090 761 46473178
Fall 43.63 16.16 1150 210973 327947 46145992
Pregnancy 43.00 16.16 36 212087 27101 46446838
Lower limb fracture 42.90 16.16 139 211984 12259 46461680
White blood cell count increased 42.83 16.16 85 212038 44134 46429805
Urinary incontinence 42.62 16.16 40 212083 28490 46445449
Aspartate aminotransferase increased 42.02 16.16 199 211924 78501 46395438
Speech disorder 41.92 16.16 62 212061 36105 46437834
Withdrawal syndrome 41.85 16.16 15 212108 18119 46455820
Chills 41.80 16.16 260 211863 95772 46378167
Nonalcoholic fatty liver disease 41.64 16.16 32 212091 757 46473182
Blood pressure systolic increased 41.10 16.16 42 212081 28745 46445194
Rash erythematous 40.68 16.16 58 212065 34292 46439647
Immobile 40.40 16.16 74 212049 4532 46469407
Transfusion 40.30 16.16 6 212117 13225 46460714
Blood creatine phosphokinase increased 40.10 16.16 40 212083 27684 46446255
Device related infection 39.85 16.16 23 212100 21018 46452921
Alanine aminotransferase increased 39.79 16.16 237 211886 88214 46385725
Small intestinal obstruction 39.74 16.16 12 212111 16160 46457779
Lung infiltration 39.20 16.16 8 212115 14035 46459904
Lower respiratory tract infection 38.82 16.16 402 211721 54687 46419252
Joint arthroplasty 38.82 16.16 47 212076 1980 46471959
Blood magnesium decreased 38.51 16.16 3 212120 10989 46462950
Pneumonia 38.35 16.16 1362 210761 374958 46098981
Myocardial ischaemia 38.33 16.16 6 212117 12743 46461196
Blood sodium decreased 38.04 16.16 26 212097 21700 46452239
Multiple sclerosis 37.93 16.16 34 212089 24757 46449182
Mania 37.89 16.16 3 212120 10843 46463096
Breast cancer metastatic 37.75 16.16 8 212115 13670 46460269
Lip swelling 37.47 16.16 36 212087 25359 46448580
Bone disorder 37.26 16.16 185 211938 19848 46454091
Fine motor skill dysfunction 37.04 16.16 63 212060 3637 46470302
Body temperature increased 36.96 16.16 35 212088 24826 46449113
Lymphocyte count decreased 36.92 16.16 37 212086 25552 46448387
Neck mass 36.92 16.16 59 212064 3234 46470705
Lipids increased 36.75 16.16 33 212090 975 46472964
Renal impairment 36.31 16.16 194 211929 74178 46399761
Haemorrhage intracranial 36.04 16.16 7 212116 12717 46461222
Skin exfoliation 35.76 16.16 59 212064 32879 46441060
Anhedonia 35.71 16.16 3 212120 10332 46463607
Coordination abnormal 35.67 16.16 4 212119 10945 46462994
Investigation abnormal 35.60 16.16 33 212090 1017 46472922
Muscle spasticity 35.28 16.16 5 212118 11435 46462504
Multiple fractures 35.14 16.16 78 212045 5489 46468450
Brain oedema 35.06 16.16 7 212116 12471 46461468
Hallucination, auditory 34.86 16.16 4 212119 10752 46463187
Nightmare 34.62 16.16 16 212107 16582 46457357
Extrapyramidal disorder 34.57 16.16 5 212118 11263 46462676
Onychomadesis 34.46 16.16 53 212070 2810 46471129
Diplopia 34.27 16.16 23 212100 19382 46454557
Cytomegalovirus infection 34.12 16.16 20 212103 18124 46455815
Haemorrhage 34.04 16.16 131 211992 54738 46419201
Diabetes mellitus inadequate control 33.97 16.16 9 212114 13205 46460734
Petechiae 33.79 16.16 8 212115 12662 46461277
Cutaneous vasculitis 33.60 16.16 63 212060 3928 46470011
Femur fracture 33.59 16.16 285 211838 36712 46437227
Pseudomonas infection 33.26 16.16 3 212120 9755 46464184
Synovial fluid analysis 33.21 16.16 36 212087 1343 46472596
Colitis ulcerative 33.15 16.16 164 211959 17568 46456371
Hair growth abnormal 33.13 16.16 49 212074 2509 46471430
Erythema multiforme 33.03 16.16 3 212120 9701 46464238
Back disorder 33.00 16.16 104 212019 9037 46464902
Therapy non-responder 32.74 16.16 308 211815 40844 46433095
Treatment noncompliance 32.51 16.16 53 212070 29678 46444261
Tenosynovitis stenosans 32.24 16.16 42 212081 1907 46472032
Underdose 32.17 16.16 25 212098 19533 46454406
SLE arthritis 32.15 16.16 25 212098 602 46473337
Blood creatinine increased 32.14 16.16 209 211914 76194 46397745
Skin ulcer 32.14 16.16 255 211868 32203 46441736
Mental disorder 31.70 16.16 33 212090 22392 46451547
