tofacitinib Indications/Contra | FAERs | Orange Book | 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

Drug dosage:

DoseUnitRoute
10 mg O

Approvals:

DateAgencyCompanyOrphan
Nov. 6, 2012 FDA PF PRISM CV

FDA Adverse Event Reporting System

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 13258.94 40.85 5413 25580 180648 4427351
Arthralgia 8746.00 40.85 3230 27763 78764 4529235
Joint swelling 6470.19 40.85 1916 29077 22162 4585837
Condition aggravated 6138.19 40.85 2283 28710 55888 4552111
Pain 5809.30 40.85 2498 28495 90372 4517627
Musculoskeletal stiffness 5773.96 40.85 1663 29330 17239 4590760
Rheumatoid arthritis 5365.62 40.85 1675 29318 23324 4584675
Synovitis 4056.64 40.85 902 30091 2703 4605296
Fatigue 3960.26 40.85 2222 28771 143344 4464655
Peripheral swelling 3932.53 40.85 1347 29646 25345 4582654
Pain in extremity 3869.04 40.85 1685 29308 62054 4545945
Headache 3858.70 40.85 2061 28932 120312 4487687
Therapeutic product effect incomplete 3133.66 40.85 1020 29973 16188 4591811
Herpes zoster 2668.34 40.85 886 30107 14977 4593022
Nasopharyngitis 2531.58 40.85 1038 29955 32479 4575520
Malaise 2418.87 40.85 1370 29623 88787 4519212
Nausea 1870.25 40.85 1509 29484 175824 4432175
Joint range of motion decreased 1822.87 40.85 448 30545 2286 4605713
Abdominal discomfort 1815.22 40.85 782 30211 27626 4580373
Sinusitis 1806.63 40.85 731 30262 21981 4586018
Infection 1776.71 40.85 828 30165 35314 4572685
Diarrhoea 1760.08 40.85 1361 29632 148824 4459175
Musculoskeletal pain 1671.73 40.85 634 30359 15954 4592045
Swelling 1662.95 40.85 704 30289 23778 4584221
Rash 1641.99 40.85 1148 29845 107240 4500759
Loss of personal independence in daily activities 1514.85 40.85 491 30502 7614 4600385
Contraindicated product administered 1506.17 40.85 440 30553 4711 4603288
Cough 1499.38 40.85 850 30143 54737 4553262
Back pain 1493.42 40.85 821 30172 49778 4558221
Drug intolerance 1458.63 40.85 620 30373 21126 4586873
Blood cholesterol increased 1448.38 40.85 483 30510 8223 4599776
Product dose omission 1431.50 40.85 881 30112 66081 4541918
Urinary tract infection 1421.67 40.85 749 30244 41641 4566358
Upper respiratory tract infection 1403.25 40.85 531 30462 13256 4594743
Weight increased 1395.53 40.85 705 30288 35876 4572123
Arthropathy 1339.58 40.85 480 30513 10218 4597781
Pneumonia 1308.83 40.85 981 30012 101834 4506165
Joint stiffness 1303.89 40.85 408 30585 5603 4602396
Tenderness 1279.55 40.85 346 30647 2717 4605282
Alopecia 1266.85 40.85 607 30386 27473 4580526
Influenza 1232.72 40.85 543 30450 20180 4587819
Therapeutic product effect decreased 1159.44 40.85 505 30488 18248 4589751
Treatment failure 1115.39 40.85 453 30540 13694 4594305
Abdominal pain upper 1090.58 40.85 590 30403 34525 4573474
Bronchitis 1066.83 40.85 486 30507 19554 4588445
Fall 1066.42 40.85 778 30215 77268 4530731
Oropharyngeal pain 1059.47 40.85 463 30530 16856 4591143
Arthritis 1047.87 40.85 438 30555 14262 4593737
Product use issue 1002.15 40.85 499 30494 24537 4583462
Rhinorrhoea 998.77 40.85 400 30593 11642 4596357
Drug hypersensitivity 913.69 40.85 673 30320 67727 4540272
Dry mouth 895.58 40.85 379 30614 12722 4595277
Dry eye 869.98 40.85 294 30699 5207 4602792
Gait disturbance 839.59 40.85 505 30488 36135 4571864
Fibromyalgia 798.89 40.85 252 30741 3549 4604450
Neck pain 798.84 40.85 337 30656 11215 4596784
Hepatic enzyme increased 774.39 40.85 377 30616 17614 4590385
C-reactive protein abnormal 772.04 40.85 188 30805 912 4607087
Tuberculin test positive 727.30 40.85 179 30814 915 4607084
