febuxostat ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
xanthine oxydase and xanthine dehydrogenase inhibitor 1137 144060-53-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • februxostat
  • febuxostat
  • feburic
  • uloric
  • adenuric
A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.
  • Molecular weight: 316.38
  • Formula: C16H16N2O3S
  • CLOGP: 4.25
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 83.21
  • ALOGS: -4.24
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
80 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 3 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.61 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Feb. 26, 2015 EMA
Feb. 13, 2009 FDA TAKEDA PHARMS USA

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
Enthesopathy 285.49 17.49 102 16391 7091 50581540
Blood parathyroid hormone decreased 252.89 17.49 93 16400 7021 50581610
Tenosynovitis 247.37 17.49 102 16391 10463 50578168
Panniculitis 240.28 17.49 94 16399 8409 50580222
Tongue disorder 239.86 17.49 96 16397 9120 50579511
Red blood cell sedimentation rate 230.15 17.49 73 16420 3513 50585118
Granuloma skin 221.46 17.49 80 16413 5738 50582893
Skin necrosis 217.99 17.49 94 16399 10773 50577858
Rheumatoid nodule 200.56 17.49 93 16400 12642 50575989
Drug eruption 190.62 17.49 110 16383 23496 50565135
Tendonitis 182.32 17.49 95 16398 16610 50572021
Hypercalcaemia 181.10 17.49 106 16387 23246 50565385
Ulcer 160.08 17.49 93 16400 20107 50568524
Renal impairment 158.82 17.49 157 16336 75504 50513127
Basal cell carcinoma 145.10 17.49 92 16401 23264 50565367
Cardiac failure 138.16 17.49 146 16347 75894 50512737
Alanine aminotransferase abnormal 135.48 17.49 51 16442 4105 50584526
C-reactive protein abnormal 135.15 17.49 94 16399 27715 50560916
Aspartate aminotransferase increased 131.58 17.49 144 16349 77854 50510777
Skin ulcer 130.11 17.49 101 16392 35217 50553414
Fear of injection 113.28 17.49 50 16443 6053 50582578
Acute kidney injury 108.31 17.49 233 16260 227825 50360806
Alanine aminotransferase increased 107.40 17.49 138 16355 88221 50500410
Red blood cell sedimentation rate increased 105.90 17.49 83 16410 29333 50559298
Rash pruritic 101.64 17.49 100 16393 47746 50540885
Psoriatic arthropathy 93.82 17.49 95 16398 46937 50541694
Blood creatinine increased 92.61 17.49 119 16374 76041 50512590
Inflammation 92.34 17.49 103 16390 56809 50531822
Loss of personal independence in daily activities 76.73 17.49 104 16389 69946 50518685
Anaemia 73.36 17.49 214 16279 252242 50336389
Hyperkalaemia 71.16 17.49 83 16410 48006 50540625
C-reactive protein increased 70.24 17.49 97 16396 66377 50522254
Drug tolerance decreased 61.69 17.49 38 16455 9122 50579509
Platelet count decreased 59.70 17.49 113 16380 100613 50488018
Drug ineffective 58.46 17.49 112 16381 819221 49769410
Hepatic function abnormal 57.94 17.49 62 16431 32619 50556012
Joint injury 56.71 17.49 51 16442 21738 50566893
Erythema 54.39 17.49 136 16357 146278 50442353
Granuloma 45.58 17.49 25 16468 4833 50583798
Neutrophil count decreased 43.92 17.49 64 16429 45962 50542669
Blood uric acid increased 42.36 17.49 22 16471 3812 50584819
Blood pressure systolic increased 39.34 17.49 53 16440 35396 50553235
Drug tolerance 37 17.49 22 16471 4954 50583677
Gout 36.24 17.49 30 16463 11440 50577191
Therapy non-responder 34.97 17.49 61 16432 50961 50537670
Toxicity to various agents 32.97 17.49 14 16479 212485 50376146
Systemic lupus erythematosus 32.13 17.49 4 16489 140618 50448013
Decreased appetite 30.52 17.49 138 16355 200785 50387846
Synovitis 30.28 17.49 99 16394 123766 50464865
