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: ONP

  • 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 10596.72 37.49 4210 19553 97414 2236908
Arthralgia 7068.66 37.49 2668 21095 51617 2282705
Condition aggravated 5224.53 37.49 1866 21897 30113 2304209
Joint swelling 4940.07 37.49 1530 22233 15289 2319033
Pain 4697.15 37.49 2073 21690 59784 2274538
Musculoskeletal stiffness 4631.76 37.49 1355 22408 10892 2323430
Rheumatoid arthritis 4171.85 37.49 1389 22374 17751 2316571
Fatigue 3456.94 37.49 1861 21902 83012 2251310
Synovitis 3354.60 37.49 773 22990 1953 2332369
Headache 3344.35 37.49 1787 21976 78392 2255930
Pain in extremity 3138.26 37.49 1403 22360 41137 2293185
Peripheral swelling 3120.85 37.49 1096 22667 16501 2317821
Therapeutic product effect incomplete 2432.90 37.49 801 22962 9730 2324592
Nasopharyngitis 2216.05 37.49 908 22855 21148 2313174
Malaise 2096.24 37.49 1164 22599 54421 2279901
Herpes zoster 1917.14 37.49 657 23106 9068 2325254
Nausea 1628.38 37.49 1294 22469 110895 2223427
Infection 1575.72 37.49 673 23090 17356 2316966
Abdominal discomfort 1543.26 37.49 657 23106 16799 2317523
Sinusitis 1534.16 37.49 644 23119 15882 2318440
Diarrhoea 1505.68 37.49 1098 22665 82466 2251856
Rash 1464.92 37.49 949 22814 58609 2275713
Swelling 1400.67 37.49 602 23161 15748 2318574
Joint range of motion decreased 1388.63 37.49 353 23410 1503 2332819
Urinary tract infection 1329.71 37.49 701 23062 29241 2305081
Musculoskeletal pain 1324.81 37.49 515 23248 10315 2324007
Cough 1310.34 37.49 718 23045 32399 2301923
Drug intolerance 1293.95 37.49 541 23222 13176 2321146
Blood cholesterol increased 1281.71 37.49 417 23346 4824 2329498
Product dose omission 1258.63 37.49 735 23028 37522 2296800
Weight increased 1244.92 37.49 610 23153 21727 2312595
Upper respiratory tract infection 1240.80 37.49 465 23298 8386 2325936
Back pain 1237.31 37.49 681 23082 30978 2303344
Contraindicated product administered 1209.37 37.49 351 23412 2670 2331652
Loss of personal independence in daily activities 1175.76 37.49 392 23371 4919 2329403
Alopecia 1116.70 37.49 564 23199 21437 2312885
Arthropathy 1115.68 37.49 409 23354 6907 2327415
Pneumonia 1106.45 37.49 743 23020 48553 2285769
Joint stiffness 1093.60 37.49 347 23416 3676 2330646
Influenza 1068.45 37.49 465 23298 12513 2321809
Tenderness 1055.64 37.49 286 23477 1632 2332690
Fall 994.79 37.49 684 23079 46415 2287907
Therapeutic product effect decreased 981.53 37.49 415 23348 10374 2323948
Treatment failure 940.62 37.49 360 23403 6879 2327443
Bronchitis 938.98 37.49 432 23331 13282 2321040
Oropharyngeal pain 935.80 37.49 409 23354 11109 2323213
Abdominal pain upper 908.02 37.49 492 23271 21608 2312714
Rhinorrhoea 843.69 37.49 336 23427 7164 2327158
Product use issue 834.93 37.49 384 23379 11785 2322537
Arthritis 812.87 37.49 355 23408 9613 2324709
Dry mouth 778.81 37.49 326 23437 7927 2326395
Drug hypersensitivity 737.33 37.49 569 23194 46074 2288248
Gait disturbance 736.29 37.49 432 23331 22113 2312209
Dry eye 734.13 37.49 256 23507 3700 2330622
Fibromyalgia 680.09 37.49 231 23532 3069 2331253
Neck pain 672.77 37.49 288 23475 7409 2326913
Hepatic enzyme increased 649.25 37.49 302 23461 9500 2324822
Myalgia 645.42 37.49 402 23361 22931 2311391
C-reactive protein abnormal 631.97 37.49 159 23604 640 2333682
Insomnia 630.57 37.49 411 23352 25376 2308946
Muscle spasms 625.49 37.49 383 23380 21183 2313139
Tuberculin test positive 625.48 37.49 149 23614 449 2333873
Dyspepsia 601.80 37.49 287 23476 9557 2324765
Osteoporosis 581.87 37.49 222 23541 4192 2330130
Blood pressure increased 576.68 37.49 334 23429 16652 2317670
Nasal congestion 573.77 37.49 250 23513 6716 2327606
Dizziness 567.02 37.49 540 23223 58125 2276197
Hypoaesthesia 513.05 37.49 330 23433 19885 2314437
Osteoarthritis 510.01 37.49 230 23533 6716 2327606