Gastritis 31.67 16.16 68 212055 34310 46439629
Cholecystitis 31.67 16.16 13 212110 14453 46459486
Muscle rigidity 31.56 16.16 4 212119 9957 46463982
Ventricular extrasystoles 31.52 16.16 6 212117 11057 46462882
Cataract 31.33 16.16 330 211793 45085 46428854
Viral upper respiratory tract infection 31.22 16.16 86 212037 6932 46467007
Oral herpes 30.52 16.16 171 211952 19219 46454720
Labelled drug-drug interaction medication error 30.32 16.16 3 212120 9058 46464881
Renal tubular necrosis 30.30 16.16 6 212117 10753 46463186
Rheumatoid factor negative 30.29 16.16 23 212100 534 46473405
Wheezing 30.28 16.16 132 211991 53254 46420685
Urosepsis 30.21 16.16 16 212107 15337 46458602
Clostridium difficile colitis 30.16 16.16 24 212099 18529 46455410
Psychomotor hyperactivity 30.12 16.16 4 212119 9609 46464330
Nausea 30.09 16.16 2703 209420 684751 45789188
Soft tissue swelling 30.01 16.16 28 212095 870 46473069
Enthesopathy 29.93 16.16 66 212057 4624 46469315
Renal injury 29.82 16.16 4 212119 9537 46464402
Aspiration 29.78 16.16 4 212119 9527 46464412
Scleritis 29.71 16.16 50 212073 2862 46471077
Myopathy 29.56 16.16 3 212120 8878 46465061
Retinal toxicity 29.39 16.16 30 212093 1043 46472896
Acute generalised exanthematous pustulosis 29.26 16.16 4 212119 9401 46464538
Blood pressure diastolic decreased 29.17 16.16 14 212109 14197 46459742
Infiltration anaesthesia 29.00 16.16 14 212109 136 46473803
Hypovolaemia 28.95 16.16 5 212118 9883 46464056
Dyspepsia 28.75 16.16 454 211669 68018 46405921
Peritonitis 28.70 16.16 31 212092 20683 46453256
Escherichia urinary tract infection 28.57 16.16 6 212117 10317 46463622
Pustular psoriasis 28.48 16.16 59 212064 3958 46469981
Urticaria 28.46 16.16 371 211752 117521 46356418
Panic attack 28.37 16.16 30 212093 20212 46453727
Cardiac disorder 28.32 16.16 103 212020 43755 46430184
Schizophrenia 28.24 16.16 3 212120 8565 46465374
Atrial flutter 28.20 16.16 4 212119 9144 46464795
Blood loss anaemia 28.20 16.16 3 212120 8554 46465385
Device breakage 28.16 16.16 5 212118 9687 46464252
Loose body in joint 27.97 16.16 29 212094 1027 46472912
Bone pain 27.79 16.16 114 212009 46776 46427163
Foot fracture 27.77 16.16 168 211955 19414 46454525
Allergic oedema 27.52 16.16 25 212098 750 46473189
Blood albumin decreased 27.52 16.16 14 212109 13731 46460208
Red blood cell sedimentation rate 27.47 16.16 37 212086 1736 46472203
Neoplasm malignant 27.46 16.16 192 211931 23307 46450632
Basal cell carcinoma 27.32 16.16 173 211950 20314 46453625
Incorrect dosage administered 27.29 16.16 36 212087 1655 46472284
Lymphopenia 27.18 16.16 18 212105 15275 46458664
Limb discomfort 27.15 16.16 187 211936 22589 46451350
Bursitis infective 27.08 16.16 30 212093 1147 46472792
Immune thrombocytopenia 26.87 16.16 3 212120 8238 46465701
Abdominal pain lower 26.87 16.16 34 212089 21147 46452792
Hypotonia 26.82 16.16 3 212120 8226 46465713
Glaucoma 26.80 16.16 143 211980 15778 46458161
Impaired healing 26.77 16.16 270 211853 36473 46437466
Oral discomfort 26.70 16.16 88 212035 7830 46466109
Cardiovascular disorder 26.60 16.16 11 212112 12176 46461763
Arteriosclerosis coronary artery 26.52 16.16 3 212120 8153 46465786
Presyncope 26.36 16.16 44 212079 24410 46449529
Bone density abnormal 26.36 16.16 49 212074 3035 46470904
Coronary artery occlusion 26.29 16.16 3 212120 8099 46465840
Polyneuropathy 26.25 16.16 10 212113 11634 46462305
Arteriosclerosis 26.24 16.16 6 212117 9727 46464212
Injection site bruising 26.24 16.16 79 212044 35557 46438382
Fear 26.18 16.16 21 212102 16151 46457788
Vasculitic rash 26.11 16.16 31 212092 1279 46472660
Transplant rejection 25.70 16.16 6 212117 9590 46464349
Musculoskeletal discomfort 25.57 16.16 129 211994 13927 46460012
Generalised oedema 25.52 16.16 17 212106 14382 46459557
Blood glucose decreased 25.38 16.16 29 212094 18863 46455076
Colitis 25.26 16.16 86 212037 37261 46436678
Intentional product misuse 24.76 16.16 325 211798 46803 46427136
