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 332.79 18.34 117 18802 8497 63461606
Tongue disorder 291.33 18.34 112 18807 10468 63459635
Blood parathyroid hormone decreased 285.24 18.34 108 18811 9683 63460420
Tenosynovitis 282.59 18.34 118 18801 13677 63456426
Panniculitis 272.89 18.34 109 18810 11276 63458827
Granuloma skin 256.42 18.34 96 18823 8341 63461762
Skin necrosis 254.78 18.34 110 18809 13840 63456263
Red blood cell sedimentation rate 246.67 18.34 81 18838 4773 63465330
Rheumatoid nodule 229.91 18.34 109 18810 17046 63453057
Drug eruption 227.30 18.34 128 18791 28566 63441537
Tendonitis 221.92 18.34 111 18808 19504 63450599
Hypercalcaemia 215.34 18.34 123 18796 28199 63441904
Ulcer 186.79 18.34 109 18810 25998 63444105
Renal impairment 181.49 18.34 174 18745 88181 63381922
Basal cell carcinoma 174.63 18.34 107 18812 27884 63442219
Cardiac failure 159.78 18.34 163 18756 88979 63381124
Aspartate aminotransferase increased 158.05 18.34 163 18756 90114 63379989
Skin ulcer 154.76 18.34 117 18802 42928 63427175
Alanine aminotransferase abnormal 143.24 18.34 53 18866 4451 63465652
C-reactive protein abnormal 137.02 18.34 112 18807 45984 63424119
Alanine aminotransferase increased 129.43 18.34 157 18762 103613 63366490
Acute kidney injury 127.16 18.34 257 18662 263158 63206945
Rash pruritic 121.26 18.34 117 18802 59682 63410421
Fear of injection 119.44 18.34 53 18866 7111 63462992
Red blood cell sedimentation rate increased 112.46 18.34 98 18821 43884 63426219
Blood creatinine increased 106.42 18.34 131 18788 87713 63382390
Drug tolerance decreased 99.37 18.34 63 18856 17410 63452693
Anaemia 98.66 18.34 248 18671 293182 63176921
Hyperkalaemia 95.02 18.34 98 18821 54105 63415998
Inflammation 93.75 18.34 119 18800 82154 63387949
Loss of personal independence in daily activities 79.67 18.34 120 18799 97170 63372933
C-reactive protein increased 79.25 18.34 118 18801 94589 63375514
Psoriatic arthropathy 73.68 18.34 112 18807 91408 63378695
Platelet count decreased 72.96 18.34 127 18792 115995 63354108
Granuloma 72.27 18.34 35 18884 5726 63464377
Drug tolerance 71.78 18.34 37 18882 6912 63463191
Erythema 66.93 18.34 156 18763 175595 63294508
Rheumatoid lung 65.85 18.34 29 18890 3819 63466284
Hepatic function abnormal 64.79 18.34 67 18852 37075 63433028
Neutrophil count decreased 57.09 18.34 77 18842 56329 63413774
Drug ineffective 57.05 18.34 144 18775 1044621 62425482
Joint injury 52.76 18.34 54 18865 29518 63440585
Tumour lysis syndrome 50.07 18.34 32 18887 8958 63461145
Systemic lupus erythematosus 47.37 18.34 4 18915 208914 63261189
Musculoskeletal disorder 46.80 18.34 43 18876 20601 63449502
Cardiac failure chronic 41.28 18.34 22 18897 4396 63465707
Blood uric acid increased 39.93 18.34 23 18896 5344 63464759
Cardiac failure acute 38.95 18.34 28 18891 9495 63460608
Gout 36.81 18.34 31 18888 13240 63456863
Blood pressure systolic increased 36.70 18.34 57 18862 47340 63422763
Sinusitis 36.66 18.34 11 18908 226642 63243461
Osteomyelitis 35.07 18.34 41 18878 25979 63444124
Decreased appetite 34.37 18.34 157 18762 250895 63219208
Fatigue 34.01 18.34 143 18776 887885 62582218
Swelling 33.93 18.34 20 18899 275358 63194745
Wound 32.33 18.34 5 18914 163258 63306845
Gastric disorder 31.85 18.34 47 18872 37322 63432781
Anaemia macrocytic 31.71 18.34 17 18902 3437 63466666
Anxiety 31.01 18.34 13 18906 217528 63252575
Toxicity to various agents 30.39 18.34 18 18901 247232 63222871
Therapeutic response decreased 29.52 18.34 60 18859 61465 63408638
Right ventricular failure 28.17 18.34 30 18889 17158 63452945
Chronic kidney disease 27.63 18.34 49 18870 45349 63424754
Depression 27.59 18.34 12 18907 196480 63273623