Myalgia 724.48 40.85 484 30509 41564 4566435
Muscle spasms 713.19 40.85 450 30543 35040 4572959
Osteoarthritis 707.01 40.85 293 30700 9311 4598688
Nasal congestion 698.19 40.85 299 30694 10327 4597672
Insomnia 693.68 40.85 485 30508 44860 4563139
Blood pressure increased 671.81 40.85 405 30588 29055 4578944
Dyspnoea 661.14 40.85 767 30226 138218 4469781
Dyspepsia 656.68 40.85 325 30668 15729 4592270
Therapeutic response unexpected 651.07 40.85 252 30741 6670 4601329
Hypoaesthesia 642.34 40.85 404 30589 31261 4576738
Osteoporosis 641.41 40.85 245 30748 6250 4601749
Liver function test increased 636.31 40.85 230 30763 5004 4602995
Pre-existing condition improved 624.86 40.85 152 30841 733 4607266
Red blood cell sedimentation rate increased 621.20 40.85 202 30791 3151 4604848
Abdominal pain 612.29 40.85 504 30489 59520 4548479
Dizziness 611.68 40.85 630 30363 99241 4508758
Joint effusion 601.25 40.85 174 30819 1789 4606210
Grip strength decreased 597.36 40.85 163 30830 1325 4606674
Hand deformity 596.28 40.85 160 30833 1212 4606787
Contusion 578.61 40.85 317 30676 18941 4589058
Product use in unapproved indication 574.91 40.85 347 30646 24926 4583073
Sensitivity to weather change 563.98 40.85 132 30861 521 4607478
Gastrointestinal disorder 548.73 40.85 288 30705 15773 4592226
Mobility decreased 541.93 40.85 268 30725 12937 4595062
Drug effective for unapproved indication 535.07 40.85 121 30872 394 4607605
Diverticulitis 531.81 40.85 219 30774 6838 4601161
Nodule 531.48 40.85 179 30814 3130 4604869
Depression 512.15 40.85 413 30580 47320 4560679
Hypertension 504.12 40.85 420 30573 50378 4557621
Red blood cell sedimentation rate abnormal 502.97 40.85 120 30873 524 4607475
Therapy cessation 495.61 40.85 223 30770 8677 4599322
Gastric disorder 492.86 40.85 197 30796 5685 4602314
Joint noise 489.01 40.85 124 30869 730 4607269
Feeling abnormal 484.39 40.85 358 30635 36047 4571952
Sleep disorder 478.26 40.85 234 30759 11029 4596970
Hypersensitivity 471.58 40.85 360 30633 38061 4569938
Paraesthesia 468.55 40.85 346 30647 34787 4573212
Constipation 467.59 40.85 372 30621 41782 4566217
Pyrexia 466.63 40.85 566 30427 106578 4501421
Foot deformity 462.66 40.85 152 30841 2451 4605548
Acne 462.13 40.85 183 30810 5149 4602850
Asthenia 458.76 40.85 505 30488 85658 4522341
C-reactive protein increased 432.58 40.85 228 30765 12584 4595415
Bone erosion 425.40 40.85 110 30883 708 4607291
Intentional product misuse 402.60 40.85 247 30746 18246 4589753
Cystitis 379.57 40.85 175 30818 7205 4600794
Mycobacterium tuberculosis complex test positive 376.41 40.85 100 30893 725 4607274
Vomiting 373.40 40.85 537 30456 119162 4488837
Limb discomfort 368.19 40.85 153 30840 4885 4603114
Crepitations 367.29 40.85 107 30886 1127 4606872
Interstitial lung disease 350.93 40.85 230 30763 19055 4588944
Bursitis 347.39 40.85 124 30869 2594 4605405
Stress 347.06 40.85 181 30812 9767 4598232
Inflammation 346.13 40.85 182 30811 9989 4598010
Off label use 343.85 40.85 538 30455 128575 4479424
Anxiety 341.25 40.85 329 30664 47682 4560317
Pruritus 337.80 40.85 397 30596 72175 4535824
Localised infection 330.83 40.85 140 30853 4681 4603318
Femur fracture 325.73 40.85 165 30828 8374 4599625
Immune system disorder 324.55 40.85 114 30879 2271 4605728
Mouth ulceration 313.65 40.85 145 30848 6005 4601994
Memory impairment 313.16 40.85 219 30774 20184 4587815
Rheumatoid factor positive 310.13 40.85 80 30913 509 4607490
Drug ineffective for unapproved indication 308.86 40.85 141 30852 5670 4602329
Sinus disorder 306.52 40.85 124 30869 3690 4604309