Tooth infection 24.68 16.16 116 212007 12170 46461769
Discouragement 24.52 16.16 9 212114 40 46473899
Depression 24.48 16.16 587 211536 169517 46304422
Bursitis 24.30 16.16 164 211959 19678 46454261
Urine output decreased 24.25 16.16 10 212113 11087 46462852
Rales 23.93 16.16 7 212116 9624 46464315
C-reactive protein decreased 23.86 16.16 22 212101 673 46473266
Anger 23.84 16.16 12 212111 11840 46462099
Bronchopulmonary aspergillosis 23.77 16.16 3 212120 7493 46466446
Trigger finger 23.75 16.16 50 212073 3392 46470547
SARS-CoV-2 test positive 23.68 16.16 36 212087 1889 46472050
Nephropathy toxic 23.60 16.16 3 212120 7451 46466488
Hydronephrosis 23.58 16.16 5 212118 8540 46465399
Localised infection 23.57 16.16 187 211936 23614 46450325
Cardiomyopathy 23.46 16.16 23 212100 16050 46457889
Rectal haemorrhage 23.30 16.16 92 212031 38163 46435776
Eosinophil count increased 22.98 16.16 4 212119 7862 46466077
Haemolytic anaemia 22.95 16.16 8 212115 9834 46464105
Feeling cold 22.92 16.16 31 212092 18740 46455199
Subarachnoid haemorrhage 22.88 16.16 11 212112 11142 46462797
Troponin increased 22.78 16.16 4 212119 7812 46466127
Pneumonia viral 22.68 16.16 74 212049 6550 46467389
Poor venous access 22.64 16.16 5 212118 8303 46465636
Skin papilloma 22.51 16.16 55 212068 4121 46469818
Myocarditis 22.47 16.16 4 212119 7735 46466204
Pneumothorax 22.45 16.16 20 212103 14609 46459330
Overlap syndrome 22.38 16.16 20 212103 587 46473352
Hepatitis acute 22.27 16.16 5 212118 8209 46465730
Cardiac murmur 22.27 16.16 12 212111 11392 46462547
Loss of employment 22.24 16.16 28 212095 1228 46472711
Disease recurrence 22.22 16.16 152 211971 18319 46455620
Drug ineffective for unapproved indication 22.14 16.16 139 211984 16274 46457665
Intestinal sepsis 22.05 16.16 14 212109 241 46473698
Granulomatous rosacea 21.96 16.16 7 212116 18 46473921
Diabetic eye disease 21.96 16.16 12 212111 154 46473785
Hyperthyroidism 21.89 16.16 13 212110 11698 46462241
Pleural thickening 21.89 16.16 41 212082 2554 46471385
Lipase increased 21.85 16.16 6 212117 8597 46465342
Nervousness 21.78 16.16 62 212061 28413 46445526
Supraventricular tachycardia 21.78 16.16 17 212106 13253 46460686
Sudden death 21.70 16.16 8 212115 9496 46464443
Obliterative bronchiolitis 21.56 16.16 33 212090 1742 46472197
Hemiplegia 21.47 16.16 3 212120 6935 46467004
Haematotoxicity 21.45 16.16 3 212120 6930 46467009
Creatinine renal clearance decreased 21.40 16.16 3 212120 6917 46467022
Kidney infection 21.30 16.16 140 211983 16649 46457290
Decreased immune responsiveness 20.99 16.16 49 212074 3566 46470373
Tooth abscess 20.95 16.16 113 212010 12520 46461419
Product storage error 20.79 16.16 14 212109 11778 46462161
Lower gastrointestinal haemorrhage 20.79 16.16 4 212119 7316 46466623
Splenomegaly 20.74 16.16 9 212114 9679 46464260
Muscular weakness 20.72 16.16 293 211830 91551 46382388
Major depression 20.45 16.16 3 212120 6687 46467252
Gestational diabetes 20.39 16.16 4 212119 7215 46466724
Injection site warmth 19.77 16.16 20 212103 13752 46460187
Gallbladder adenocarcinoma 19.52 16.16 9 212114 78 46473861
Injection site rash 19.43 16.16 26 212097 15787 46458152
Cold sweat 19.29 16.16 13 212110 10932 46463007
Hepatitis 19.29 16.16 78 212045 32137 46441802
Intestinal ischaemia 19.22 16.16 4 212119 6921 46467018
Muscle twitching 19.19 16.16 23 212100 14649 46459290
Latent tuberculosis 19.13 16.16 33 212090 1927 46472012
Multiple system atrophy 19.08 16.16 12 212111 203 46473736
Bronchitis 19.05 16.16 623 211500 105356 46368583
Product prescribing error 19.01 16.16 39 212084 20008 46453931
Skin cancer 18.98 16.16 85 212038 8738 46465201
Root canal infection 18.95 16.16 10 212113 119 46473820
Throat tightness 18.86 16.16 41 212082 20598 46453341
Injection site urticaria 18.80 16.16 16 212107 11951 46461988
Stress cardiomyopathy 18.73 16.16 6 212117 7778 46466161
Epstein-Barr virus infection 18.66 16.16 4 212119 6780 46467159
Sexual abuse 18.60 16.16 10 212113 124 46473815