Cardiac failure chronic 29.79 17.49 17 16476 3546 50585085
Fatigue 29.40 17.49 125 16368 707476 49881155
Cardiac failure acute 29.07 17.49 23 16470 8227 50580404
Sinusitis 28.50 17.49 10 16483 170548 50418083
Rash 28.38 17.49 241 16252 437230 50151401
Anxiety 27.07 17.49 12 16481 177594 50411037
Rheumatoid lung 26.82 17.49 14 16479 2451 50586180
Chronic kidney disease 26.54 17.49 47 16446 39724 50548907
Depression 25.49 17.49 11 16482 165412 50423219
Coronavirus test positive 25.15 17.49 9 16484 627 50588004
Systemic infection 24.94 17.49 13 16480 2270 50586361
Tumour lysis syndrome 24.68 17.49 20 16473 7401 50581230
Right ventricular failure 24.44 17.49 28 16465 15865 50572766
Pneumonia aspiration 22.46 17.49 38 16455 30966 50557665
Cerebral infarction 22.01 17.49 31 16462 21573 50567058
Anaemia vitamin B12 deficiency 21.88 17.49 7 16486 346 50588285
Swelling 21.81 17.49 20 16473 200852 50387779
Haemorrhoidal haemorrhage 21.65 17.49 14 16479 3653 50584978
Upper respiratory tract inflammation 21.60 17.49 12 16481 2377 50586254
Infusion related reaction 21.08 17.49 110 16383 169447 50419184
Hyperuricaemia 20.82 17.49 15 16478 4665 50583966
Paraesthesia 20.16 17.49 7 16486 120236 50468395
Renal failure 19.87 17.49 78 16415 106555 50482076
Wound 19.85 17.49 5 16488 105789 50482842
Renal function test abnormal 19.64 17.49 12 16481 2837 50585794
Product dose omission issue 19.15 17.49 19 16474 183819 50404812
Myoglobin blood increased 18.98 17.49 9 16484 1284 50587347
Urinary retention 18.84 17.49 32 16461 26158 50562473
Tubulointerstitial nephritis 18.82 17.49 24 16469 15187 50573444
General physical health deterioration 18.81 17.49 94 16399 142340 50446291
Hyperferritinaemia 18.67 17.49 5 16488 131 50588500
Peripheral swelling 18.11 17.49 122 16371 205814 50382817
Renal disorder 17.70 17.49 32 16461 27473 50561158
Pulmonary arterial hypertension 17.58 17.49 27 16466 20292 50568339

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
Renal impairment 177.89 13.60 279 25145 81054 29468049
Tenosynovitis 164.67 13.60 75 25349 3658 29545445
Enthesopathy 161.34 13.60 74 25350 3669 29545434
Cardiac failure 146.34 13.60 252 25172 79035 29470068
Tongue disorder 126.14 13.60 67 25357 4569 29544534
Hepatic function abnormal 113.81 13.60 154 25270 39105 29509998
C-reactive protein abnormal 112.27 13.60 70 25354 6466 29542637
Interstitial lung disease 99.33 13.60 178 25246 57540 29491563
Alanine aminotransferase abnormal 98.57 13.60 49 25375 2908 29546195
Synovitis 90.51 13.60 75 25349 10815 29538288
Hyperkalaemia 87.85 13.60 175 25249 61217 29487886
Tendonitis 81.54 13.60 62 25362 7899 29541204
Acute kidney injury 78.13 13.60 440 24984 264827 29284276
Cerebral infarction 77.95 13.60 101 25323 24574 29524529
Gout 64.32 13.60 76 25348 16835 29532268
Aspartate aminotransferase increased 58.10 13.60 146 25278 59579 29489524
Psoriatic arthropathy 55.83 13.60 66 25358 14625 29534478
Platelet count decreased 50.77 13.60 201 25223 104471 29444632
Alanine aminotransferase increased 47.96 13.60 152 25272 70792 29478311
Tumour lysis syndrome 45.67 13.60 58 25366 13826 29535277
Pemphigoid 44.68 13.60 43 25381 7538 29541565
Blood uric acid increased 42.34 13.60 37 25387 5731 29543372
Haemorrhage subcutaneous 42.25 13.60 25 25399 2100 29547003
Loss of personal independence in daily activities 41.85 13.60 77 25347 25363 29523740
Contraindicated product administered 41.67 13.60 64 25360 18202 29530901
Cardiac failure acute 41.21 13.60 45 25379 9147 29539956
Cardiac failure chronic 40.62 13.60 38 25386 6429 29542674
General physical health deterioration 40.18 13.60 185 25239 102672 29446431