Rheumatoid nodule 306.34 40.85 85 30908 739 4607260
Lower respiratory tract infection 298.38 40.85 164 30829 9839 4598160
Cataract 295.61 40.85 161 30832 9485 4598514
Carpal tunnel syndrome 295.41 40.85 112 30881 2792 4605207
Fungal infection 295.26 40.85 151 30842 7818 4600181
Oral herpes 289.81 40.85 113 30880 3045 4604954
Synovial cyst 289.37 40.85 89 30904 1144 4606855
Viral infection 281.48 40.85 147 30846 7951 4600048
Chest pain 275.96 40.85 301 30692 50399 4557600
Abdominal distension 275.83 40.85 193 30800 17796 4590203
Ear infection 275.30 40.85 124 30869 4829 4603170
Migraine 275.27 40.85 174 30819 13535 4594464
Impaired work ability 273.39 40.85 107 30886 2913 4605086
Gastrooesophageal reflux disease 271.81 40.85 178 30815 14715 4593284
Joint injury 267.14 40.85 111 30882 3541 4604458
Weight decreased 266.71 40.85 306 30687 54158 4553841
Muscular weakness 263.94 40.85 220 30773 26330 4581669
Erythema 262.00 40.85 268 30725 41672 4566327
Influenza like illness 260.41 40.85 191 30802 18962 4589037
Musculoskeletal discomfort 257.77 40.85 105 30888 3181 4604818
Nail disorder 257.31 40.85 88 30905 1613 4606386
Intentional product use issue 246.49 40.85 129 30864 7006 4600993
Kidney infection 244.12 40.85 102 30891 3300 4604699
Stomatitis 242.31 40.85 173 30820 16466 4591533
Anti-cyclic citrullinated peptide antibody positive 241.46 40.85 56 30937 210 4607789
Onychomycosis 237.77 40.85 72 30921 875 4607124
Joint laxity 234.66 40.85 44 30949 31 4607968
Impaired healing 233.71 40.85 132 30861 8347 4599652
Lung disorder 233.43 40.85 151 30842 12220 4595779
Synovial fluid analysis 232.68 40.85 40 30953 2 4607997
Cellulitis 232.30 40.85 169 30824 16563 4591436
Disease recurrence 227.42 40.85 124 30869 7317 4600682
Night sweats 226.24 40.85 116 30877 6035 4601964
Productive cough 226.10 40.85 134 30859 9279 4598720
Nephrolithiasis 223.21 40.85 131 30862 8908 4599091
Liver function test abnormal 219.09 40.85 155 30838 14537 4593462
Soft tissue disorder 219.03 40.85 56 30937 342 4607657
Neoplasm malignant 216.53 40.85 138 30855 10883 4597116
Pollakiuria 215.10 40.85 118 30875 7047 4600952
Tooth infection 214.79 40.85 89 30904 2818 4605181
Adverse drug reaction 214.03 40.85 153 30840 14586 4593413
Bone disorder 211.32 40.85 103 30890 4804 4603195
Chills 209.18 40.85 200 30793 28639 4579360
Limb injury 207.38 40.85 96 30897 3985 4604014
Ulcer 206.99 40.85 90 30903 3217 4604782
Finger deformity 206.80 40.85 67 30926 1030 4606969
Synovial disorder 205.73 40.85 44 30949 101 4607898
Hot flush 205.20 40.85 130 30863 10145 4597854
Visual impairment 201.16 40.85 165 30828 19295 4588704
Sjogren's syndrome 200.74 40.85 68 30925 1209 4606790
Anaemia 198.07 40.85 304 30689 71256 4536743
Tenosynovitis stenosans 196.99 40.85 44 30949 133 4607866
Tuberculosis 194.64 40.85 95 30898 4444 4603555
Joint dislocation 193.84 40.85 76 30917 2078 4605921
Hair growth abnormal 192.43 40.85 60 30933 809 4607190
Lipids increased 192.14 40.85 55 30938 541 4607458
Respiratory tract infection 189.83 40.85 109 30884 7111 4600888
Coeliac disease 187.43 40.85 65 30928 1244 4606755
Scleritis 186.77 40.85 51 30942 415 4607584
Non-Hodgkin's lymphoma 185.13 40.85 73 30920 2027 4605972
Flatulence 185.11 40.85 112 30881 8052 4599947
Haematochezia 184.39 40.85 125 30868 10939 4597060
Wound 178.41 40.85 90 30903 4522 4603477
Skin lesion 177.68 40.85 106 30887 7427 4600572
Gait inability 177.26 40.85 116 30877 9569 4598430
Skin disorder 174.99 40.85 99 30894 6277 4601722
Pulmonary fibrosis 169.76 40.85 93 30900 5537 4602462