Paraesthesia 26.52 18.34 7 18912 156959 63313144
Therapy non-responder 26.28 18.34 65 18854 75836 63394267
Pneumonia aspiration 25.99 18.34 41 18878 34499 63435604
Hyperuricaemia 24.78 18.34 17 18902 5353 63464750
Coronavirus test positive 24.55 18.34 9 18910 736 63469367
Melaena 24.18 18.34 37 18882 30328 63439775
Cerebral infarction 23.23 18.34 32 18887 23861 63446242
Rash 23.16 18.34 262 18657 560609 62909494
Product dose omission issue 22.48 18.34 22 18897 234291 63235812
Upper respiratory tract inflammation 22.00 18.34 12 18907 2511 63467592
Pericarditis 21.98 18.34 6 18913 131573 63338530
Renal failure 21.95 18.34 81 18838 117571 63352532
Pulmonary arterial hypertension 21.59 18.34 30 18889 22547 63447556
Anaemia vitamin B12 deficiency 21.31 18.34 7 18912 412 63469691
Cardiac failure congestive 21.04 18.34 68 18851 92365 63377738
Haemorrhoidal haemorrhage 20.82 18.34 14 18905 4265 63465838
Synovitis 20.63 18.34 110 18809 186808 63283295
Impaired healing 20.61 18.34 3 18916 102539 63367564
Altered state of consciousness 20.45 18.34 31 18888 25199 63444904
Anti-neutrophil cytoplasmic antibody positive vasculitis 20.44 18.34 12 18907 2887 63467216
Blood urea increased 19.41 18.34 31 18888 26348 63443755
Interstitial lung disease 19.34 18.34 51 18868 61857 63408246
Disseminated intravascular coagulation 19.25 18.34 26 18893 19025 63451078
Myoglobin blood increased 19.03 18.34 9 18910 1396 63468707
Concomitant disease aggravated 18.77 18.34 18 18901 9094 63461009
Peripheral swelling 18.45 18.34 139 18780 265803 63204300
Gastrointestinal disorder 18.44 18.34 8 18911 131231 63338872

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 197.39 13.74 318 29824 94195 34832594
Tenosynovitis 177.05 13.74 84 30058 4486 34922303
Enthesopathy 173.25 13.74 83 30059 4530 34922259
Cardiac failure 171.68 13.74 293 29849 90955 34835834
Tongue disorder 141.78 13.74 76 30066 5263 34921526
Hepatic function abnormal 128.14 13.74 174 29968 44189 34882600
Interstitial lung disease 119.22 13.74 207 29935 65075 34861714
C-reactive protein abnormal 112.15 13.74 78 30064 8632 34918157
Acute kidney injury 112.07 13.74 539 29603 304449 34622340
Alanine aminotransferase abnormal 97.93 13.74 57 30085 4631 34922158
Tendonitis 93.02 13.74 71 30071 9069 34917720
Synovitis 90.78 13.74 84 30058 13982 34912807
Hyperkalaemia 88.50 13.74 189 29953 69200 34857589
Cerebral infarction 87.43 13.74 113 30029 27342 34899447
Tumour lysis syndrome 86.02 13.74 89 30053 16970 34909819
Gout 68.87 13.74 84 30058 19169 34907620
Respiratory tract haemorrhage 67.13 13.74 29 30113 1241 34925548
Aspartate aminotransferase increased 65.92 13.74 166 29976 67617 34859172
Red blood cell sedimentation rate 59.12 13.74 26 30116 1162 34925627
Granuloma skin 57.28 13.74 26 30116 1253 34925536
Platelet count decreased 56.16 13.74 228 29914 119489 34807300
Alanine aminotransferase increased 52.36 13.74 171 29971 80644 34846145
Panniculitis 51.86 13.74 28 30114 1966 34924823
Psoriatic arthropathy 51.66 13.74 74 30068 19724 34907065
Drug eruption 51.37 13.74 74 30068 19824 34906965
Cardiac failure chronic 50.73 13.74 47 30095 7832 34918957
Blood parathyroid hormone decreased 50.66 13.74 25 30117 1455 34925334
Neutrophil count decreased 49.51 13.74 125 30017 50979 34875810
Anaemia 49.33 13.74 357 29785 232978 34693811
Contraindicated product administered 48.46 13.74 75 30067 21406 34905383
Cardiac failure acute 45.97 13.74 51 30091 10519 34916270
Pemphigoid 45.10 13.74 46 30096 8620 34918169
Toxicity to various agents 44.42 13.74 65 30077 200297 34726492
Haemorrhage subcutaneous 42.65 13.74 26 30116 2298 34924491