Hand deformity 509.79 37.49 143 23620 943 2333379
Abdominal pain 500.49 37.49 400 23363 33974 2300348
Grip strength decreased 499.89 37.49 140 23623 917 2333405
Dyspnoea 489.80 37.49 573 23190 78160 2256162
Contusion 486.08 37.49 271 23492 12539 2321783
Red blood cell sedimentation rate abnormal 473.46 37.49 116 23647 407 2333915
Joint effusion 465.10 37.49 138 23625 1138 2333184
Constipation 461.63 37.49 317 23446 21312 2313010
Liver function test increased 459.66 37.49 170 23593 2931 2331391
Red blood cell sedimentation rate increased 453.59 37.49 153 23610 1984 2332338
Therapeutic response unexpected 440.92 37.49 175 23588 3684 2330638
Pyrexia 436.16 37.49 450 23313 53258 2281064
Asthenia 435.88 37.49 423 23340 46503 2287819
Nodule 435.78 37.49 150 23613 2076 2332246
Hypersensitivity 429.95 37.49 314 23449 23279 2311043
Sensitivity to weather change 424.65 37.49 104 23659 364 2333958
Gastrointestinal disorder 423.30 37.49 219 23544 8698 2325624
Pre-existing condition improved 419.95 37.49 106 23657 433 2333889
Sleep disorder 414.17 37.49 195 23568 6294 2328028
Foot deformity 412.67 37.49 140 23623 1849 2332473
Paraesthesia 407.04 37.49 296 23467 21792 2312530
Depression 406.30 37.49 326 23437 27806 2306516
Gastric disorder 405.65 37.49 163 23600 3547 2330775
Therapy cessation 403.64 37.49 179 23584 5014 2329308
Hypertension 399.25 37.49 319 23444 27042 2307280
Product use in unapproved indication 395.21 37.49 226 23537 10974 2323348
Vomiting 389.14 37.49 487 23276 71115 2263207
Joint noise 385.38 37.49 102 23661 522 2333800
Feeling abnormal 385.31 37.49 294 23469 23287 2311035
Intentional product misuse 379.75 37.49 208 23555 9281 2325041
Bone erosion 366.22 37.49 96 23667 470 2333852
Acne 366.20 37.49 145 23618 3031 2331291
Cystitis 358.34 37.49 169 23594 5473 2328849
Diverticulitis 347.74 37.49 151 23612 4014 2330308
Mobility decreased 338.44 37.49 188 23575 8622 2325700
C-reactive protein increased 332.86 37.49 166 23597 6089 2328233
Stress 325.19 37.49 169 23594 6769 2327553
Pruritus 322.67 37.49 347 23416 42993 2291329
Inflammation 310.41 37.49 158 23605 6055 2328267
Crepitations 300.29 37.49 85 23678 581 2333741
Anxiety 297.49 37.49 278 23485 29081 2305241
Femur fracture 292.65 37.49 156 23607 6583 2327739
Immune system disorder 286.49 37.49 98 23665 1328 2332994
Localised infection 285.74 37.49 118 23645 2758 2331564
Abdominal distension 281.30 37.49 177 23586 10234 2324088
Viral infection 278.39 37.49 134 23629 4542 2329780
Bursitis 276.82 37.49 103 23660 1805 2332517
Off label use 273.48 37.49 417 23346 73181 2261141
Memory impairment 272.09 37.49 188 23575 12735 2321587
Drug effective for unapproved indication 270.53 37.49 64 23699 185 2334137
Cataract 265.67 37.49 140 23623 5768 2328554
Mycobacterium tuberculosis complex test positive 265.12 37.49 70 23693 354 2333968
Fungal infection 263.79 37.49 131 23632 4758 2329564
Sinus disorder 263.09 37.49 109 23654 2569 2331753
Lower respiratory tract infection 259.54 37.49 134 23629 5290 2329032
Nail disorder 255.55 37.49 85 23678 1051 2333271
Gastrooesophageal reflux disease 254.18 37.49 158 23605 8937 2325385
Mouth ulceration 253.96 37.49 119 23644 3793 2330529
Ear infection 252.59 37.49 114 23649 3327 2330995
Rheumatoid nodule 247.85 37.49 72 23691 546 2333776
Joint injury 246.05 37.49 101 23662 2323 2331999
Weight decreased 242.92 37.49 245 23518 28126 2306196
Carpal tunnel syndrome 242.33 37.49 95 23668 1930 2332392
Onychomycosis 240.49 37.49 69 23694 498 2333824
Interstitial lung disease 236.92 37.49 143 23620 7669 2326653
Joint laxity 230.51 37.49 44 23719 18 2334304
Erythema 229.66 37.49 225 23538 24934 2309388
Muscular weakness 228.39 37.49 179 23584 14718 2319604
Disease recurrence 224.08 37.49 105 23658 3346 2330976