Neutrophil count decreased 38.74 13.60 103 25321 43464 29505639
Drug eruption 37.27 13.60 58 25366 16683 29532420
Anaemia 35.91 13.60 295 25129 200656 29348447
Hypocalcaemia 35.83 13.60 64 25360 20601 29528502
Lactic acidosis 34.85 13.60 79 25345 30168 29518935
Gouty tophus 34.68 13.60 10 25414 125 29548978
Toxicity to various agents 32.96 13.60 62 25362 173599 29375504
Cerebral haemorrhage 32.84 13.60 79 25345 31347 29517756
Blood creatinine increased 32.43 13.60 152 25272 84950 29464153
Death 32.33 13.60 168 25256 341916 29207187
Rash 31.96 13.60 275 25149 189544 29359559
Erythema 31.77 13.60 139 25285 75467 29473636
Orthostatic intolerance 31.41 13.60 14 25410 648 29548455
Congenital diaphragmatic anomaly 31.18 13.60 7 25417 28 29549075
Concomitant disease aggravated 30.78 13.60 29 25395 4949 29544154
Red blood cell sedimentation rate 30.47 13.60 13 25411 541 29548562
Granuloma skin 28.51 13.60 13 25411 635 29548468
Renal failure 27.92 13.60 186 25238 118413 29430690
Corneal abscess 27.81 13.60 6 25418 19 29549084
Hyperkinetic heart syndrome 27.05 13.60 8 25416 110 29548993
Panniculitis 25.95 13.60 15 25409 1206 29547897
Blood parathyroid hormone decreased 25.54 13.60 13 25411 811 29548292
Blood lactic acid 25.45 13.60 10 25414 336 29548767
Hepatic enzyme increased 25.22 13.60 75 25349 33724 29515379
Hyperuricaemia 24.61 13.60 30 25394 6859 29542244
Transformation to acute myeloid leukaemia 24.60 13.60 12 25412 683 29548420
Fatigue 24.39 13.60 166 25258 316655 29232448
Renal ischaemia 24.34 13.60 11 25413 526 29548577
Asthenia 24.27 13.60 99 25325 215151 29333952
Shock haemorrhagic 23.97 13.60 35 25389 9516 29539587
Pneumonia bacterial 23.11 13.60 34 25390 9309 29539794
Liver disorder 23.05 13.60 64 25360 27685 29521418
Treatment failure 23.00 13.60 77 25347 36862 29512241
Intentional overdose 22.93 13.60 3 25421 38525 29510578
Arrhythmia 22.90 13.60 69 25355 31244 29517859
Cytomegalovirus nephritis 22.46 13.60 7 25417 116 29548987
Gastric cancer 22.42 13.60 24 25400 4770 29544333
Rubber sensitivity 21.92 13.60 7 25417 126 29548977
Procedural failure 21.43 13.60 6 25418 67 29549036
Pulmonary alveolar haemorrhage 19.95 13.60 26 25398 6354 29542749
C-reactive protein increased 19.82 13.60 83 25341 44180 29504923
Fulminant type 1 diabetes mellitus 19.54 13.60 10 25414 631 29548472
Depression 19.31 13.60 27 25397 85120 29463983
Chronic kidney disease 19.31 13.60 72 25352 36344 29512759
Conjunctival ulcer 18.83 13.60 5 25419 45 29549058
Anxiety 18.45 13.60 28 25396 85337 29463766
Off label use 18.30 13.60 168 25256 300632 29248471
Multiple drug therapy 18.18 13.60 8 25416 359 29548744
Suicidal ideation 17.82 13.60 4 25420 34712 29514391
Hypercalcaemia 17.77 13.60 36 25388 12723 29536380
Hyperhidrosis 17.25 13.60 18 25406 64522 29484581
Nephrogenic anaemia 17.18 13.60 14 25410 1971 29547132
Pseudohyponatraemia 16.89 13.60 5 25419 69 29549034
Dyspnoea paroxysmal nocturnal 16.85 13.60 12 25412 1382 29547721
Altered state of consciousness 16.64 13.60 46 25378 19843 29529260
Hypothyroidism 16.62 13.60 40 25384 15866 29533237
Thirst 16.60 13.60 24 25400 6467 29542636
Aggression 16.52 13.60 5 25419 35536 29513567
Cerebral ventricular rupture 16.44 13.60 6 25418 164 29548939
Blood uric acid decreased 16.17 13.60 7 25417 302 29548801
Seizure 16.14 13.60 35 25389 93088 29456015
Thalamus haemorrhage 16.05 13.60 10 25414 922 29548181
Thrombotic cerebral infarction 15.85 13.60 7 25417 317 29548786
Low cardiac output syndrome 15.81 13.60 8 25416 493 29548610
Respiratory tract haemorrhage 15.74 13.60 10 25414 954 29548149
Product prescribing error 15.46 13.60 42 25382 17934 29531169