Blood creatinine increased 42.24 13.74 178 29964 94798 34831991
Gouty tophus 41.95 13.74 12 30130 145 34926644
Death 41.86 13.74 189 29953 397860 34528929
Hypocalcaemia 40.40 13.74 74 30068 24215 34902574
Rash 38.30 13.74 325 29817 222427 34704362
Rheumatoid nodule 37.01 13.74 26 30116 2921 34923868
Loss of personal independence in daily activities 36.22 13.74 85 30057 33094 34893695
General physical health deterioration 35.41 13.74 210 29932 128059 34798730
Hyperuricaemia 35.30 13.74 39 30103 8004 34918785
Chronic kidney disease 35.01 13.74 96 30046 41114 34885675
Concomitant disease aggravated 34.76 13.74 33 30109 5668 34921121
Lactic acidosis 33.61 13.74 85 30057 34687 34892102
Cerebral haemorrhage 33.35 13.74 85 30057 34852 34891937
C-reactive protein increased 31.95 13.74 111 30031 53987 34872802
Erythema 31.71 13.74 156 29986 88624 34838165
Congenital diaphragmatic anomaly 31.16 13.74 7 30135 28 34926761
Fatigue 31.07 13.74 190 29952 370463 34556326
Fulminant type 1 diabetes mellitus 30.35 13.74 15 30127 876 34925913
Hypercalcaemia 29.43 13.74 50 30092 15418 34911371
Renal failure 29.40 13.74 203 29939 130354 34796435
Hepatic enzyme increased 29.26 13.74 87 30055 38993 34887796
Asthenia 29.09 13.74 111 30031 245140 34681649
Orthostatic intolerance 28.46 13.74 14 30128 809 34925980
Liver disorder 28.15 13.74 77 30065 32920 34893869
Blood uric acid increased 28.13 13.74 38 30104 9586 34917203
Corneal abscess 27.80 13.74 6 30136 19 34926770
Shock haemorrhagic 27.53 13.74 41 30101 11313 34915476
Osteoma 27.50 13.74 8 30134 103 34926686
Polycystic liver disease 27.43 13.74 8 30134 104 34926685
Skin necrosis 26.76 13.74 29 30113 5824 34920965
Splenic necrosis 26.63 13.74 8 30134 116 34926673
Hyperkinetic heart syndrome 26.38 13.74 8 30134 120 34926669
Transformation to acute myeloid leukaemia 26.27 13.74 13 30129 761 34926028
Haemoglobin urine present 25.90 13.74 8 30134 128 34926661
Splenic cyst 25.79 13.74 8 30134 130 34926659
Hypokalaemia 25.77 13.74 109 30033 58105 34868684
Drug ineffective 25.75 13.74 261 29881 456490 34470299
Rubber sensitivity 25.46 13.74 9 30133 223 34926566
Blood lactic acid 25.42 13.74 10 30132 336 34926453
Depression 25.11 13.74 28 30114 97070 34829719
Activated partial thromboplastin time abnormal 24.87 13.74 8 30134 147 34926642
Intentional overdose 24.71 13.74 4 30138 43670 34883119
Anxiety 24.28 13.74 30 30112 99398 34827391
Hyperhidrosis 24.12 13.74 18 30124 75674 34851115
Renal ischaemia 23.70 13.74 11 30131 558 34926231
Decreased appetite 23.10 13.74 232 29910 166160 34760629
Cerebral ventricular rupture 22.56 13.74 8 30134 200 34926589
Suicidal ideation 22.19 13.74 4 30138 40384 34886405
Product prescribing error 22.10 13.74 56 30086 22871 34903918
Pneumonia bacterial 22.09 13.74 38 30104 11834 34914955
Cytomegalovirus nephritis 22.05 13.74 7 30135 123 34926666
Product dose omission issue 21.76 13.74 44 30098 119667 34807122
Procedural failure 21.41 13.74 6 30136 67 34926722
Pulmonary alveolar haemorrhage 20.96 13.74 29 30113 7483 34919306
Off label use 20.72 13.74 247 29895 419277 34507512
Arrhythmia 20.72 13.74 73 30069 35735 34891054
Post infection glomerulonephritis 20.72 13.74 6 30136 76 34926713
Splenic lesion 20.62 13.74 8 30134 259 34926530
Thalamus haemorrhage 20.41 13.74 12 30130 993 34925796
Seizure 20.40 13.74 37 30105 104820 34821969
Treatment failure 20.33 13.74 87 30055 46610 34880179
Urinary sediment present 19.95 13.74 8 30134 283 34926506
Nephrogenic anaemia 19.95 13.74 16 30126 2195 34924594
Adrenal insufficiency 19.91 13.74 40 30102 14007 34912782
Disseminated intravascular coagulation 19.70 13.74 52 30090 21764 34905025
Altered state of consciousness 19.10 13.74 53 30089 22840 34903949