Lung disorder 223.40 37.49 127 23636 6085 2328237
Oral herpes 220.95 37.49 91 23672 2111 2332211
Soft tissue disorder 219.13 37.49 54 23709 195 2334127
Adverse drug reaction 216.66 37.49 138 23625 8145 2326177
Rheumatoid factor positive 215.78 37.49 62 23701 450 2333872
Pollakiuria 215.61 37.49 105 23658 3651 2330671
Stomatitis 215.57 37.49 146 23617 9564 2324758
Migraine 214.89 37.49 151 23612 10502 2323820
Anti-cyclic citrullinated peptide antibody positive 214.41 37.49 51 23712 152 2334170
Kidney infection 213.93 37.49 93 23670 2476 2331846
Chest pain 213.89 37.49 228 23535 27909 2306413
Chills 213.15 37.49 175 23588 15377 2318945
Limb discomfort 210.75 37.49 100 23663 3279 2331043
Intentional product use issue 210.69 37.49 102 23661 3500 2330822
Musculoskeletal discomfort 209.93 37.49 87 23676 2051 2332271
Liver function test abnormal 208.97 37.49 130 23633 7360 2326962
Influenza like illness 208.59 37.49 156 23607 11958 2322364
Synovial cyst 207.33 37.49 68 23695 802 2333520
Impaired healing 200.99 37.49 113 23650 5298 2329024
Non-Hodgkin's lymphoma 199.99 37.49 67 23696 848 2333474
Cellulitis 198.67 37.49 136 23627 9065 2325257
Anaemia 198.53 37.49 243 23520 34549 2299773
Bone disorder 197.93 37.49 95 23668 3197 2331125
Coeliac disease 194.13 37.49 64 23699 768 2333554
Impaired work ability 189.09 37.49 77 23686 1733 2332589
Night sweats 186.46 37.49 93 23670 3407 2330915
Tooth infection 186.21 37.49 78 23685 1890 2332432
Hot flush 183.45 37.49 118 23645 7081 2327241
Sjogren's syndrome 181.29 37.49 64 23699 957 2333365
Productive cough 181.20 37.49 105 23658 5216 2329106
Tuberculosis 180.77 37.49 76 23687 1859 2332463
Joint dislocation 180.19 37.49 70 23693 1386 2332936
Respiratory tract infection 179.75 37.49 95 23668 3934 2330388
Drug ineffective for unapproved indication 179.55 37.49 86 23677 2880 2331442
Nephrolithiasis 177.25 37.49 98 23665 4445 2329877
Wound 177.09 37.49 83 23680 2645 2331677
Flatulence 174.87 37.49 97 23666 4428 2329894
Synovial fluid analysis 173.01 37.49 31 23732 0 2334322
Ulcer 169.50 37.49 72 23691 1808 2332514
Synovial disorder 167.65 37.49 37 23726 69 2334253
Limb injury 164.89 37.49 77 23686 2433 2331889
Visual impairment 164.65 37.49 134 23629 11621 2322701
Neoplasm malignant 164.19 37.49 97 23666 4996 2329326
Finger deformity 158.00 37.49 55 23708 787 2333535
Eye infection 151.88 37.49 60 23703 1244 2333078
Hyperhidrosis 150.17 37.49 143 23620 15279 2319043
Poor quality sleep 150.17 37.49 67 23696 1900 2332422
Rheumatic fever 149.36 37.49 33 23730 62 2334260
Gastroenteritis viral 148.91 37.49 72 23691 2462 2331860
Tenosynovitis stenosans 148.23 37.49 35 23728 100 2334222
Skin lesion 146.60 37.49 83 23680 3942 2330380
Scleritis 146.52 37.49 41 23722 267 2334055
Therapeutic product effect variable 146.50 37.49 36 23727 128 2334194
Pelvic fracture 145.36 37.49 59 23704 1316 2333006
Gait inability 145.30 37.49 95 23668 5860 2328462
Skin disorder 143.49 37.49 79 23684 3552 2330770
Swelling face 143.11 37.49 113 23650 9380 2324942
Increased tendency to bruise 142.67 37.49 61 23702 1557 2332765
Therapeutic product effect delayed 142.64 37.49 45 23718 464 2333858
Glossodynia 141.32 37.49 64 23699 1881 2332441
Foot fracture 141.18 37.49 72 23691 2766 2331556
Pulmonary fibrosis 140.18 37.49 70 23693 2570 2331752
Surgery 139.22 37.49 90 23673 5445 2328877
Oedema peripheral 135.47 37.49 166 23597 23597 2310725
Discomfort 134.98 37.49 86 23677 5073 2329249
Oral pain 134.49 37.49 74 23689 3323 2330999
Onychomadesis 130.85 37.49 42 23721 460 2333862
Cushingoid 130.67 37.49 44 23719 566 2333756
Haematochezia 128.03 37.49 84 23679 5211 2329111
Blister 127.33 37.49 92 23671 6679 2327643
Systemic lupus erythematosus 127.23 37.49 77 23686 4144 2330178
Decreased appetite 126.15 37.49 177 23586 28714 2305608
Flank pain 125.59 37.49 55 23708 1490 2332832