Pelvic fracture 168.37 40.85 65 30928 1703 4606296
Increased tendency to bruise 166.69 40.85 70 30923 2293 4605706
Knee arthroplasty 166.59 40.85 82 30911 3907 4604092
Hyperhidrosis 165.01 40.85 179 30814 29738 4578261
Oedema peripheral 164.82 40.85 211 30782 41761 4566238
Joint lock 162.74 40.85 49 30944 583 4607416
Thrombosis 161.41 40.85 142 30851 18262 4589737
Swelling face 160.04 40.85 129 30864 14711 4593288
Asthma 158.30 40.85 137 30856 17237 4590762
Discomfort 156.34 40.85 101 30892 8149 4599850
Pulmonary embolism 155.98 40.85 186 30807 34240 4573759
Hip arthroplasty 155.62 40.85 70 30923 2715 4605284
Eye infection 154.70 40.85 63 30930 1906 4606093
Systemic lupus erythematosus 154.09 40.85 86 30907 5310 4602689
Gastroenteritis viral 153.56 40.85 76 30917 3664 4604335
Rheumatic fever 151.89 40.85 33 30960 84 4607915
Flank pain 151.48 40.85 68 30925 2625 4605374
Nodal osteoarthritis 148.93 40.85 33 30960 95 4607904
Foot fracture 148.84 40.85 74 30919 3603 4604396
Surgery 148.58 40.85 103 30890 9344 4598655
Mass 148.13 40.85 70 30923 3045 4604954
Blister 147.91 40.85 111 30882 11398 4596601
Therapeutic product effect delayed 147.16 40.85 49 30944 824 4607175
Cushingoid 146.42 40.85 52 30941 1070 4606929
Poor quality sleep 146.19 40.85 71 30922 3284 4604715
Back disorder 145.91 40.85 66 30927 2594 4605405
Glossodynia 145.80 40.85 67 30926 2733 4605266
Therapeutic product effect variable 143.62 40.85 39 30954 310 4607689
Ill-defined disorder 143.15 40.85 84 30909 5706 4602293
Oral pain 142.59 40.85 80 30913 4990 4603009
Wheezing 141.89 40.85 107 30886 11067 4596932
Tooth abscess 138.92 40.85 67 30926 3051 4604948
Exostosis 138.59 40.85 58 30935 1883 4606116
Feeling jittery 137.82 40.85 66 30927 2958 4605041
Onychomadesis 136.55 40.85 44 30949 664 4607335
Spinal stenosis 135.45 40.85 59 30934 2117 4605882
Groin pain 134.50 40.85 59 30934 2154 4605845
Low density lipoprotein increased 133.99 40.85 61 30932 2434 4605565
Laryngitis 133.46 40.85 56 30937 1830 4606169
Musculoskeletal disorder 132.15 40.85 69 30924 3726 4604273
Dry skin 130.79 40.85 101 30892 10821 4597178
Trigger finger 130.33 40.85 42 30951 634 4607365
Ocular hyperaemia 129.86 40.85 82 30911 6358 4601641
Pleuritic pain 129.44 40.85 48 30945 1122 4606877
Antinuclear antibody positive 128.59 40.85 52 30941 1544 4606455
Palpitations 127.20 40.85 143 30850 24703 4583296
Prescribed overdose 126.83 40.85 68 30925 3876 4604123
Pulmonary mass 126.08 40.85 65 30928 3418 4604581
Burning sensation 123.35 40.85 101 30892 11771 4596228
Arthritis bacterial 121.15 40.85 50 30943 1566 4606433
Eye disorder 119.91 40.85 72 30921 5102 4602897
Conjunctivitis 119.58 40.85 68 30925 4352 4603647
Disability 118.52 40.85 48 30945 1431 4606568
Blood triglycerides increased 118.00 40.85 72 30921 5253 4602746
Tinnitus 117.16 40.85 88 30905 9045 4598954
Skin mass 117.06 40.85 50 30943 1709 4606290
Pain in jaw 116.17 40.85 86 30907 8646 4599353
Sepsis 115.58 40.85 180 30813 42659 4565340
Respiratory tract congestion 115.40 40.85 62 30931 3549 4604450
Psoriasis 115.32 40.85 150 30843 30134 4577865
Sinus congestion 114.86 40.85 58 30935 2919 4605080
Decreased appetite 113.66 40.85 208 30785 56189 4551810
Skin ulcer 113.62 40.85 79 30914 7199 4600800
Body height decreased 113.60 40.85 49 30944 1716 4606283
Rheumatoid factor increased 113.46 40.85 33 30960 345 4607654
Depressed mood 112.97 40.85 85 30908 8759 4599240
Dysphonia 112.81 40.85 91 30902 10383 4597616
Liver disorder 112.71 40.85 100 30893 12998 4595001
Lung neoplasm malignant 112.61 40.85 77 30916 6829 4601170