Ovarian cyst 18.52 16.16 22 212101 14065 46459874
Metastases to lung 18.46 16.16 13 212110 10683 46463256
Mass excision 18.45 16.16 13 212110 268 46473671
Incontinence 18.36 16.16 11 212112 9851 46464088
Presbyacusis 18.33 16.16 40 212083 2782 46471157
Drug eruption 18.16 16.16 162 211961 21167 46452772
Cardiac failure acute 18.11 16.16 7 212116 8071 46465868
Metastases to lymph nodes 18.05 16.16 4 212119 6627 46467312
Bone cyst 18.05 16.16 33 212090 2018 46471921
Bedridden 18.05 16.16 86 212037 9073 46464866
Sleep apnoea syndrome 17.99 16.16 47 212076 22154 46451785
Anaphylactic shock 17.93 16.16 41 212082 20233 46453706
Cyst 17.92 16.16 105 212018 11995 46461944
Dementia 17.89 16.16 25 212098 14905 46459034
Butterfly rash 17.71 16.16 22 212101 952 46472987
Proteinuria 17.64 16.16 30 212093 16523 46457416
Escherichia infection 17.57 16.16 14 212109 10803 46463136
Blood magnesium increased 17.54 16.16 41 212082 2986 46470953
Aortic valve incompetence 17.52 16.16 3 212120 5967 46467972
Eczema 17.45 16.16 42 212081 20358 46453581
Eyelid oedema 17.34 16.16 13 212110 10344 46463595
Salivary hypersecretion 17.32 16.16 4 212119 6441 46467498
Erysipelas 17.32 16.16 5 212118 6933 46467006
Drug level decreased 17.29 16.16 3 212120 5909 46468030
Sensory loss 17.18 16.16 5 212118 6897 46467042
Body height decreased 17.15 16.16 88 212035 9564 46464375
Bundle branch block left 17.14 16.16 4 212119 6395 46467544
Aspergillus infection 17.14 16.16 5 212118 6885 46467054
Blood thyroid stimulating hormone increased 17.11 16.16 3 212120 5866 46468073
Red blood cell count decreased 17.11 16.16 83 212040 32540 46441399
Toe amputation 17.10 16.16 32 212091 1992 46471947
Secretion discharge 17.04 16.16 85 212038 9134 46464805
Toe operation 17.03 16.16 17 212106 575 46473364
Sinusitis bacterial 16.98 16.16 19 212104 735 46473204
Bursa disorder 16.92 16.16 9 212114 109 46473830
Weight increased 16.81 16.16 911 211212 163562 46310377
Tooth extraction 16.80 16.16 13 212110 10180 46463759
Contraindication to medical treatment 16.77 16.16 17 212106 586 46473353
Thiopurine methyltransferase decreased 16.72 16.16 13 212110 313 46473626
Duodenal ulcer 16.61 16.16 6 212117 7212 46466727
Injection site induration 16.52 16.16 8 212115 8071 46465868
Stress 16.36 16.16 327 211796 51224 46422715
Eyelid ptosis 16.32 16.16 4 212119 6184 46467755
Blood calcium increased 16.31 16.16 7 212116 7580 46466359
Sensory disturbance 16.29 16.16 19 212104 12248 46461691
Hyperventilation 16.22 16.16 3 212120 5644 46468295
Angina unstable 16.17 16.16 7 212116 7541 46466398

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
Drug ineffective 2867.86 21.65 2849 37809 337538 29574282
Rheumatoid arthritis 1420.86 21.65 811 39847 40386 29871434
Joint swelling 1271.58 21.65 791 39867 46155 29865665
Therapeutic product effect incomplete 854.68 21.65 546 40112 33288 29878532
Arthralgia 826.07 21.65 966 39692 134825 29776995
Musculoskeletal stiffness 808.39 21.65 539 40119 35342 29876478
Drug intolerance 797.83 21.65 585 40073 44706 29867114
Therapeutic product effect decreased 681.86 21.65 448 40210 28628 29883192
Treatment failure 679.32 21.65 478 40180 34201 29877619
Contraindicated product administered 594.69 21.65 340 40318 16891 29894929
Synovitis 563.43 21.65 272 40386 9511 29902309
Pain 477.73 21.65 845 39813 171796 29740024
Condition aggravated 432.64 21.65 714 39944 137152 29774668
Peripheral swelling 397.48 21.65 451 40207 60623 29851197
Arthropathy 394.60 21.65 281 40377 20446 29891374
Drug hypersensitivity 319.71 21.65 428 40230 68091 29843729
Herpes zoster 303.66 21.65 281 40377 29662 29882158
C-reactive protein abnormal 290.52 21.65 145 40513 5448 29906372
Loss of personal independence in daily activities 261.85 21.65 224 40434 21311 29890509
Acute kidney injury 255.42 21.65 35 40623 273807 29638013
Joint range of motion decreased 238.85 21.65 129 40529 5716 29906104