Tooth abscess 124.97 37.49 60 23703 2019 2332303
Exostosis 124.97 37.49 53 23710 1325 2332997
Dry skin 124.22 37.49 90 23673 6562 2327760
Wheezing 122.93 37.49 88 23675 6296 2328026
Groin pain 122.68 37.49 52 23711 1298 2333024
Back disorder 119.84 37.49 54 23709 1568 2332754
Asthma 117.97 37.49 109 23654 11205 2323117
Leukopenia 117.66 37.49 104 23659 10092 2324230
Palpitations 117.30 37.49 129 23634 16327 2317995
Pneumonia viral 116.79 37.49 38 23725 436 2333886
Dysphonia 114.07 37.49 84 23679 6280 2328042
Burning sensation 113.32 37.49 91 23672 7737 2326585
Conjunctivitis 111.21 37.49 58 23705 2335 2331987
Tinnitus 111.03 37.49 76 23687 5059 2329263
Wrist deformity 109.92 37.49 26 23737 75 2334247
Hair growth abnormal 108.50 37.49 38 23725 554 2333768
Pemphigus 107.29 37.49 39 23724 637 2333685
Ocular hyperaemia 107.06 37.49 68 23695 3988 2330334
Upper limb fracture 106.91 37.49 59 23704 2664 2331658
Intentional dose omission 105.41 37.49 33 23730 331 2333991
Pain in jaw 105.06 37.49 80 23683 6292 2328030
Pulmonary mass 105.01 37.49 52 23711 1874 2332448
Pleuritic pain 104.97 37.49 38 23725 613 2333709
Thrombosis 104.97 37.49 93 23670 9051 2325271
Sepsis 103.48 37.49 128 23635 18360 2315962
Laryngitis 103.31 37.49 47 23716 1396 2332926
Eye disorder 102.93 37.49 61 23702 3158 2331164
Movement disorder 102.12 37.49 58 23705 2770 2331552
Feeling jittery 101.90 37.49 51 23712 1881 2332441
Extremity contracture 100.85 37.49 25 23738 93 2334229
Body height decreased 100.29 37.49 44 23719 1197 2333125
Spinal pain 100.07 37.49 45 23718 1300 2333022
Musculoskeletal disorder 99.87 37.49 55 23708 2473 2331849
Ankle fracture 99.86 37.49 53 23710 2212 2332110
Diabetes mellitus 99.81 37.49 83 23680 7412 2326910
Skin ulcer 99.61 37.49 65 23698 3994 2330328
Nodal osteoarthritis 99.55 37.49 24 23739 77 2334245
Low density lipoprotein increased 99.45 37.49 44 23719 1222 2333100
Antinuclear antibody positive 99.40 37.49 42 23721 1040 2333282
Scar 99.33 37.49 50 23713 1867 2332455
Liver disorder 98.05 37.49 77 23686 6337 2327985
Spinal stenosis 97.79 37.49 45 23718 1373 2332949
Trigger finger 96.11 37.49 33 23730 452 2333870
Knee arthroplasty 94.84 37.49 56 23707 2879 2331443
Staphylococcal infection 94.77 37.49 70 23693 5256 2329066
Renal disorder 93.67 37.49 65 23698 4423 2329899
Urticaria 93.29 37.49 140 23623 24121 2310201
Intervertebral disc degeneration 92.37 37.49 45 23718 1564 2332758
Tendonitis 92.26 37.49 50 23713 2177 2332145
Respiratory tract congestion 92.00 37.49 51 23712 2323 2331999
Epistaxis 91.98 37.49 89 23674 9690 2324632
Depressed mood 91.78 37.49 68 23695 5130 2329192
Therapeutic response decreased 90.29 37.49 77 23686 7118 2327204
Soft tissue swelling 89.99 37.49 21 23742 56 2334266
Sinus congestion 88.59 37.49 47 23716 1960 2332362
Dysstasia 86.99 37.49 53 23710 2886 2331436
Pharyngitis 86.57 37.49 48 23715 2187 2332135
Eye irritation 85.59 37.49 56 23707 3456 2330866
Fungal skin infection 85.47 37.49 31 23732 503 2333819
Dysuria 84.42 37.49 58 23705 3883 2330439
Pustular psoriasis 83.49 37.49 35 23728 849 2333473
Muscle fatigue 83.44 37.49 28 23735 356 2333966
Sciatica 83.31 37.49 46 23717 2079 2332243
Skin discolouration 82.70 37.49 65 23698 5355 2328967
Feeling hot 82.59 37.49 72 23691 6856 2327466
Throat irritation 82.58 37.49 63 23700 4967 2329355
Psoriasis 81.42 37.49 109 23654 16899 2317423
Intervertebral disc protrusion 80.30 37.49 51 23712 2990 2331332
Blood glucose increased 80.13 37.49 92 23671 12198 2322124
Hip arthroplasty 79.79 37.49 43 23720 1851 2332471
Wound infection 79.79 37.49 38 23725 1255 2333067
Road traffic accident 79.76 37.49 58 23705 4250 2330072
Viral upper respiratory tract infection 79.76 37.49 36 23727 1049 2333273
Eye pain 79.73 37.49 61 23702 4830 2329492