Drug hypersensitivity 15.31 13.60 106 25318 68300 29480803
Blood urea increased 15.25 13.60 56 25368 28056 29521047
Drug ineffective 15.02 13.60 221 25203 362949 29186154
Hypovolaemic shock 14.87 13.60 22 25402 6050 29543053
Erythema multiforme 14.81 13.60 25 25399 7692 29541411
Decreased appetite 14.67 13.60 190 25234 145152 29403951
Puncture site infection 14.51 13.60 4 25420 42 29549061
Brain natriuretic peptide increased 14.43 13.60 18 25406 4212 29544891
Mental status changes 14.38 13.60 6 25418 34921 29514182
Rheumatoid nodule 14.36 13.60 13 25411 2109 29546994
Nephrotic syndrome 14.19 13.60 22 25402 6306 29542797
Cardiac arrest 14.15 13.60 33 25391 85558 29463545
Echocardiogram abnormal 14.13 13.60 9 25415 862 29548241
Cerebrovascular accident 14.09 13.60 28 25396 76883 29472220
Respiratory distress 14.07 13.60 5 25419 32101 29517002
Agitation 14.06 13.60 14 25410 51290 29497813
Drug titration error 13.85 13.60 7 25417 430 29548673
Suicide attempt 13.81 13.60 6 25418 34104 29514999
Stevens-Johnson syndrome 13.65 13.60 38 25386 16459 29532644
Colon cancer 13.64 13.60 24 25400 7631 29541472

FDA Adverse Event Reporting System (Geriatric)

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
Enthesopathy 370.86 13.08 159 39345 9479 64449749
Tenosynovitis 342.67 13.08 160 39344 11673 64447555
Renal impairment 328.86 13.08 409 39095 134608 64324620
Tongue disorder 300.05 13.08 147 39357 11933 64447295
Cardiac failure 273.84 13.08 370 39134 132003 64327225
Tendonitis 223.95 13.08 145 39359 20137 64439091
Alanine aminotransferase abnormal 220.90 13.08 100 39404 6788 64452440
Blood parathyroid hormone decreased 199.10 13.08 95 39409 7271 64451957
Red blood cell sedimentation rate 193.02 13.08 76 39428 3638 64455590
Panniculitis 190.92 13.08 98 39406 8781 64450447
Acute kidney injury 188.34 13.08 653 38851 448587 64010641
Hepatic function abnormal 187.96 13.08 214 39290 64099 64395129
C-reactive protein abnormal 183.55 13.08 148 39356 28899 64430329
Granuloma skin 175.42 13.08 82 39422 5992 64453236
Hyperkalaemia 168.27 13.08 255 39249 100874 64358354
Drug eruption 167.10 13.08 154 39350 35982 64423246
Aspartate aminotransferase increased 156.96 13.08 271 39233 119517 64339711
Rheumatoid nodule 150.95 13.08 95 39409 12556 64446672
Skin necrosis 147.34 13.08 98 39406 14231 64444997
Hypercalcaemia 135.85 13.08 129 39375 31287 64427941
Psoriatic arthropathy 131.50 13.08 147 39357 43134 64416094
Alanine aminotransferase increased 126.00 13.08 269 39235 138762 64320466
Platelet count decreased 125.83 13.08 301 39203 167410 64291818
Interstitial lung disease 123.94 13.08 218 39286 97514 64361714
Ulcer 110.21 13.08 100 39404 22890 64436338
Cerebral infarction 107.24 13.08 129 39375 40915 64418313
Anaemia 103.31 13.08 482 39022 378198 64081030
Blood creatinine increased 103.21 13.08 245 39259 135537 64323691
Loss of personal independence in daily activities 91.03 13.08 161 39343 72293 64386935
Fear of injection 87.55 13.08 51 39453 5861 64453367
Neutrophil count decreased 86.19 13.08 163 39341 77033 64382195
Basal cell carcinoma 82.32 13.08 98 39406 30740 64428488
Tumour lysis syndrome 80.57 13.08 78 39426 19362 64439866
Skin ulcer 77.51 13.08 114 39390 43860 64415368
Toxicity to various agents 75.49 13.08 67 39437 363446 64095782
Cardiac failure acute 72.33 13.08 68 39436 16276 64442952
Gout 70.70 13.08 76 39428 21337 64437891
Drug ineffective 70.59 13.08 271 39233 839976 63619252
C-reactive protein increased 66.46 13.08 166 39338 94743 64364485
Cardiac failure chronic 65.59 13.08 50 39454 8991 64450237
Erythema 60.65 13.08 251 39253 186819 64272409