Red blood cell sedimentation rate increased 238.30 21.65 139 40519 7156 29904664
Bone erosion 226.15 21.65 93 40565 2200 29909620
Red blood cell sedimentation rate abnormal 216.81 21.65 84 40574 1691 29910129
Drug interaction 213.30 21.65 15 40643 199553 29712267
Toxicity to various agents 213.04 21.65 6 40652 177177 29734643
Disability 201.70 21.65 105 40553 4313 29907507
Drug effective for unapproved indication 200.95 21.65 70 40588 1029 29910791
Hypotension 188.31 21.65 25 40633 200540 29711280
Mobility decreased 179.09 21.65 198 40460 25801 29886019
Pain in extremity 168.21 21.65 424 40234 109797 29802023
Joint stiffness 166.80 21.65 122 40536 9239 29902581
Onychoclasis 166.03 21.65 68 40590 1591 29910229
Swelling 161.85 21.65 221 40437 35754 29876066
Sensitivity to weather change 160.68 21.65 64 40594 1390 29910430
Gastric disorder 147.50 21.65 119 40539 10424 29901396
Rheumatoid factor negative 144.09 21.65 46 40612 507 29911313
Musculoskeletal pain 139.05 21.65 190 40468 30750 29881070
Chondropathy 135.09 21.65 49 40609 815 29911005
Lymphoma 134.77 21.65 111 40547 10010 29901810
Joint lock 128.19 21.65 50 40608 1025 29910795
Mycobacterium tuberculosis complex test positive 126.39 21.65 48 40610 913 29910907
Hand deformity 122.85 21.65 57 40601 1816 29910004
C-reactive protein increased 122.29 21.65 215 40443 43258 29868562
Liver function test increased 120.89 21.65 109 40549 11107 29900713
Completed suicide 120.85 21.65 3 40655 99489 29812331
Vomiting 120.44 21.65 75 40583 219743 29692077
Death 118.96 21.65 189 40469 357094 29554726
Arthritis 117.50 21.65 155 40503 24246 29887574
Acne cystic 116.48 21.65 38 40620 451 29911369
Osteoarthritis 111.51 21.65 131 40527 18218 29893602
Thrombocytopenia 111.17 21.65 25 40633 137019 29774801
Confusional state 110.58 21.65 24 40634 134810 29777010
Abdominal discomfort 108.23 21.65 218 40440 48573 29863247
Diverticulitis 106.77 21.65 125 40533 17320 29894500
Apparent death 106.52 21.65 64 40594 3478 29908342
Tooth loss 104.80 21.65 66 40592 3903 29907917
Neutropenia 103.15 21.65 24 40634 128516 29783304
Atlantoaxial instability 100.62 21.65 31 40627 301 29911519
Tuberculin test positive 100.46 21.65 41 40617 950 29910870
Spinal instability 99.36 21.65 31 40627 315 29911505
Dislocation of vertebra 99.32 21.65 32 40626 364 29911456
Mineral metabolism disorder 99.01 21.65 31 40627 319 29911501
Alopecia 93.66 21.65 123 40535 19152 29892668
Anaemia 93.39 21.65 87 40571 207905 29703915
Physical disability 91.76 21.65 40 40618 1097 29910723
Dehydration 91.63 21.65 27 40631 123512 29788308
Ill-defined disorder 90.30 21.65 90 40568 10394 29901426
Seizure 88.26 21.65 14 40644 98461 29813359
Limb discomfort 87.92 21.65 83 40575 8967 29902853
Cytology abnormal 86.92 21.65 29 40629 371 29911449
Mass 86.17 21.65 74 40584 7066 29904754
Knee arthroplasty 86.14 21.65 67 40591 5563 29906257
Drug tolerance decreased 85.33 21.65 38 40620 1098 29910722
Headache 84.15 21.65 477 40181 181829 29729991
Pulmonary thrombosis 83.26 21.65 69 40589 6274 29905546
Terminal state 83.01 21.65 55 40603 3549 29908271
Intervertebral disc space narrowing 79.95 21.65 31 40627 625 29911195
Nasopharyngitis 76.98 21.65 214 40444 58635 29853185
Neoplasm malignant 76.40 21.65 107 40551 17707 29894113
Sarcoidosis 76.14 21.65 47 40611 2682 29909138
Bradycardia 75.87 21.65 3 40655 65523 29846297
Rheumatoid factor positive 75.82 21.65 28 40630 491 29911329
Product use issue 74.21 21.65 181 40477 45835 29865985
Hip arthroplasty 74.09 21.65 52 40606 3688 29908132
Syncope 74.01 21.65 13 40645 84890 29826930
Overdose 73.33 21.65 13 40645 84324 29827496
Hyperkalaemia 73.26 21.65 4 40654 66006 29845814
Cardiac arrest 73.15 21.65 18 40640 92832 29818988
Pyrexia 71.24 21.65 187 40471 294302 29617518
Polyarthritis 70.76 21.65 48 40610 3221 29908599
Product dose omission in error 67.80 21.65 16 40642 47 29911773
Sleep disorder due to general medical condition, insomnia type 67.77 21.65 33 40625 1173 29910647