Arthritis bacterial 79.32 37.49 33 23730 785 2333537
Multiple fractures 79.30 37.49 31 23732 624 2333698
Neuralgia 78.71 37.49 49 23714 2773 2331549
White blood cell count decreased 78.60 37.49 111 23652 18097 2316225
Prescribed overdose 78.49 37.49 42 23721 1782 2332540
Iron deficiency anaemia 78.36 37.49 44 23719 2055 2332267
Vision blurred 77.98 37.49 99 23664 14569 2319753
Ill-defined disorder 77.80 37.49 52 23711 3326 2330996
Rib fracture 77.49 37.49 47 23716 2538 2331784
Skin cancer 77.27 37.49 41 23722 1710 2332612
Lipids increased 76.54 37.49 24 23739 242 2334080
Toothache 76.51 37.49 47 23716 2597 2331725
Amnesia 75.82 37.49 70 23693 7183 2327139
Rotator cuff syndrome 75.67 37.49 41 23722 1784 2332538
Hepatitis B virus test positive 75.33 37.49 18 23745 55 2334267
Renal impairment 75.17 37.49 81 23682 10011 2324311
Photophobia 74.81 37.49 44 23719 2245 2332077
Injection site reaction 74.40 37.49 98 23665 14954 2319368
Blood creatinine increased 74.04 37.49 82 23681 10451 2323871
Lymphadenopathy 73.58 37.49 62 23701 5636 2328686
Red blood cell count decreased 73.50 37.49 55 23708 4211 2330111
Pericarditis 73.49 37.49 38 23725 1502 2332820
Temperature intolerance 73.04 37.49 33 23730 964 2333358
Blood triglycerides increased 73.00 37.49 43 23720 2200 2332122
Inflammatory marker increased 72.45 37.49 28 23735 546 2333776
Ear pain 72.33 37.49 46 23717 2703 2331619
Seasonal allergy 71.46 37.49 38 23725 1592 2332730
Deafness 70.57 37.49 45 23718 2656 2331666
Hepatic steatosis 70.51 37.49 48 23715 3165 2331157
Heart rate increased 70.50 37.49 82 23681 11023 2323299
Lung neoplasm malignant 70.47 37.49 47 23716 2995 2331327
Hypoacusis 70.06 37.49 49 23714 3376 2330946
Skin infection 69.83 37.49 36 23727 1414 2332908
Middle insomnia 69.20 37.49 36 23727 1441 2332881
Post procedural infection 69.20 37.49 33 23730 1093 2333229
Arthritis infective 69.11 37.49 28 23735 621 2333701
Deformity 69.04 37.49 26 23737 471 2333851
Dysphagia 68.98 37.49 87 23676 12718 2321604
Skin papilloma 68.59 37.49 27 23736 554 2333768
Immunosuppression 67.75 37.49 32 23731 1037 2333285
Balance disorder 66.99 37.49 75 23688 9672 2324650
Hip fracture 66.53 37.49 54 23709 4658 2329664
Lower limb fracture 65.39 37.49 39 23724 2042 2332280
Meniscus injury 63.90 37.49 31 23732 1067 2333255
Tendon rupture 62.65 37.49 34 23729 1484 2332838
Walking aid user 62.21 37.49 27 23736 715 2333607
Atelectasis 62.20 37.49 37 23726 1928 2332394
Colon cancer 61.20 37.49 36 23727 1837 2332485
Herpes virus infection 61.03 37.49 28 23735 848 2333474
Pulmonary embolism 60.62 37.49 98 23665 17985 2316337
Haemoglobin decreased 60.35 37.49 98 23665 18053 2316269
Upper-airway cough syndrome 60.30 37.49 29 23734 979 2333343
Furuncle 60.13 37.49 29 23734 985 2333337
Incorrect dosage administered 60.09 37.49 22 23741 367 2333955
Concussion 59.81 37.49 28 23735 889 2333433
Bone pain 59.74 37.49 68 23695 8928 2325394
Adverse event 59.73 37.49 63 23700 7596 2326726
Spinal fracture 59.23 37.49 41 23722 2778 2331544
Laboratory test abnormal 59.10 37.49 53 23710 5237 2329085
Aphonia 58.97 37.49 31 23732 1268 2333054
Vitamin D decreased 58.89 37.49 29 23734 1032 2333290
Osteomyelitis 58.53 37.49 45 23718 3588 2330734
Death 58.52 37.49 246 23517 81222 2253100
Type 2 diabetes mellitus 58.43 37.49 37 23726 2157 2332165
Chronic obstructive pulmonary disease 58.40 37.49 60 23703 7017 2327305
Cyst 58.40 37.49 33 23730 1560 2332762
Oedema 57.63 37.49 71 23692 10132 2324190
Colitis ulcerative 57.11 37.49 40 23723 2762 2331560
Pharyngitis streptococcal 56.51 37.49 32 23731 1519 2332803
Gastroenteritis 56.20 37.49 41 23722 3019 2331303
Thyroid disorder 56.09 37.49 32 23731 1541 2332781
Energy increased 56.09 37.49 22 23741 447 2333875
Wrist fracture 55.99 37.49 33 23730 1690 2332632
Epicondylitis 55.75 37.49 19 23744 254 2334068