Spinal pain 112.13 40.85 51 30942 2030 4605969
Movement disorder 112.04 40.85 67 30926 4712 4603287
White blood cell count decreased 110.97 40.85 154 30839 32911 4575088
Intentional dose omission 110.89 40.85 36 30957 557 4607442
Extremity contracture 109.09 40.85 28 30965 174 4607825
Upper limb fracture 108.91 40.85 60 30933 3610 4604389
Dysstasia 108.59 40.85 66 30927 4781 4603218
Urticaria 107.76 40.85 167 30826 39406 4568593
Leukopenia 107.68 40.85 123 30870 21613 4586386
Hepatic steatosis 107.66 40.85 72 30921 6156 4601843
Staphylococcal infection 107.01 40.85 89 30904 10599 4597400
Hernia 106.55 40.85 53 30940 2582 4605417
Pemphigus 106.03 40.85 40 30953 982 4607017
Diabetes mellitus 105.74 40.85 104 30889 15397 4592602
Intervertebral disc protrusion 105.02 40.85 64 30929 4658 4603341
Skin cancer 103.89 40.85 57 30936 3402 4604597
Wrist deformity 103.09 40.85 26 30967 149 4607850
Osteomyelitis 103.08 40.85 70 30923 6138 4601861
Viral upper respiratory tract infection 102.65 40.85 45 30948 1640 4606359
Ankle fracture 102.44 40.85 54 30939 2973 4605026
Pneumonia viral 102.44 40.85 38 30955 889 4607110
Inflammatory marker increased 102.27 40.85 39 30954 987 4607012
Eye irritation 101.66 40.85 65 30928 5149 4602850
Renal disorder 99.85 40.85 81 30912 9315 4598684
Eye pain 98.19 40.85 74 30919 7643 4600356
Hypoacusis 97.35 40.85 68 30925 6241 4601758
Intervertebral disc degeneration 97.08 40.85 48 30945 2308 4605691
Chronic obstructive pulmonary disease 96.80 40.85 94 30899 13700 4594299
Sciatica 96.74 40.85 52 30941 2979 4605020
Nerve compression 96.65 40.85 42 30951 1498 4606501
Scar 95.80 40.85 51 30942 2865 4605134
Soft tissue swelling 95.72 40.85 23 30970 104 4607895
Arthritis infective 95.03 40.85 38 30955 1095 4606904
Tendonitis 94.77 40.85 56 30937 3852 4604147
Skin discolouration 94.43 40.85 76 30917 8642 4599357
Hepatitis B virus test positive 93.82 40.85 23 30970 115 4607884
Throat irritation 93.41 40.85 70 30923 7168 4600831
Colitis ulcerative 93.39 40.85 64 30929 5696 4602303
Therapeutic response decreased 93.11 40.85 94 30899 14357 4593642
Balance disorder 92.63 40.85 99 30894 16157 4591842
Photophobia 91.42 40.85 54 30939 3712 4604287
Rotator cuff syndrome 91.22 40.85 49 30944 2803 4605196
Pharyngitis 90.49 40.85 53 30940 3586 4604413
Epistaxis 90.35 40.85 107 30886 19536 4588463
Haemoglobin decreased 88.97 40.85 149 30844 37508 4570491
Therapy non-responder 88.75 40.85 96 30897 15881 4592118
Vision blurred 88.47 40.85 119 30874 24684 4583315
Toothache 88.29 40.85 53 30940 3753 4604246
Feeling hot 88.28 40.85 79 30914 10382 4597617
Fungal skin infection 87.55 40.85 34 30959 905 4607094
Bone pain 87.39 40.85 88 30905 13398 4594601
Neuralgia 87.04 40.85 56 30937 4484 4603515
Rib fracture 87.01 40.85 56 30937 4486 4603513
Colon cancer 86.78 40.85 54 30939 4079 4603920
Renal impairment 86.48 40.85 119 30874 25219 4582780
Ophthalmic herpes zoster 85.00 40.85 29 30964 527 4607472
Lymphadenopathy 84.78 40.85 77 30916 10315 4597684
Dysuria 84.25 40.85 69 30924 8041 4599958
Road traffic accident 84.13 40.85 70 30923 8339 4599660
Muscle fatigue 83.94 40.85 31 30962 716 4607283
Pustular psoriasis 83.59 40.85 37 30956 1380 4606619
Wound infection 83.32 40.85 44 30949 2431 4605568
Post procedural infection 82.36 40.85 40 30953 1849 4606150
Seasonal allergy 81.96 40.85 43 30950 2344 4605655
Injection site reaction 80.93 40.85 102 30891 19848 4588151
Immunosuppression 79.37 40.85 40 30953 2004 4605995
Photosensitivity reaction 78.80 40.85 53 30940 4573 4603426