Respiratory failure 65.99 21.65 27 40631 100615 29811205
Disease progression 65.87 21.65 14 40644 79860 29831960
Photosensitivity reaction 65.28 21.65 73 40585 9621 29902199
Osteosclerosis 65.24 21.65 32 40626 1156 29910664
Drug ineffective for unapproved indication 64.97 21.65 77 40581 10803 29901017
Tachycardia 64.90 21.65 11 40647 73728 29838092
Colitis ulcerative 63.84 21.65 88 40570 14346 29897474
Decreased appetite 62.29 21.65 67 40591 149843 29761977
Gastrointestinal haemorrhage 62.27 21.65 18 40640 83428 29828392
Prerenal failure 62.01 21.65 36 40622 1835 29909985
Platelet count decreased 61.12 21.65 34 40624 106095 29805725
Tenderness 60.18 21.65 55 40603 5700 29906120
Tooth fracture 59.20 21.65 43 40615 3219 29908601
Joint noise 59.13 21.65 24 40634 548 29911272
General physical health deterioration 59.04 21.65 31 40627 99913 29811907
Pancytopenia 58.77 21.65 21 40637 85031 29826789
Plasma cell myeloma 57.04 21.65 4 40654 53458 29858362
Gastrointestinal disorder 56.81 21.65 121 40537 28016 29883804
Blood creatinine increased 55.98 21.65 27 40631 91348 29820472
Asthenia 55.37 21.65 138 40520 221152 29690668
Multiple organ dysfunction syndrome 54.71 21.65 10 40648 63477 29848343
Haematochezia 54.51 21.65 134 40524 34088 29877732
Intestinal sepsis 54.41 21.65 21 40637 418 29911402
Hallucination 54.34 21.65 3 40655 49056 29862764
Somnolence 54.28 21.65 32 40626 96731 29815089
Acne 53.42 21.65 65 40593 9371 29902449
Anti-cyclic citrullinated peptide antibody positive 53.24 21.65 24 40634 714 29911106
Inflammation 53.13 21.65 102 40556 21924 29889896
Product dose omission issue 52.66 21.65 255 40403 91376 29820444
Oral surgery 52.35 21.65 22 40636 550 29911270
Skin mass 52.32 21.65 41 40617 3441 29908379
Fine motor skill dysfunction 51.29 21.65 27 40631 1134 29910686
Joint arthroplasty 50.41 21.65 22 40636 605 29911215
Therapeutic response unexpected 49.87 21.65 61 40597 8842 29902978
Hair growth abnormal 49.84 21.65 22 40636 622 29911198
Grip strength decreased 49.72 21.65 33 40625 2135 29909685
Impaired work ability 49.62 21.65 49 40609 5594 29906226
Frequent bowel movements 49.38 21.65 59 40599 8346 29903474
Blood pressure decreased 48.86 21.65 4 40654 47071 29864749
Hypoglycaemia 48.58 21.65 6 40652 50975 29860845
Hypokalaemia 47.60 21.65 6 40652 50186 29861634
Haematuria 46.01 21.65 4 40654 44830 29866990
Rheumatoid factor increased 45.32 21.65 19 40639 472 29911348
Aspartate aminotransferase increased 44.94 21.65 15 40643 63407 29848413
Infection 43.93 21.65 216 40442 77858 29833962
Therapy interrupted 42.96 21.65 41 40617 4488 29907332
Intestinal polyp 42.80 21.65 22 40636 879 29910941
Fall 42.72 21.65 117 40541 181755 29730065
Hypoxia 42.40 21.65 7 40651 47847 29863973
Pre-existing condition improved 42.40 21.65 29 40629 1972 29909848
Joint effusion 42.25 21.65 37 40621 3626 29908194
Blood cholesterol increased 41.44 21.65 79 40579 16891 29894929
Adverse reaction 41.33 21.65 33 40625 2845 29908975
Alanine aminotransferase increased 41.03 21.65 25 40633 74251 29837569
Lymph node calcification 40.94 21.65 14 40644 194 29911626
Delirium 40.69 21.65 4 40654 40627 29871193
Rhinorrhoea 40.45 21.65 88 40570 20666 29891154
Fear of injection 40.24 21.65 19 40639 630 29911190
Hypoacusis 39.80 21.65 70 40588 14069 29897751
Off label use 39.22 21.65 513 40145 248777 29663043
Seronegative arthritis 39.05 21.65 20 40638 793 29911027
Dizziness 38.95 21.65 135 40523 194774 29717046
Dyspnoea 38.93 21.65 279 40379 333016 29578804
Atrial fibrillation 38.88 21.65 54 40604 108070 29803750
Coronary artery disease 38.43 21.65 10 40648 49702 29862118
Loss of consciousness 38.20 21.65 31 40627 79344 29832476
Infusion related reaction 38.10 21.65 5 40653 40559 29871261
Septic shock 37.14 21.65 20 40638 63587 29848233
Cardiac failure congestive 36.97 21.65 36 40622 84371 29827449
Therapy non-responder 36.42 21.65 105 40553 29348 29882472
Sinusitis 35.70 21.65 113 40545 33232 29878588