Tooth disorder 55.59 37.49 46 23717 4077 2330245
Ligament sprain 55.51 37.49 31 23732 1432 2332890
Nerve compression 55.19 37.49 27 23736 947 2333375
Photosensitivity reaction 55.02 37.49 37 23726 2390 2331932
Osteopenia 54.98 37.49 34 23729 1901 2332421
Joint warmth 54.82 37.49 19 23744 268 2334054
Respiratory disorder 54.67 37.49 45 23718 3959 2330363
Rosacea 53.64 37.49 22 23741 504 2333818
Breast cancer 53.51 37.49 66 23697 9429 2324893
Menopausal symptoms 53.38 37.49 20 23743 357 2333965
Increased appetite 53.25 37.49 30 23733 1410 2332912
Blood test abnormal 52.95 37.49 29 23734 1289 2333033
Spinal disorder 52.45 37.49 28 23735 1182 2333140
Rheumatoid factor negative 52.37 37.49 11 23752 14 2334308
Gallbladder disorder 52.11 37.49 38 23725 2796 2331526
Limb deformity 52.06 37.49 18 23745 252 2334070
Somnolence 51.63 37.49 106 23657 23379 2310943
Irritable bowel syndrome 51.42 37.49 32 23731 1809 2332513
Paranasal sinus discomfort 51.42 37.49 20 23743 397 2333925
White blood cell count increased 51.29 37.49 56 23707 7022 2327300
Tremor 51.13 37.49 98 23665 20563 2313759
Blood pressure abnormal 51.10 37.49 31 23732 1674 2332648
Bacterial infection 50.69 37.49 34 23729 2187 2332135
Sputum discoloured 50.59 37.49 27 23736 1139 2333183
Immobile 50.53 37.49 22 23741 587 2333735
Cerebrovascular accident 50.27 37.49 96 23667 20090 2314232
Decreased immune responsiveness 50.24 37.49 23 23740 693 2333629
Haemorrhage 50.16 37.49 69 23694 10970 2323352
Rash papular 49.86 37.49 36 23727 2608 2331714
Fluid retention 49.76 37.49 55 23708 6991 2327331
Onychoclasis 49.63 37.49 24 23739 820 2333502
Intervertebral disc disorder 49.45 37.49 22 23741 619 2333703
Joint lock 49.09 37.49 19 23744 372 2333950
Nervousness 48.35 37.49 47 23716 5142 2329180
Cardiac disorder 48.31 37.49 57 23706 7776 2326546
Myocardial infarction 48.06 37.49 91 23672 18922 2315400
Adverse reaction 47.99 37.49 29 23734 1555 2332767
Oral discomfort 47.78 37.49 27 23736 1276 2333046
Bone swelling 47.78 37.49 16 23747 202 2334120
Sleep apnoea syndrome 47.21 37.49 32 23731 2094 2332228
Sinusitis bacterial 47.08 37.49 13 23750 80 2334242
Clostridium difficile infection 47.00 37.49 36 23727 2854 2331468
Therapy non-responder 46.75 37.49 57 23706 8047 2326275
Atrial fibrillation 46.66 37.49 75 23688 13693 2320629
Raynaud's phenomenon 46.52 37.49 24 23739 944 2333378
Rheumatoid factor increased 46.40 37.49 16 23747 222 2334100
Nerve injury 46.24 37.49 25 23738 1083 2333239
Alanine aminotransferase increased 45.60 37.49 75 23688 13957 2320365
Dry throat 45.60 37.49 24 23739 984 2333338
Food poisoning 44.82 37.49 19 23744 474 2333848
Lymphoma 44.80 37.49 30 23733 1924 2332398
Tendon disorder 44.38 37.49 22 23741 794 2333528
Hunger 44.19 37.49 21 23742 690 2333632
Upper respiratory tract congestion 44.11 37.49 18 23745 407 2333915
Sneezing 43.64 37.49 32 23731 2374 2331948
Gingival bleeding 43.43 37.49 30 23733 2025 2332297
Skin atrophy 43.01 37.49 20 23743 625 2333697
Oral mucosal blistering 42.88 37.49 22 23741 855 2333467
Candida infection 42.84 37.49 34 23729 2839 2331483
Bone cyst 42.76 37.49 14 23749 164 2334158
Chondropathy 42.64 37.49 17 23746 361 2333961
Sinus pain 42.60 37.49 14 23749 166 2334156
General physical health deterioration 42.53 37.49 73 23690 14066 2320256
Rotator cuff repair 42.25 37.49 15 23748 228 2334094
Chest discomfort 42.13 37.49 74 23689 14521 2319801
Ear discomfort 42.06 37.49 24 23739 1156 2333166
Injection site hypersensitivity 41.43 37.49 17 23746 390 2333932
Crying 41.30 37.49 40 23723 4356 2329966
Hepatotoxicity 41.12 37.49 36 23727 3445 2330877
Helicobacter infection 41.00 37.49 19 23744 589 2333733
Ophthalmic herpes zoster 40.88 37.49 16 23747 323 2333999
Tenosynovitis 40.74 37.49 18 23745 498 2333824
Muscle strain 40.72 37.49 23 23740 1086 2333236