Aggression 19.09 13.74 5 30137 38959 34887830
Hypothyroidism 19.06 13.74 50 30092 20852 34905937
Ulcer 18.75 13.74 30 30112 8805 34917984
Drug-induced liver injury 18.64 13.74 61 30081 28771 34898018
Blood uric acid decreased 18.54 13.74 8 30134 341 34926448
Diabetic nephropathy 18.35 13.74 15 30127 2113 34924676
Lordosis 18.31 13.74 8 30134 352 34926437
Haematochezia 18.22 13.74 84 30058 46450 34880339
Gastric cancer 18.09 13.74 25 30117 6444 34920345
Agitation 17.84 13.74 14 30128 57385 34869404
Conjunctival ulcer 17.67 13.74 5 30137 58 34926731
Oedema peripheral 17.56 13.74 169 29973 119643 34807146
Red blood cell abnormality 17.42 13.74 8 30134 396 34926393
Pseudohyponatraemia 16.87 13.74 5 30137 69 34926720
Metastases to soft tissue 16.84 13.74 8 30134 428 34926361
Respiratory distress 16.68 13.74 5 30137 35660 34891129
Stress 16.68 13.74 3 30139 30344 34896445
Mental status changes 16.65 13.74 6 30136 38077 34888712
Weight decreased 16.53 13.74 87 30055 176214 34750575
Multiple drug therapy 16.41 13.74 8 30134 453 34926336
Stevens-Johnson syndrome 16.40 13.74 44 30098 18595 34908194
Hypovolaemic shock 16.34 13.74 25 30117 7060 34919729
International normalised ratio abnormal 16.09 13.74 17 30125 3318 34923471
Dyspnoea paroxysmal nocturnal 16.03 13.74 12 30130 1487 34925302
Rheumatoid lung 15.92 13.74 10 30132 932 34925857
Suicide attempt 15.73 13.74 7 30135 39109 34887680
Myelosuppression 15.48 13.74 44 30098 19221 34907568
Enterocolitis 15.34 13.74 26 30116 8000 34918789
Cardiac arrest 15.30 13.74 38 30104 96121 34830668
Haematocrit abnormal 15.27 13.74 9 30133 748 34926041
Erythema multiforme 15.20 13.74 27 30115 8622 34918167
Glomerular filtration rate decreased 15.01 13.74 34 30108 12927 34913862
Rash pruritic 14.80 13.74 54 30088 26887 34899902
Thrombotic cerebral infarction 14.76 13.74 7 30135 373 34926416
Lower gastrointestinal haemorrhage 14.71 13.74 28 30114 9424 34917365
Drug hypersensitivity 14.58 13.74 119 30023 80410 34846379
Brain natriuretic peptide increased 14.53 13.74 21 30121 5638 34921151
Nephrotic syndrome 14.41 13.74 24 30118 7279 34919510
Hypoparathyroidism 14.36 13.74 8 30134 597 34926192
Thirst 14.33 13.74 25 30117 7870 34918919
Blood urea increased 14.33 13.74 58 30084 30306 34896483
Low cardiac output syndrome 14.33 13.74 8 30134 600 34926189
Tonsil cancer 14.20 13.74 10 30132 1128 34925661
Acute myeloid leukaemia 13.98 13.74 41 30101 18229 34908560
Infective spondylitis 13.97 13.74 6 30136 253 34926536
Melaena 13.95 13.74 64 30078 35316 34891473

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 421.19 13.80 181 46239 11427 79686541
Renal impairment 382.54 13.80 465 45955 157318 79540650
Tenosynovitis 376.53 13.80 183 46237 15371 79682597
Tongue disorder 355.15 13.80 170 46250 13805 79684163
Cardiac failure 322.32 13.80 423 45997 154419 79543549
Tendonitis 265.14 13.80 168 46252 23662 79674306
Acute kidney injury 257.37 13.80 773 45647 518631 79179337
Blood parathyroid hormone decreased 243.13 13.80 120 46300 10416 79687552
Panniculitis 236.26 13.80 124 46296 12247 79685721
Alanine aminotransferase abnormal 231.80 13.80 110 46310 8757 79689211
Red blood cell sedimentation rate 229.29 13.80 95 46325 5470 79692498
Granuloma skin 225.21 13.80 109 46311 9065 79688903
Hepatic function abnormal 214.67 13.80 238 46182 72869 79625099
Drug eruption 204.94 13.80 184 46236 43751 79654217
Skin necrosis 194.95 13.80 125 46295 17962 79680006
Hyperkalaemia 192.11 13.80 282 46138 114116 79583852
Rheumatoid nodule 191.63 13.80 122 46298 17316 79680652
Aspartate aminotransferase increased 185.77 13.80 308 46112 138333 79559635