Nodule 35.62 21.65 38 40620 4750 29907070
Neck pain 35.47 21.65 84 40574 20860 29890960
Angioedema 35.46 21.65 3 40655 34381 29877439
Defaecation urgency 35.36 21.65 23 40635 1438 29910382
Ascites 34.78 21.65 4 40654 35917 29875903
Skin laceration 34.69 21.65 58 40600 11193 29900627
Dysphagia 34.34 21.65 17 40641 56681 29855139
Hyperglycaemia 33.88 21.65 4 40654 35196 29876624
Mental status changes 33.81 21.65 5 40653 37074 29874746
Oral disorder 33.37 21.65 34 40624 4028 29907792
Hepatic function abnormal 33.27 21.65 8 40650 41937 29869883
Pulmonary fibrosis 32.83 21.65 69 40589 15821 29895999
Psoriatic arthropathy 32.06 21.65 68 40590 15693 29896127
Respiratory distress 31.12 21.65 4 40654 32968 29878852
Lipids increased 30.59 21.65 18 40640 941 29910879
Dysarthria 30.53 21.65 3 40655 30487 29881333
Feeling abnormal 30.47 21.65 155 40503 56601 29855219
Influenza 30.30 21.65 128 40530 43270 29868550
Nodal osteoarthritis 30.12 21.65 9 40649 78 29911742
Stomatitis 30.06 21.65 115 40543 37164 29874656
Finger deformity 30.02 21.65 18 40640 974 29910846
Coma 29.66 21.65 9 40649 40440 29871380
Malaise 29.37 21.65 351 40307 166611 29745209
Therapy cessation 29.29 21.65 64 40594 15073 29896747
Arthritis bacterial 29.00 21.65 33 40625 4431 29907389
Pneumonia aspiration 28.44 21.65 8 40650 37772 29874048
Melaena 28.17 21.65 5 40653 32432 29879388
Oxygen saturation decreased 27.89 21.65 12 40646 43428 29868392
Feeding disorder 27.79 21.65 37 40621 5834 29905986
Cutaneous symptom 26.59 21.65 11 40647 264 29911556
Renal impairment 26.47 21.65 46 40612 84138 29827682
Rheumatoid factor 26.31 21.65 8 40650 74 29911746
Back pain 26.29 21.65 233 40425 102363 29809457
Thrombosis 26.02 21.65 120 40538 42111 29869709
Cardiac failure 25.85 21.65 46 40612 83372 29828448
Mucosal inflammation 25.84 21.65 5 40653 30489 29881331
Hernia 25.75 21.65 44 40614 8642 29903178
Cerebral infarction 25.37 21.65 3 40655 26370 29885450
Immune recovery uveitis 25.09 21.65 6 40652 19 29911801
Musculoskeletal disorder 24.99 21.65 32 40626 4857 29906963
Suicidal ideation 24.79 21.65 9 40649 36105 29875715
Urinary retention 24.72 21.65 7 40651 32910 29878910
Cerebral haemorrhage 24.69 21.65 7 40651 32880 29878940
Oedema 24.40 21.65 14 40644 42979 29868841
Trigger finger 24.37 21.65 14 40644 699 29911121
Intentional product use issue 24.30 21.65 106 40552 36334 29875486
Hepatocellular injury 24.25 21.65 3 40655 25468 29886352
Illness 24.25 21.65 26 40632 3268 29908552
Interstitial lung disease 24.12 21.65 152 40506 60045 29851775
Cholestasis 23.61 21.65 3 40655 24947 29886873
Blood alkaline phosphatase increased 23.09 21.65 7 40651 31480 29880340
Bone marrow failure 23.00 21.65 6 40652 29779 29882041
Heart rate increased 22.86 21.65 12 40646 38709 29873111
Pleural effusion 22.81 21.65 41 40617 74025 29837795
Acute myocardial infarction 22.69 21.65 23 40635 52916 29858904
Hepatic enzyme increased 22.00 21.65 97 40561 33397 29878423
Intentional dose omission 21.89 21.65 17 40641 1408 29910412
Product use in unapproved indication 21.87 21.65 173 40485 73520 29838300
Bowel movement irregularity 21.78 21.65 21 40637 2328 29909492

Pharmacologic Action:

SourceCodeDescription
ATC L04AA29 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000190857 Janus Kinase Inhibitors
FDA EPC N0000190858 Janus Kinase Inhibitor
CHEBI has role CHEBI:35842 antirheumatic agent
CHEBI has role CHEBI:76617 abl inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Rheumatoid arthritis indication 69896004 DOID:7148

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.27 acidic
pKa2 6.48 Basic
pKa3 0.91 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE XELJANZ PF PRISM CV N203214 May 30, 2018 RX TABLET ORAL May 30, 2021 TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 5MG BASE XELJANZ PF PRISM CV N203214 Nov. 6, 2012 RX TABLET ORAL May 30, 2021 TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 5MG BASE XELJANZ PF PRISM CV N203214 Nov. 6, 2012 RX TABLET ORAL Sept. 25, 2023 NEW PATIENT POPULATION