Glaucoma 40.59 37.49 29 23734 2066 2332256
Enteritis infectious 40.23 37.49 15 23748 264 2334058
Butterfly rash 40.10 37.49 14 23749 202 2334120
Fracture 40.04 37.49 32 23731 2699 2331623
Joint contracture 39.85 37.49 14 23749 206 2334116
Swollen joint count increased 39.62 37.49 8 23755 7 2334315
Skin mass 39.26 37.49 22 23741 1023 2333299
Granulomatous rosacea 39.06 37.49 7 23756 0 2334322
Nail growth abnormal 38.72 37.49 12 23751 116 2334206
High density lipoprotein increased 38.61 37.49 13 23750 167 2334155
Muscle tightness 38.37 37.49 27 23736 1878 2332444
Spinal operation 38.31 37.49 20 23743 806 2333516
Blood urine present 38.28 37.49 27 23736 1885 2332437
Fine motor skill dysfunction 38.23 37.49 15 23748 305 2334017
Red cell distribution width increased 38.06 37.49 18 23745 585 2333737
Breast mass 37.55 37.49 22 23741 1114 2333208
Pain of skin 37.52 37.49 24 23739 1424 2332898

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 2238.50 45.82 924 4585 62877 1678395
Arthralgia 1429.13 45.82 513 4996 22931 1718341
Joint swelling 1292.88 45.82 351 5158 6002 1735270
Musculoskeletal stiffness 1034.14 45.82 290 5219 5586 1735686
Pain 943.01 45.82 394 5115 26263 1715009
Condition aggravated 931.00 45.82 366 5143 20784 1720488
Rheumatoid arthritis 804.31 45.82 226 5283 4359 1736913
Peripheral swelling 685.08 45.82 227 5282 7744 1733528
Therapeutic product effect incomplete 593.83 45.82 186 5323 5262 1736010
Pain in extremity 560.87 45.82 246 5263 18226 1723046
Synovitis 532.88 45.82 114 5395 631 1740641
Fatigue 510.73 45.82 322 5187 50459 1690813
Joint range of motion decreased 413.79 45.82 94 5415 712 1740560
Herpes zoster 411.08 45.82 135 5374 4438 1736834
Headache 364.26 45.82 226 5283 34150 1707122
Loss of personal independence in daily activities 294.92 45.82 90 5419 2309 1738963
Musculoskeletal pain 294.02 45.82 108 5401 4966 1736306
Malaise 247.59 45.82 168 5341 29397 1711875
Pneumonia 242.33 45.82 198 5311 45984 1695288
Back pain 240.45 45.82 134 5375 16479 1724793
Nasopharyngitis 238.47 45.82 113 5396 9897 1731375
Contraindicated product administered 233.48 45.82 67 5442 1377 1739895
Infection 227.39 45.82 117 5392 12243 1729029
Swelling 226.96 45.82 98 5411 6898 1734374
Product use issue 220.30 45.82 102 5407 8469 1732803
Diarrhoea 211.95 45.82 196 5313 53656 1687616
Product dose omission 200.76 45.82 133 5376 22307 1718965
Drug effective for unapproved indication 198.24 45.82 39 5470 129 1741143
Mobility decreased 197.92 45.82 76 5433 3944 1737328
Sinusitis 195.42 45.82 81 5428 5142 1736130
Mass 189.31 45.82 54 5455 1084 1740188
Joint stiffness 186.93 45.82 59 5450 1692 1739580
Cough 184.38 45.82 119 5390 19078 1722194
Dyspnoea 182.78 45.82 178 5331 51881 1689391
Arthropathy 180.72 45.82 65 5444 2802 1738470
Product use in unapproved indication 178.39 45.82 91 5418 9331 1731941
Abdominal discomfort 172.77 45.82 88 5421 8993 1732279
Treatment failure 170.53 45.82 70 5439 4331 1736941
Rash 167.88 45.82 149 5360 38544 1702728
Arthritis 166.96 45.82 67 5442 3908 1737364
Limb discomfort 164.33 45.82 51 5458 1381 1739891
Influenza 159.78 45.82 76 5433 6691 1734581
Osteoarthritis 159.65 45.82 56 5453 2240 1739032
Diverticulitis 155.15 45.82 55 5454 2270 1739002
Tenderness 154.26 45.82 45 5464 980 1740292
Therapeutic product effect decreased 152.58 45.82 72 5437 6225 1735047
Red blood cell sedimentation rate increased 151.41 45.82 45 5464 1048 1740224
Rhinorrhoea 143.93 45.82 60 5449 3857 1737415
Upper respiratory tract infection 141.39 45.82 60 5449 4033 1737239
Joint lock 136.97 45.82 30 5479 187 1741085
Nausea 134.39 45.82 150 5359 51046 1690226
Sensitivity to weather change 134.06 45.82 28 5481 134 1741138
Disability 132.56 45.82 35 5474 519 1740753
Abdominal pain upper 127.66 45.82 77 5432 10924 1730348