Hypercalcaemia 173.44 13.80 158 46262 38272 79659696
C-reactive protein abnormal 167.66 13.80 172 46248 48195 79649773
Tumour lysis syndrome 154.59 13.80 121 46299 23818 79674150
Interstitial lung disease 153.29 13.80 252 46168 112348 79585620
Platelet count decreased 149.67 13.80 342 46078 194322 79503646
Alanine aminotransferase increased 147.05 13.80 305 46115 162265 79535703
Anaemia 143.61 13.80 575 45845 444440 79253528
Ulcer 140.69 13.80 126 46294 29846 79668122
Blood creatinine increased 129.92 13.80 282 46138 154775 79543193
Cerebral infarction 122.63 13.80 142 46278 45534 79652434
Basal cell carcinoma 111.94 13.80 123 46297 37252 79660716
Neutrophil count decreased 111.64 13.80 198 46222 93761 79604207
Fear of injection 109.77 13.80 63 46357 7411 79690557
Skin ulcer 103.39 13.80 142 46278 54008 79643960
Psoriatic arthropathy 98.69 13.80 169 46251 77830 79620138
Rash pruritic 87.74 13.80 153 46267 71476 79626492
Cardiac failure acute 87.69 13.80 79 46341 18850 79679118
Cardiac failure chronic 86.79 13.80 63 46357 11072 79686896
C-reactive protein increased 83.29 13.80 212 46208 128815 79569153
Toxicity to various agents 82.99 13.80 74 46346 421466 79276502
Loss of personal independence in daily activities 81.83 13.80 183 46237 102397 79595571
Drug ineffective 80.85 13.80 340 46080 1080573 78617395
Gout 80.33 13.80 85 46335 24664 79673304
Drug tolerance decreased 71.92 13.80 60 46360 12918 79685050
Rheumatoid lung 71.08 13.80 39 46381 4206 79693762
Drug abuse 69.55 13.80 7 46413 162684 79535284
Respiratory tract haemorrhage 68.00 13.80 29 46391 1794 79696174
Erythema 67.43 13.80 283 46137 223007 79474961
Fatigue 66.63 13.80 297 46123 929430 78768538
Hyperuricaemia 64.24 13.80 54 46366 11745 79686223
Chronic kidney disease 63.14 13.80 127 46293 66027 79631941
Drug tolerance 62.92 13.80 47 46373 8628 79689340
Sinusitis 62.71 13.80 18 46402 195483 79502485
Granuloma 62.53 13.80 46 46374 8251 79689717
Inflammation 61.48 13.80 155 46265 93598 79604370
Decreased appetite 60.39 13.80 373 46047 342045 79355923
Pemphigoid 59.56 13.80 58 46362 15257 79682711
Renal failure 58.56 13.80 252 46168 200716 79497252
Anxiety 57.34 13.80 37 46383 248475 79449493
Hypocalcaemia 56.45 13.80 103 46317 49821 79648147
Cerebral haemorrhage 55.38 13.80 111 46309 57562 79640406
Haemorrhage subcutaneous 53.71 13.80 34 46386 4775 79693193
Red blood cell sedimentation rate increased 53.49 13.80 96 46324 45846 79652122
Depression 51.77 13.80 31 46389 216759 79481209
General physical health deterioration 50.51 13.80 303 46117 274935 79423033
Concomitant disease aggravated 49.59 13.80 49 46371 13118 79684850
Glossodynia 48.19 13.80 3 46417 103334 79594634
Intentional overdose 46.77 13.80 4 46416 105956 79592012
Systemic lupus erythematosus 45.15 13.80 8 46412 121141 79576827
Pain 43.85 13.80 236 46184 703566 78994402
Disseminated intravascular coagulation 43.14 13.80 76 46344 35766 79662202
Joint injury 42.41 13.80 70 46350 31265 79666703
Musculoskeletal disorder 42.06 13.80 57 46363 21391 79676577
Discomfort 41.33 13.80 11 46409 125606 79572362
Transformation to acute myeloid leukaemia 41.00 13.80 17 46403 980 79696988
Asthenia 39.26 13.80 159 46261 511530 79186438
Altered state of consciousness 38.13 13.80 81 46339 43741 79654227
Lactic acidosis 37.72 13.80 108 46312 70251 79627717
Lower respiratory tract infection 37.72 13.80 14 46406 129206 79568762
Nephrogenic anaemia 37.24 13.80 25 46395 3877 79694091
Swelling 36.95 13.80 43 46377 216668 79481300
Migraine 36.78 13.80 4 46416 87489 79610479
Liver disorder 36.75 13.80 109 46311 72308 79625660
Melaena 36.14 13.80 97 46323 60793 79637175
Hyperhidrosis 35.69 13.80 22 46398 151470 79546498