Rash pruritic 60.12 13.08 118 39386 57286 64401942
Drug abuse 59.53 13.08 6 39498 132368 64326860
Pemphigoid 59.34 13.08 55 39449 12931 64446297
General physical health deterioration 59.14 13.08 265 39239 204160 64255068
Synovitis 53.03 13.08 157 39347 98933 64360295
Fatigue 52.70 13.08 258 39246 748472 63710756
Haemorrhage subcutaneous 52.65 13.08 33 39471 4328 64454900
Inflammation 50.83 13.08 119 39385 65181 64394047
Renal failure 50.65 13.08 233 39271 181455 64277773
Hypocalcaemia 48.87 13.08 90 39414 41663 64417565
Cerebral haemorrhage 48.70 13.08 101 39403 50989 64408239
Sinusitis 47.68 13.08 15 39489 145913 64313315
Decreased appetite 46.42 13.08 313 39191 280976 64178252
Hyperuricaemia 46.25 13.08 43 39461 10148 64449080
Blood uric acid increased 46.13 13.08 39 39465 8124 64451104
Red blood cell sedimentation rate increased 45.27 13.08 74 39430 31161 64428067
Anxiety 44.91 13.08 35 39469 202614 64256614
Depression 44.10 13.08 29 39475 183262 64275966
Intentional overdose 43.39 13.08 3 39501 89941 64369287
Concomitant disease aggravated 41.72 13.08 43 39461 11499 64447729
Chronic kidney disease 41.26 13.08 102 39402 57817 64401411
Transformation to acute myeloid leukaemia 39.13 13.08 16 39488 845 64458383
Lactic acidosis 38.43 13.08 103 39401 61307 64397921
Joint injury 36.88 13.08 57 39447 22890 64436338
Liver disorder 35.95 13.08 92 39412 53259 64405969
Blood urea increased 33.85 13.08 80 39424 44073 64415155
Pain 32.66 13.08 202 39302 553309 63905919
Orthostatic intolerance 32.49 13.08 17 39487 1583 64457645
Altered state of consciousness 31.62 13.08 71 39433 37831 64421397
Asthenia 30.87 13.08 146 39358 427898 64031330
Melaena 30.71 13.08 87 39417 53461 64405767
Nephrogenic anaemia 30.04 13.08 21 39483 3304 64455924
Hyperhidrosis 29.72 13.08 20 39484 124900 64334328
Systemic infection 29.38 13.08 23 39481 4298 64454930
Swelling 29.22 13.08 33 39471 160185 64299043
Hyperkinetic heart syndrome 29.08 13.08 8 39496 120 64459108
Glossodynia 28.90 13.08 3 39501 64693 64394535
Drug tolerance decreased 28.84 13.08 28 39476 6970 64452258
Lower respiratory tract infection 28.70 13.08 11 39493 94603 64364625
Gastric cancer 28.70 13.08 27 39477 6466 64452762
Disseminated intravascular coagulation 28.57 13.08 62 39442 32286 64426942
Granuloma 28.18 13.08 27 39477 6614 64452614
Contraindicated product administered 27.62 13.08 135 39369 107694 64351534
Discomfort 26.97 13.08 8 39496 80870 64378358
Arrhythmia 26.53 13.08 82 39422 52862 64406366
Pneumonia bacterial 26.51 13.08 39 39465 14996 64444232
Haematochezia 26.33 13.08 95 39409 66278 64392950
Injection site pain 26.28 13.08 18 39486 111390 64347838
Gastrointestinal disorder 26.28 13.08 11 39493 89698 64369530
Rash 26.18 13.08 410 39094 458139 64001089
Blood lactic acid 25.91 13.08 10 39494 453 64458775
Therapy non-responder 25.87 13.08 94 39410 65805 64393423
Atrial fibrillation 25.60 13.08 186 39318 170903 64288325
Migraine 25.36 13.08 4 39500 62673 64396555
Systemic lupus erythematosus 25.30 13.08 8 39496 77604 64381624
Suicidal ideation 25.28 13.08 5 39499 66537 64392691
Aplasia pure red cell 25.11 13.08 26 39478 6988 64452240
Rhabdomyolysis 25.06 13.08 117 39387 91609 64367619
Cardiac failure congestive 25.01 13.08 151 39353 130429 64328799
Right ventricular failure 24.77 13.08 46 39458 21425 64437803
Pulmonary alveolar haemorrhage 24.43 13.08 30 39474 9708 64449520
Corneal abscess 24.32 13.08 6 39498 57 64459171
Paraesthesia 24.21 13.08 28 39476 134494 64324734
Renal disorder 23.84 13.08 61 39443 35304 64423924
Renal ischaemia 23.41 13.08 12 39492 1071 64458157
Upper respiratory tract inflammation 23.30 13.08 19 39485 3763 64455465