EQ 1MG/ML BASE XELJANZ PFIZER N213082 Sept. 25, 2020 RX SOLUTION ORAL Sept. 25, 2023 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
JAK2/TYK2 Kinase INHIBITOR IC50 6.64 CHEMBL CHEMBL
JAK1/TYK2 Kinase INHIBITOR IC50 7.46 CHEMBL CHEMBL
JAK2/JAK1 Kinase INHIBITOR IC50 6.39 DRUG LABEL DRUG LABEL
JAK3/JAK1 Kinase INHIBITOR IC50 7.25 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR Kd 9.24 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase Kd 6.27 CHEMBL
Ribosomal protein S6 kinase alpha-1 Kinase Kd 5.85 CHEMBL
JAK1/JAK2/TYK2 Kinase INHIBITOR IC50 7.12 CHEMBL
Tyrosine-protein kinase JAK1 Kinase INHIBITOR Ki 9.17 CHEMBL
G protein-coupled receptor kinase 7 Kinase Kd 5.37 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 5.92 CHEMBL
Rho-associated protein kinase 1 Kinase Kd 6.33 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase Kd 6.26 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 5.15 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 5.80 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR Ki 8.36 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D Kinase Kd 5.80 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 5.37 CHEMBL
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 8.48 WOMBAT-PK
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kinase Kd 5.46 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.19 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 6.38 CHEMBL
Tyrosine-protein kinase Fyn Kinase Kd 5.96 CHEMBL
Protein kinase C delta type Kinase Kd 5.70 CHEMBL
Serine/threonine-protein kinase DCLK3 Kinase Kd 8.35 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 5.48 CHEMBL
Myotonin-protein kinase Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 6.34 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 6.62 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 5.57 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 6.77 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.32 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.92 CHEMBL
Ribosomal protein S6 kinase alpha-2 Kinase Kd 6.22 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase DCLK1 Kinase Kd 5.17 CHEMBL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase PknB Kinase Kd 5.70 CHEMBL
Tyrosine-protein kinase JAK3 Kinase IC50 7.32 CHEMBL
Tyrosine-protein kinase JAK2 Kinase IC50 5.69 CHEMBL

External reference:

IDSource
D09783 KEGG_DRUG
4031786 VUID
N0000186059 NUI
540737-29-9 SECONDARY_CAS_RN
4031786 VANDF
C3179368 UMLSCUI
CHEBI:71200 CHEBI
MI1 PDB_CHEM_ID
CHEMBL221959 ChEMBL_ID
CHEMBL459769 ChEMBL_ID
CHEMBL2103743 ChEMBL_ID
9926791 PUBCHEM_CID
C479163 MESH_SUPPLEMENTAL_RECORD_UI
9298 INN_ID
DB08895 DRUGBANK_ID
87LA6FU830 UNII
5677 IUPHAR_LIGAND_ID
1357536 RXNORM
194456 MMSL
28976 MMSL
31571 MMSL
d07925 MMSL
014743 NDDF
014744 NDDF
704313003 SNOMEDCT_US
704314009 SNOMEDCT_US
704316006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
XELJANZ XR HUMAN PRESCRIPTION DRUG LABEL 1 0069-0501 TABLET, FILM COATED, EXTENDED RELEASE 11 mg ORAL NDA 35 sections
XELJANZ XR HUMAN PRESCRIPTION DRUG LABEL 1 0069-0502 TABLET, FILM COATED, EXTENDED RELEASE 22 mg ORAL NDA 35 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-1001 TABLET, FILM COATED 5 mg ORAL NDA 35 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-1002 TABLET, FILM COATED 10 mg ORAL NDA 35 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-1029 SOLUTION 1 mg ORAL NDA 35 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 63539-012 TABLET, FILM COATED 5 mg ORAL NDA 30 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 63539-016 TABLET, FILM COATED 10 mg ORAL NDA 30 sections
XELJANZ XR HUMAN PRESCRIPTION DRUG LABEL 1 63539-501 TABLET, EXTENDED RELEASE 11 mg ORAL NDA 30 sections
XELJANZ XR HUMAN PRESCRIPTION DRUG LABEL 1 63539-502 TABLET, EXTENDED RELEASE 22 mg ORAL NDA 30 sections