Blood urea increased 35.52 13.80 84 46336 48706 79649262
Blood uric acid increased 34.95 13.80 41 46379 13319 79684649
Haematochezia 34.57 13.80 121 46299 87524 79610444
Gastrointestinal disorder 34.41 13.80 14 46406 122191 79575777
Synovitis 33.64 13.80 175 46245 150559 79547409
Product dose omission issue 33.39 13.80 58 46362 247479 79450489
Cardiac failure congestive 32.94 13.80 167 46253 142235 79555733
Fulminant type 1 diabetes mellitus 31.58 13.80 16 46404 1467 79696501
Atrial fibrillation 31.40 13.80 210 46210 197676 79500292
Osteomyelitis 31.24 13.80 63 46357 32802 79665166
Oedema peripheral 30.51 13.80 251 46169 252037 79445931
Injection site pain 30.38 13.80 19 46401 129819 79568149
Orthostatic intolerance 30.36 13.80 17 46403 1907 79696061
Osteoma 30.27 13.80 8 46412 108 79697860
Stress 30.23 13.80 5 46415 79607 79618361
Right ventricular failure 29.81 13.80 51 46369 23446 79674522
Rhabdomyolysis 29.76 13.80 129 46291 103002 79594966
White blood cell count decreased 29.38 13.80 199 46221 188089 79509879
Aplasia pure red cell 29.29 13.80 29 46391 7781 79690187
Pericarditis 29.25 13.80 12 46408 104224 79593744
Hyperkinetic heart syndrome 28.89 13.80 8 46412 130 79697838
Wound 28.60 13.80 16 46404 116163 79581805
Suicidal ideation 28.53 13.80 5 46415 76335 79621633
Blood pressure fluctuation 28.40 13.80 3 46417 67142 79630826
Duodenal ulcer perforation 27.90 13.80 3 46417 66208 79631760
Pneumonia aspiration 27.75 13.80 94 46326 66873 79631095
Shock haemorrhagic 27.40 13.80 45 46375 20015 79677953
Hypokalaemia 27.30 13.80 160 46260 143880 79554088
Pneumonia bacterial 27.26 13.80 44 46376 19287 79678681
Polycystic liver disease 27.10 13.80 8 46412 165 79697803
Splenic necrosis 26.83 13.80 8 46412 171 79697797
Confusional state 26.83 13.80 95 46325 317902 79380066
Cerebral ventricular rupture 26.47 13.80 10 46410 450 79697518
Pulmonary alveolar haemorrhage 26.44 13.80 33 46387 11424 79686544
Impaired healing 26.43 13.80 9 46411 87646 79610322
Blood lactic acid 26.41 13.80 10 46410 453 79697515
Intentional product use issue 26.11 13.80 30 46390 152082 79545886
Thalamus haemorrhage 26.11 13.80 15 46405 1767 79696201
Paraesthesia 25.94 13.80 39 46381 176284 79521684
Acute myeloid leukaemia 25.62 13.80 56 46364 30829 79667139
Rash 25.38 13.80 475 45945 577883 79120085
Helicobacter infection 25.12 13.80 5 46415 69699 79628269
Injury 25.08 13.80 7 46413 77489 79620479
Renal disorder 24.91 13.80 67 46353 42038 79655930
Enterocolitis 24.64 13.80 36 46384 14476 79683492
Gastric disorder 24.64 13.80 62 46358 37371 79660597
Corneal abscess 24.62 13.80 6 46414 57 79697911
Arrhythmia 24.51 13.80 85 46335 61187 79636781
Suicide attempt 24.18 13.80 9 46411 82923 79615045
Influenza like illness 24.12 13.80 6 46414 71701 79626267
Blood pressure decreased 23.95 13.80 118 46302 99348 79598620
Nephrotic syndrome 23.92 13.80 31 46389 11143 79686825
Seizure 23.89 13.80 46 46374 188788 79509180
Splenic cyst 23.77 13.80 8 46412 256 79697712
Myelosuppression 23.71 13.80 64 46356 40232 79657736
Diabetic nephropathy 23.71 13.80 17 46403 2930 79695038
Vomiting 23.56 13.80 261 46159 665567 79032401
Gouty tophus 23.43 13.80 9 46411 424 79697544
Cytomegalovirus nephritis 23.37 13.80 7 46413 152 79697816
Gait disturbance 23.37 13.80 54 46366 207452 79490516
Product prescribing error 23.26 13.80 68 46352 44745 79653223
Drug titration error 23.19 13.80 12 46408 1150 79696818
Renal ischaemia 23.19 13.80 12 46408 1150 79696818
Colon cancer 23.19 13.80 35 46385 14488 79683480
Upper respiratory tract inflammation 23.07 13.80 19 46401 4016 79693952
Brain natriuretic peptide increased 22.76 13.80 27 46393 8873 79689095