Shock haemorrhagic 23.28 13.08 39 39465 16752 64442476
Cytomegalovirus nephritis 23.24 13.08 7 39497 147 64459081
Pneumonia aspiration 22.80 13.08 84 39420 59187 64400041
Drug tolerance 22.59 13.08 23 39481 6062 64453166
Product dose omission issue 22.54 13.08 54 39450 194693 64264535
Oedema peripheral 22.52 13.08 212 39292 210105 64249123
Procedural failure 22.47 13.08 6 39498 80 64459148
Enterocolitis 22.40 13.08 32 39472 11986 64447242
Stress 22.07 13.08 5 39499 60529 64398699
Seizure 22.03 13.08 43 39461 166849 64292379
Suicide attempt 21.96 13.08 8 39496 70999 64388229
Cardiac arrest 21.84 13.08 38 39466 154026 64305202
Plasma cell myeloma 21.84 13.08 70 39434 46005 64413223
Blood pressure fluctuation 21.70 13.08 3 39501 51868 64407360
Nephrotic syndrome 21.66 13.08 28 39476 9539 64449689
Thalamus haemorrhage 21.45 13.08 13 39491 1606 64457622
Blood lactate dehydrogenase increased 21.21 13.08 56 39448 33022 64426206
Thirst 21.17 13.08 34 39470 14103 64445125
Colon cancer 20.97 13.08 32 39472 12707 64446521
Rheumatoid lung 20.88 13.08 15 39489 2464 64456764
Influenza like illness 20.76 13.08 6 39498 61696 64397532
Fulminant type 1 diabetes mellitus 20.59 13.08 11 39493 1069 64458159
Gait disturbance 20.51 13.08 47 39457 172108 64287120
Hypercreatininaemia 20.47 13.08 10 39494 805 64458423
Alopecia 19.93 13.08 45 39459 165645 64293583
Erythema multiforme 19.84 13.08 35 39469 15666 64443562
Cerebral ventricular rupture 19.76 13.08 8 39496 412 64458816
Injury 19.68 13.08 5 39499 55987 64403241
Folate deficiency 19.42 13.08 15 39489 2748 64456480
Blood creatine phosphokinase increased 19.27 13.08 79 39425 58479 64400749
Drug titration error 19.12 13.08 10 39494 930 64458298
Conjunctival ulcer 18.91 13.08 5 39499 64 64459164
Agitation 18.64 13.08 16 39488 88351 64370877
Tachycardia 18.50 13.08 40 39464 149539 64309689
Confusional state 18.26 13.08 90 39414 261054 64198174
Off label use 18.03 13.08 276 39228 632530 63826698
Blood pressure decreased 18.00 13.08 102 39402 86097 64373131
Gouty tophus 17.77 13.08 7 39497 335 64458893
Diabetic nephropathy 17.77 13.08 14 39490 2640 64456588
Troponin increased 17.77 13.08 33 39471 15366 64443862
Low cardiac output syndrome 17.74 13.08 9 39495 786 64458442
Heart rate increased 17.26 13.08 21 39483 98654 64360574
Hypovolaemic shock 17.20 13.08 26 39478 10240 64448988
Sudden death 17.15 13.08 38 39466 20058 64439170
Mental status changes 17.12 13.08 8 39496 61154 64398074
Azotaemia 17.05 13.08 22 39482 7480 64451748
Brain natriuretic peptide increased 16.75 13.08 22 39482 7611 64451617
Injection site reaction 16.72 13.08 4 39500 46660 64412568
Glomerular filtration rate decreased 16.70 13.08 37 39467 19535 64439693
Dyspnoea paroxysmal nocturnal 16.59 13.08 12 39492 1992 64457236
Renal function test abnormal 16.57 13.08 16 39488 3958 64455270
Tubulointerstitial nephritis 16.54 13.08 49 39455 30860 64428368
Vomiting 16.51 13.08 238 39266 550879 63908349
Eosinophilia 16.39 13.08 56 39448 38020 64421208
White blood cell count decreased 16.34 13.08 158 39346 157679 64301549
Obstructive pancreatitis 16.25 13.08 8 39496 655 64458573
Coronavirus test positive 16.22 13.08 9 39495 942 64458286
Stevens-Johnson syndrome 16.20 13.08 52 39452 34197 64425031
Product prescribing error 16.18 13.08 53 39451 35216 64424012
Enteritis infectious 16.16 13.08 14 39490 3014 64456214
Pain in extremity 16.12 13.08 114 39390 302971 64156257
Death 16.06 13.08 204 39300 482501 63976727
Cerebrovascular accident 16.03 13.08 38 39466 137545 64321683
Dehydration 16.03 13.08 203 39301 216560 64242668
Injection site erythema 15.96 13.08 12 39492 70788 64388440