Furuncle 78.64 40.85 38 30955 1737 4606262
Blood glucose increased 78.61 40.85 111 30882 24093 4583906
Middle insomnia 77.90 40.85 42 30951 2420 4605579
Hip fracture 77.52 40.85 61 30932 6713 4601286
Skin infection 76.87 40.85 43 30950 2665 4605334
Red blood cell count decreased 76.67 40.85 66 30927 8237 4599762
Ear pain 76.32 40.85 48 30945 3694 4604305
Joint contracture 76.00 40.85 25 30968 404 4607595
Physical disability 75.80 40.85 24 30969 341 4607658
Incorrect dosage administered 75.36 40.85 28 30965 658 4607341
Blood creatinine increased 75.27 40.85 115 30878 26785 4581214
Breast cancer 75.03 40.85 72 30921 10339 4597660
Iron deficiency anaemia 75.00 40.85 46 30947 3386 4604613
Lymphoma 74.89 40.85 52 30941 4726 4603273
Joint warmth 74.42 40.85 24 30969 363 4607636
Multiple fractures 74.10 40.85 31 30962 1005 4606994
Temperature intolerance 73.97 40.85 35 30958 1526 4606473
Skin papilloma 73.81 40.85 31 30962 1015 4606984
Spinal fracture 72.74 40.85 48 30945 4012 4603987
Lower limb fracture 72.63 40.85 43 30950 2968 4605031
Amnesia 72.39 40.85 78 30915 12843 4595156
Osteopenia 71.96 40.85 41 30952 2633 4605366
Myocardial infarction 71.77 40.85 159 30834 49217 4558782
Onychoclasis 71.35 40.85 31 30962 1105 4606894
Deformity 71.26 40.85 27 30966 671 4607328
Oral mucosal blistering 71.06 40.85 32 30961 1244 4606755
Pericarditis 70.85 40.85 44 30949 3311 4604688
Heart rate increased 70.80 40.85 92 30901 18450 4589549
Wrist fracture 69.26 40.85 37 30956 2093 4605906
Herpes virus infection 68.69 40.85 33 30960 1489 4606510
Deep vein thrombosis 68.54 40.85 107 30886 25387 4582612
Rosacea 68.38 40.85 27 30966 752 4607247
Fracture 68.32 40.85 48 30945 4445 4603554
Atelectasis 67.77 40.85 46 30947 4029 4603970
Cerebrovascular accident 67.63 40.85 141 30852 41859 4566140
Cyst 67.27 40.85 38 30955 2400 4605599
Pharyngitis streptococcal 66.57 40.85 36 30957 2087 4605912
Upper-airway cough syndrome 66.36 40.85 32 30961 1456 4606543
Blood pressure abnormal 65.85 40.85 40 30953 2893 4605106
Ligament sprain 65.35 40.85 35 30958 1990 4606009
Spinal disorder 65.34 40.85 34 30959 1822 4606177
Walking aid user 64.89 40.85 28 30965 981 4607018
Thyroid disorder 64.85 40.85 36 30957 2198 4605801
Tooth disorder 64.49 40.85 52 30941 5926 4602073
Deafness 64.08 40.85 49 30944 5170 4602829
Energy increased 63.66 40.85 26 30967 792 4607207
Type 2 diabetes mellitus 63.53 40.85 45 30948 4222 4603777
Malignant melanoma 63.19 40.85 44 30949 4017 4603982
Latent tuberculosis 63.09 40.85 24 30969 603 4607396
Bone swelling 62.86 40.85 20 30973 289 4607710
Meniscus injury 62.17 40.85 31 30962 1518 4606481
Clostridium difficile infection 62.02 40.85 48 30945 5156 4602843
Dysphagia 61.59 40.85 102 30891 25429 4582570
Respiratory disorder 61.52 40.85 57 30936 7831 4600168
Tendon rupture 61.51 40.85 41 30952 3485 4604514
Increased appetite 61.42 40.85 37 30956 2636 4605363
Paranasal sinus discomfort 61.18 40.85 23 30970 559 4607440
Limb deformity 61.13 40.85 21 30972 390 4607609
Dry throat 60.79 40.85 30 30963 1436 4606563
Decreased immune responsiveness 60.21 40.85 27 30966 1039 4606960
Nervousness 60.18 40.85 56 30937 7736 4600263
Laboratory test abnormal 60.00 40.85 63 30930 10070 4597929
Vitamin D decreased 59.93 40.85 30 30963 1481 4606518
Pulmonary thrombosis 59.73 40.85 33 30960 1996 4606003
Oedema 59.42 40.85 85 30908 18666 4589333
Rotator cuff repair 59.37 40.85 20 30973 349 4607650
Gastroenteritis 59.25 40.85 48 30945 5507 4602492
Chest discomfort 59.06 40.85 95 30898 23115 4584884