Heart rate increased 22.75 13.80 22 46398 120702 79577266
Therapy non-responder 22.58 13.80 110 46310 92195 79605773
Procedural failure 22.50 13.80 6 46414 84 79697884
Pleural effusion 22.34 13.80 153 46267 145109 79552859
Erythema multiforme 21.98 13.80 38 46382 17613 79680355
Blood lactate dehydrogenase increased 21.85 13.80 61 46359 39109 79658859
Activated partial thromboplastin time abnormal 21.66 13.80 8 46412 338 79697630
Drug-induced liver injury 21.66 13.80 86 46334 66031 79631937
Post infection glomerulonephritis 21.53 13.80 6 46414 100 79697868
Gastric cancer 21.41 13.80 28 46392 10151 79687817
Nasopharyngitis 21.30 13.80 76 46344 253805 79444163
Glomerular filtration rate decreased 20.96 13.80 43 46377 22659 79675309
Pulmonary arterial hypertension 20.82 13.80 49 46371 28317 79669651
Sleep disorder 20.79 13.80 12 46408 85665 79612303
Pain in extremity 20.60 13.80 126 46294 364412 79333556
Dry mouth 20.42 13.80 13 46407 88006 79609962
Contraindicated product administered 20.26 13.80 159 46261 157379 79540589
Blood creatine phosphokinase increased 20.09 13.80 84 46336 66006 79631962
Off label use 20.08 13.80 390 46030 906825 78791143
Stevens-Johnson syndrome 19.91 13.80 59 46361 39107 79658861
Adverse drug reaction 19.70 13.80 7 46413 66385 79631583
Plasma cell myeloma 19.69 13.80 72 46348 53187 79644781
Lordosis 19.60 13.80 8 46412 443 79697525
Prostatic specific antigen abnormal 19.43 13.80 8 46412 453 79697515
Product use in unapproved indication 19.03 13.80 78 46342 250281 79447687
Joint swelling 18.91 13.80 95 46325 288551 79409417
Sudden death 18.88 13.80 41 46379 22470 79675498
Asthma 18.81 13.80 31 46389 135064 79562904
Therapeutic response decreased 18.80 13.80 83 46337 66770 79631198
Dehydration 18.78 13.80 224 46196 247963 79450005
Hypovolaemic shock 18.77 13.80 29 46391 12247 79685721
Low cardiac output syndrome 18.61 13.80 10 46410 1035 79696933
Infective spondylitis 18.59 13.80 8 46412 506 79697462
Hypercreatininaemia 18.53 13.80 10 46410 1043 79696925
Cardiac arrest 18.41 13.80 46 46374 172050 79525918
Intentional product misuse 18.33 13.80 17 46403 95148 79602820
Mental status changes 18.32 13.80 8 46412 66951 79631017
Prerenal failure 18.25 13.80 16 46404 3682 79694286
Memory impairment 18.15 13.80 23 46397 111711 79586257
Febrile neutropenia 18.14 13.80 210 46210 230789 79467179
Conjunctival ulcer 18.07 13.80 5 46415 81 79697887
Coronavirus test positive 17.88 13.80 10 46410 1119 79696849
Agitation 17.84 13.80 19 46401 99696 79598272
Drug ineffective for unapproved indication 17.80 13.80 4 46416 51234 79646734
Bile duct stone 17.79 13.80 19 46401 5570 79692398
Azotaemia 17.78 13.80 23 46397 8253 79689715
Anaemia macrocytic 17.76 13.80 19 46401 5578 79692390
Splenic lesion 17.69 13.80 8 46412 570 79697398
Injection site reaction 17.63 13.80 5 46415 54780 79643188
Hypoaesthesia 17.62 13.80 50 46370 179302 79518666
Subdural haematoma 17.57 13.80 49 46371 31385 79666583
Adrenal insufficiency 17.53 13.80 46 46374 28441 79669527
Folate deficiency 17.52 13.80 15 46405 3345 79694623
Weight decreased 17.45 13.80 128 46292 355070 79342898
Metastases to soft tissue 17.29 13.80 8 46412 601 79697367
Embolic stroke 17.20 13.80 22 46398 7804 79690164
Tachycardia 17.14 13.80 50 46370 177718 79520250
Tubulointerstitial nephritis 17.03 13.80 55 46365 38180 79659788
Death 17.01 13.80 230 46190 566284 79131684
Thirst 16.87 13.80 35 46385 18584 79679384
Blood uric acid decreased 16.66 13.80 10 46410 1278 79696690
Aortic dissection 16.59 13.80 16 46404 4159 79693809
Alopecia 16.40 13.80 74 46346 231281 79466687
Injection site erythema 16.24 13.80 13 46407 78184 79619784
Hepatocellular carcinoma 16.23 13.80 23 46397 8998 79688970