Embolic stroke 15.76 13.08 20 39484 6691 64452537
Henoch-Schonlein purpura 15.56 13.08 12 39492 2194 64457034
Pseudohyponatraemia 15.52 13.08 5 39499 132 64459096
Subdural haematoma 15.52 13.08 45 39459 28009 64431219
Thrombotic cerebral infarction 15.46 13.08 7 39497 475 64458753
Impaired healing 15.32 13.08 9 39495 60464 64398764
Treatment failure 15.23 13.08 123 39381 116693 64342535
Urinary retention 15.12 13.08 65 39439 49136 64410092
Hypoaesthesia 14.98 13.08 40 39464 139068 64320160
Sleep disorder 14.96 13.08 9 39495 59700 64399528
Intentional product use issue 14.94 13.08 22 39482 95342 64363886
Puncture site infection 14.93 13.08 4 39500 54 64459174
Respiratory tract haemorrhage 14.89 13.08 10 39494 1474 64457754
Pericarditis 14.87 13.08 10 39494 62506 64396722
Subarachnoid haemorrhage 14.77 13.08 34 39470 18404 64440824
Aortic dissection 14.58 13.08 14 39490 3438 64455790
Dysphagia 14.54 13.08 27 39477 106785 64352443
Shock symptom 14.52 13.08 5 39499 163 64459065
Bacterial prostatitis 14.36 13.08 4 39500 63 64459165
Pulmonary arterial hypertension 14.33 13.08 41 39463 25326 64433902
Anaemia vitamin B12 deficiency 14.14 13.08 7 39497 580 64458648
Shunt occlusion 14.10 13.08 9 39495 1218 64458010
Nasal mucosal erosion 13.97 13.08 4 39500 70 64459158
Drug-induced liver injury 13.92 13.08 62 39442 47581 64411647
Labelled drug-drug interaction medication error 13.79 13.08 37 39467 22025 64437203
Haemoptysis 13.71 13.08 63 39441 48985 64410243
Wound 13.67 13.08 16 39488 76461 64382767
Mesenteric vein thrombosis 13.61 13.08 9 39495 1293 64457935
Keratoconus 13.61 13.08 4 39500 77 64459151
Haemorrhagic cerebral infarction 13.54 13.08 9 39495 1305 64457923
Prerenal failure 13.48 13.08 13 39491 3209 64456019
Umbilical hernia 13.43 13.08 15 39489 4390 64454838
Cytomegalovirus enterocolitis 13.28 13.08 9 39495 1346 64457882
Feeling abnormal 13.22 13.08 40 39464 133562 64325666

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M04AA03 MUSCULO-SKELETAL SYSTEM
ANTIGOUT PREPARATIONS
ANTIGOUT PREPARATIONS
Preparations inhibiting uric acid production
FDA MoA N0000000206 Xanthine Oxidase Inhibitors
MeSH PA D018501 Antirheumatic Agents
MeSH PA D006074 Gout Suppressants
FDA EPC N0000175698 Xanthine Oxidase Inhibitor
CHEBI has role CHEBI:35634 xanthine oxidase inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hyperuricemia indication 35885006 DOID:1920
Gout Prevention indication
Myocardial infarction contraindication 22298006 DOID:5844
Liver function tests abnormal contraindication 166603001
Cerebrovascular accident contraindication 230690007
Thromboembolic disorder contraindication 371039008




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.3 acidic
pKa2 0.46 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
40MG ULORIC TAKEDA PHARMS USA N021856 Feb. 13, 2009 RX TABLET ORAL 8372872 Sept. 8, 2031 USE OF FEBUXOSTAT FOR THE MANAGEMENT OF HYPERURICEMIA IN PATIENTS SUFFERING FROM GOUT AND, WHEN USED WITH THEOPHYLLINE WITHOUT THE NEED FOR DOSE ADJUSTMENT OF THEOPHYLLINE
40MG ULORIC TAKEDA PHARMS USA N021856 Feb. 13, 2009 RX TABLET ORAL 9107912 Sept. 8, 2031 USE OF FEBUXOSTAT FOR THE MANAGEMENT OF HYPERURICEMIA IN PATIENTS SUFFERING FROM GOUT AND, WHEN USED WITH THEOPHYLLINE WITHOUT THE NEED FOR DOSE ADJUSTMENT OF THEOPHYLLINE
80MG ULORIC TAKEDA PHARMS USA N021856 Feb. 13, 2009 RX TABLET ORAL 8372872 Sept. 8, 2031 USE OF FEBUXOSTAT FOR THE MANAGEMENT OF HYPERURICEMIA IN PATIENTS SUFFERING FROM GOUT AND, WHEN USED WITH THEOPHYLLINE WITHOUT THE NEED FOR DOSE ADJUSTMENT OF THEOPHYLLINE