Therapeutic response unexpected 127.05 45.82 48 5461 2376 1738896
Drug hypersensitivity 126.21 45.82 86 5423 15049 1726223
Liver function test increased 120.38 45.82 41 5468 1498 1739774
Blood cholesterol increased 120.13 45.82 49 5460 2977 1738295
Drug ineffective for unapproved indication 117.21 45.82 42 5467 1787 1739485
Tuberculin test positive 114.88 45.82 29 5480 356 1740916
C-reactive protein abnormal 114.86 45.82 27 5482 240 1741032
Mycobacterium tuberculosis complex test positive 114.23 45.82 28 5481 302 1740970
Hypoaesthesia 111.92 45.82 68 5441 9767 1731505
Hypertension 111.19 45.82 88 5421 19360 1721912
Weight increased 107.83 45.82 70 5439 11287 1729985
Interstitial lung disease 107.66 45.82 66 5443 9630 1731642
Physical disability 107.06 45.82 23 5486 129 1741143
C-reactive protein increased 105.95 45.82 55 5454 5830 1735442
Nasal congestion 105.40 45.82 45 5464 3066 1738206
Depression 105.22 45.82 80 5429 16589 1724683
Pre-existing condition improved 103.34 45.82 25 5484 254 1741018
Neck pain 98.77 45.82 44 5465 3322 1737950
Skin mass 97.77 45.82 28 5481 569 1740703
Blood pressure increased 96.51 45.82 64 5445 10689 1730583
Drug intolerance 95.96 45.82 52 5457 6010 1735262
Joint noise 95.42 45.82 22 5487 178 1741094
Oropharyngeal pain 95.34 45.82 48 5461 4770 1736502
Joint effusion 93.49 45.82 27 5482 566 1740706
Hepatic enzyme increased 91.67 45.82 52 5457 6569 1734703
Myalgia 89.76 45.82 71 5438 15587 1725685
Gait disturbance 87.02 45.82 64 5445 12606 1728666
Rheumatoid factor positive 86.67 45.82 17 5492 55 1741217
Pulmonary embolism 85.29 45.82 64 5445 12995 1728277
Bronchitis 84.31 45.82 46 5463 5386 1735886
Off label use 84.22 45.82 103 5406 38468 1702804
Gastric disorder 83.47 45.82 33 5476 1845 1739427
Acne 81.16 45.82 32 5477 1776 1739496
Dry mouth 80.40 45.82 40 5469 3873 1737399
Ill-defined disorder 79.93 45.82 32 5477 1849 1739423
Therapy cessation 79.37 45.82 37 5472 3102 1738170
Insomnia 76.94 45.82 66 5443 16210 1725062
Hair growth abnormal 76.75 45.82 19 5490 214 1741058
Muscle spasms 75.98 45.82 57 5452 11564 1729708
Dry eye 74.51 45.82 27 5482 1185 1740087
Abdominal pain 74.05 45.82 73 5436 21417 1719855
Feeling abnormal 73.51 45.82 55 5454 11111 1730161
Chest pain 71.13 45.82 69 5440 19845 1721427
Gastrointestinal disorder 70.35 45.82 39 5470 4709 1736563
Hernia 69.97 45.82 26 5483 1226 1740046
Hip arthroplasty 69.90 45.82 23 5486 753 1740519
Haematochezia 68.96 45.82 39 5470 4893 1736379
Rheumatoid factor increased 67.08 45.82 15 5494 104 1741168
Fall 66.45 45.82 77 5432 27137 1714135
Contusion 66.29 45.82 39 5470 5270 1736002
Knee arthroplasty 65.86 45.82 23 5486 905 1740367
Pyrexia 63.61 45.82 99 5410 46301 1694971
Hand deformity 61.03 45.82 16 5493 230 1741042
Pulmonary thrombosis 60.71 45.82 21 5488 803 1740469
Sleep disorder 59.16 45.82 33 5476 4030 1737242
Grip strength decreased 58.16 45.82 17 5492 372 1740900
Therapy non-responder 55.45 45.82 37 5472 6229 1735043
Dyspepsia 55.44 45.82 34 5475 4951 1736321
Oral herpes 54.94 45.82 19 5490 726 1740546
Impaired work ability 54.55 45.82 21 5488 1092 1740180
Nephrolithiasis 54.27 45.82 31 5478 3961 1737311
Alopecia 53.33 45.82 30 5479 3723 1737549
Paraesthesia 52.67 45.82 44 5465 10407 1730865
Constipation 51.70 45.82 51 5458 14949 1726323
Nodal osteoarthritis 51.67 45.82 9 5500 11 1741261
Nodule 51.59 45.82 19 5490 873 1740399
Intentional product misuse 50.09 45.82 37 5472 7321 1733951
Lung neoplasm malignant 49.52 45.82 27 5482 3152 1738120
Productive cough 49.12 45.82 28 5481 3563 1737709
Gilbert's syndrome 48.49 45.82 11 5498 82 1741190
Prescribed overdose 48.28 45.82 22 5487 1748 1739524
Osteoporosis 47.76 45.82 21 5488 1534 1739738
Night sweats 45.95 45.82 23 5486 2253 1739019

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