Dyspnoea paroxysmal nocturnal 16.00 13.80 12 46408 2216 79695752
Pseudohyponatraemia 15.77 13.80 5 46415 132 79697836
Weight increased 15.60 13.80 96 46324 277290 79420678
Enteritis infectious 15.59 13.80 14 46406 3324 79694644
Red blood cell abnormality 15.58 13.80 8 46412 754 79697214
Lower gastrointestinal haemorrhage 15.43 13.80 31 46389 16094 79681874
Anaemia vitamin B12 deficiency 15.33 13.80 8 46412 780 79697188
Cognitive disorder 15.32 13.80 11 46409 69915 79628053
Feeling abnormal 15.19 13.80 45 46375 159154 79538814
Cerebellar haemorrhage 15.15 13.80 13 46407 2907 79695061
Urinary retention 14.95 13.80 69 46351 56561 79641407
Troponin increased 14.94 13.80 34 46386 19221 79678747
Tonsil cancer 14.93 13.80 9 46411 1159 79696809
Systemic infection 14.86 13.80 23 46397 9729 79688239
Gait inability 14.66 13.80 8 46412 58909 79639059
Thrombotic cerebral infarction 14.65 13.80 7 46413 565 79697403
Bacterial prostatitis 14.56 13.80 4 46416 63 79697905
Folliculitis 14.55 13.80 7 46413 55373 79642595
Physical deconditioning 14.53 13.80 11 46409 2059 79695909
Cough 14.48 13.80 140 46280 366649 79331319
Obstructive pancreatitis 14.42 13.80 8 46412 882 79697086
Dysphagia 14.38 13.80 31 46389 122105 79575863
Spinal compression fracture 14.35 13.80 31 46389 16927 79681041
Blister 14.34 13.80 30 46390 119446 79578522
Renal function test abnormal 14.19 13.80 16 46404 4982 79692986
Nasal mucosal erosion 14.17 13.80 4 46416 70 79697898
Osteoarthritis 14.15 13.80 18 46402 87291 79610677
Psoriasis 13.98 13.80 19 46401 89568 79608400
Sleep disorder due to general medical condition, insomnia type 13.97 13.80 4 46416 43552 79654416
Henoch-Schonlein purpura 13.93 13.80 12 46408 2698 79695270
Haemoglobin urine present 13.89 13.80 8 46412 947 79697021
Type 2 diabetes mellitus 13.86 13.80 8 46412 57114 79640854
Blood cholesterol increased 13.84 13.80 17 46403 83703 79614265

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 | Suggest Off label Use Form| |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
ATP-binding cassette sub-family G member 2 Transporter IC50 7.57 CHEMBL
Flavin reductase (NADPH) Enzyme Kd 5.79 CHEMBL
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 30 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0054-0413 TABLET 40 mg ORAL ANDA 30 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0054-0414 TABLET 80 mg ORAL ANDA 30 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0054-0414 TABLET 80 mg ORAL ANDA 30 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0378-3925 TABLET, FILM COATED 40 mg ORAL ANDA 29 sections
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 0378-3925 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 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 0527-2244 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 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 27808-206 TABLET 40 mg ORAL ANDA 32 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
Febuxostat HUMAN PRESCRIPTION DRUG LABEL 1 27808-207 TABLET 80 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 43547-295 TABLET 40 mg ORAL ANDA 29 sections
FEBUXOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 43547-295 TABLET 40 mg ORAL ANDA 29 sections
FEBUXOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 43547-296 TABLET 80 mg ORAL ANDA 29 sections
FEBUXOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 43547-296 TABLET 80 mg ORAL ANDA 29 sections
Febuxostat Human Prescription Drug Label 1 46708-190 TABLET, COATED 40 mg ORAL ANDA 29 sections
Febuxostat Human Prescription Drug Label 1 46708-190 TABLET, COATED 40 mg ORAL ANDA 29 sections