80MG ULORIC TAKEDA PHARMS USA N021856 Feb. 13, 2009 RX TABLET ORAL 9107912 Sept. 8, 2031 USE OF FEBUXOSTAT FOR THE MANAGEMENT OF HYPERURICEMIA IN PATIENTS SUFFERING FROM GOUT AND, WHEN USED WITH THEOPHYLLINE WITHOUT THE NEED FOR DOSE ADJUSTMENT OF THEOPHYLLINE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Xanthine dehydrogenase/oxidase Enzyme INHIBITOR Ki 9.22 WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel EC50 7.44 WOMBAT-PK
Xanthine dehydrogenase/oxidase Enzyme IC50 8.52 CHEMBL
Xanthine dehydrogenase/oxidase Enzyme IC50 8.40 CHEMBL

External reference:

IDSource
4025245 VUID
N0000179385 NUI
D01206 KEGG_DRUG
4025245 VANDF
C0249529 UMLSCUI
CHEBI:31596 CHEBI
TEI PDB_CHEM_ID
CHEMBL1164729 ChEMBL_ID
DB04854 DRUGBANK_ID
D000069465 MESH_DESCRIPTOR_UI
134018 PUBCHEM_CID
6817 IUPHAR_LIGAND_ID
8140 INN_ID
101V0R1N2E UNII
73689 RXNORM
161190 MMSL
232999 MMSL
26212 MMSL
d07397 MMSL
012966 NDDF
441610003 SNOMEDCT_US
441743008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0054-0413 TABLET 40 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0054-0414 TABLET 80 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0378-3925 TABLET, FILM COATED 40 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0378-3926 TABLET, FILM COATED 80 mg ORAL ANDA 29 sections
FEBUXOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 0527-2244 TABLET 40 mg ORAL ANDA 32 sections
FEBUXOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 0527-2248 TABLET 80 mg ORAL ANDA 32 sections
Febuxostat Human Prescription Drug Label 1 14445-156 TABLET, FILM COATED 40 mg ORAL ANDA 27 sections
Febuxostat Human Prescription Drug Label 1 14445-157 TABLET, FILM COATED 80 mg ORAL ANDA 27 sections
Febuxostat Human Prescription Drug Label 1 16714-059 TABLET, FILM COATED 40 mg ORAL ANDA 31 sections
Febuxostat Human Prescription Drug Label 1 16714-060 TABLET, FILM COATED 80 mg ORAL ANDA 31 sections
ULORIC HUMAN PRESCRIPTION DRUG LABEL 1 21695-516 TABLET 80 mg ORAL NDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 27808-206 TABLET 40 mg ORAL ANDA 32 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 27808-207 TABLET 80 mg ORAL ANDA 32 sections
ULORIC HUMAN PRESCRIPTION DRUG LABEL 1 43353-305 TABLET 40 mg ORAL NDA 29 sections
Febuxostat Human Prescription Drug Label 1 46708-190 TABLET, COATED 40 mg ORAL ANDA 29 sections
Febuxostat Human Prescription Drug Label 1 46708-191 TABLET, COATED 80 mg ORAL ANDA 29 sections
Febuxostat Human Prescription Drug Label 1 47335-721 TABLET, FILM COATED 40 mg ORAL ANDA 31 sections
Febuxostat Human Prescription Drug Label 1 47335-722 TABLET, FILM COATED 80 mg ORAL ANDA 31 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 51407-293 TABLET 40 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 51407-294 TABLET 80 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 55111-796 TABLET 40 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 55111-797 TABLET 80 mg ORAL ANDA 29 sections
ULORIC HUMAN PRESCRIPTION DRUG LABEL 1 55154-5158 TABLET 40 mg ORAL NDA 32 sections
ULORIC HUMAN PRESCRIPTION DRUG LABEL 1 55154-5159 TABLET 80 mg ORAL NDA 32 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 60687-538 TABLET, FILM COATED 40 mg ORAL ANDA 31 sections
Febuxostat Human Prescription Drug Label 1 62332-190 TABLET, COATED 40 mg ORAL ANDA 29 sections
Febuxostat Human Prescription Drug Label 1 62332-191 TABLET, COATED 80 mg ORAL ANDA 29 sections
ULORIC HUMAN PRESCRIPTION DRUG LABEL 1 64764-677 TABLET 80 mg ORAL NDA 32 sections
ULORIC HUMAN PRESCRIPTION DRUG LABEL 1 64764-918 TABLET 40 mg ORAL NDA 32 sections
Febuxostat Human Prescription Drug Label 1 67877-668 TABLET, FILM COATED 40 mg ORAL ANDA 28 sections