Irritable bowel syndrome 59.06 40.85 36 30957 2620 4605379
Gallbladder disorder 58.66 40.85 42 30951 4008 4603991
Aphonia 58.53 40.85 32 30961 1896 4606103
Rheumatoid factor negative 58.52 40.85 13 30980 38 4607961
Menopausal symptoms 57.89 40.85 20 30973 378 4607621
Sputum discoloured 57.87 40.85 32 30961 1939 4606060
Blood test abnormal 57.86 40.85 34 30959 2314 4605685
Tremor 57.52 40.85 121 30872 36138 4571861
Concussion 56.51 40.85 28 30965 1352 4606647
Rash papular 55.97 40.85 43 30950 4568 4603431
White blood cell count increased 55.57 40.85 74 30919 15193 4592806
Appendicitis 55.50 40.85 34 30959 2497 4605502
Fluid retention 55.48 40.85 64 30929 11357 4596642
Atrial fibrillation 55.24 40.85 109 30884 31106 4576893
Muscle strain 55.17 40.85 30 30963 1758 4606241
Chondropathy 55.08 40.85 21 30972 531 4607468
Somnolence 55.08 40.85 133 30860 43527 4564472
Gastrointestinal perforation 53.35 40.85 30 30963 1878 4606121
Epicondylitis 52.61 40.85 19 30974 411 4607588
Change of bowel habit 52.56 40.85 19 30974 412 4607587
Tendon disorder 52.46 40.85 27 30966 1414 4606585
Adverse reaction 52.39 40.85 33 30960 2546 4605453
Pneumocystis jirovecii pneumonia 52.20 40.85 44 30949 5334 4602665
Postoperative wound infection 52.10 40.85 30 30963 1965 4606034
Intervertebral disc disorder 51.96 40.85 24 30969 990 4607009
Death 51.73 40.85 369 30624 197794 4410205
Fine motor skill dysfunction 51.31 40.85 19 30974 442 4607557
High density lipoprotein increased 51.21 40.85 17 30976 283 4607716
Nerve injury 51.07 40.85 28 30965 1668 4606331
Adverse event 50.78 40.85 73 30920 16099 4591900
Sneezing 50.21 40.85 37 30956 3691 4604308
Oral discomfort 49.98 40.85 29 30964 1927 4606072
Raynaud's phenomenon 49.57 40.85 26 30967 1416 4606583
Spinal compression fracture 49.38 40.85 33 30960 2816 4605183
Malignant polyp 48.74 40.85 10 30983 17 4607982
Skin atrophy 48.47 40.85 23 30970 1009 4606990
Upper respiratory tract congestion 48.11 40.85 20 30973 638 4607361
Fear of injection 47.74 40.85 24 30969 1196 4606803
Sinusitis bacterial 47.49 40.85 14 30979 154 4607845
Spinal operation 46.72 40.85 24 30969 1252 4606747
Muscle tightness 46.70 40.85 33 30960 3084 4604915
Cardiac disorder 46.24 40.85 72 30921 17037 4590962
Sleep apnoea syndrome 46.05 40.85 38 30955 4473 4603526
Neuropathy peripheral 45.99 40.85 86 30907 23583 4584416
Swollen joint count increased 45.61 40.85 9 30984 11 4607988
Gilbert's syndrome 45.49 40.85 13 30980 127 4607872
Immobile 45.35 40.85 22 30971 1014 4606985
Limb operation 45.25 40.85 20 30973 743 4607256
Glaucoma 45.11 40.85 34 30959 3510 4604489
Immunodeficiency 45.07 40.85 26 30967 1709 4606290
Nail growth abnormal 45.01 40.85 14 30979 187 4607812
Vitamin D deficiency 44.96 40.85 28 30965 2117 4605882
Bursitis infective 44.87 40.85 14 30979 189 4607810
Sinus pain 44.84 40.85 15 30978 256 4607743
Hepatotoxicity 44.56 40.85 49 30944 8250 4599749
Musculoskeletal chest pain 44.46 40.85 35 30958 3853 4604146
Gingival bleeding 44.46 40.85 34 30959 3587 4604412
Large intestine perforation 43.84 40.85 30 30963 2662 4605337
Bowel movement irregularity 43.74 40.85 21 30972 946 4607053
Haemorrhage 43.71 40.85 88 30905 25474 4582525
Granulomatous rosacea 43.61 40.85 9 30984 16 4607983
Bacterial infection 43.05 40.85 37 30956 4606 4603393
Helicobacter infection 42.91 40.85 22 30971 1143 4606856
Crying 42.66 40.85 42 30951 6221 4601778
Injection site hypersensitivity 42.15 40.85 17 30976 501 4607498
Eye swelling 42.10 40.85 43 30950 6654 4601345
Pain of skin 41.43 40.85 27 30966 2209 4605790
Food poisoning 41.29 40.85 19 30974 777 4607222
Butterfly rash 41.00 40.85 14 30979 255 4607744
Ear discomfort 40.94 40.85 24 30969 1626 4606373
Pulmonary toxicity 40.93 40.85 26 30967 2035 4605964
Candida infection 40.87 40.85 38 30955 5243 4602756

Pharmacologic Action:

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

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE XELJANZ PF PRISM CV N203214 May 30, 2018 RX TABLET ORAL 7842699 Dec. 8, 2020 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 7091208 Dec. 8, 2020 TREATMENT OF RHEUMATOID ARTHRITIS
EQ 5MG BASE XELJANZ PF PRISM CV N203214 Nov. 6, 2012 RX TABLET ORAL 7842699 Dec. 8, 2020 TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 11MG BASE XELJANZ XR PFIZER INC N208246 Feb. 23, 2016 RX TABLET, EXTENDED RELEASE ORAL 7091208 Dec. 8, 2020 TREATMENT OF RHEUMATOID ARTHRITIS
EQ 11MG BASE XELJANZ XR PFIZER INC N208246 Feb. 23, 2016 RX TABLET, EXTENDED RELEASE ORAL 7842699 Dec. 8, 2020 TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)
EQ 22MG BASE XELJANZ XR PFIZER INC N208246 Dec. 12, 2019 RX TABLET, EXTENDED RELEASE ORAL 7842699 Dec. 8, 2020 TREATMENT OF ADULT PATIENTS WITH MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 5MG BASE XELJANZ PF PRISM CV N203214 Nov. 6, 2012 RX TABLET ORAL Dec. 14, 2020 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO METHOTREXATE OR OTHER NON-BIOLOGIC DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
EQ 11MG BASE XELJANZ XR PFIZER INC N208246 Feb. 23, 2016 RX TABLET, EXTENDED RELEASE ORAL Dec. 14, 2020 TREATMENT OF ADULT PATIENTS WITH ACTIVE PSORIATIC ARTHRITIS WHO HAVE HAD AN INADEQUATE RESPONSE OR INTOLERANCE TO METHOTREXATE OR OTHER NON-BIOLOGIC DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
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)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
JAK1/TYK2 Kinase INHIBITOR IC50 7.46 CHEMBL CHEMBL
JAK2/TYK2 Kinase INHIBITOR IC50 6.64 CHEMBL CHEMBL
JAK2/JAK1 Kinase INHIBITOR IC50 6.39 DRUG LABEL DRUG LABEL
JAK3/JAK1 Kinase INHIBITOR IC50 7.25 DRUG LABEL DRUG LABEL
Calcium/calmodulin-dependent protein kinase type 1 Kinase Kd 5.92 CHEMBL
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
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
Rho-associated protein kinase 1 Kinase Kd 6.33 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase DCLK1 Kinase Kd 5.17 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
C2930696 UMLSCUI
87LA6FU830 UNII
9298 INN_ID
CHEMBL221959 ChEMBL_ID
CHEMBL459769 ChEMBL_ID
540737-29-9 SECONDARY_CAS_RN
DB08895 DRUGBANK_ID
CHEBI:71200 CHEBI
C479163 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2103743 ChEMBL_ID
9926791 PUBCHEM_CID
5677 IUPHAR_LIGAND_ID
704316006 SNOMEDCT_US
1357536 RXNORM
28976 MMSL
d07925 MMSL
014743 NDDF
4031786 VANDF
704313003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-0501 TABLET, FILM COATED, EXTENDED RELEASE 11 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-0502 TABLET, FILM COATED, EXTENDED RELEASE 22 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-1001 TABLET, FILM COATED 5 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 0069-1002 TABLET, FILM COATED 10 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 63539-012 TABLET, FILM COATED 5 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 63539-016 TABLET, FILM COATED 10 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 63539-501 TABLET, EXTENDED RELEASE 11 mg ORAL NDA 20 sections
XELJANZ HUMAN PRESCRIPTION DRUG LABEL 1 63539-502 TABLET, EXTENDED RELEASE 22 mg ORAL NDA 20 sections