febuxostat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
xanthine oxydase and xanthine dehydrogenase inhibitor	1137	144060-53-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
80	mg	O

ADMET properties:

Property	Value	Reference
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 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Feb. 26, 2015	EMA
Feb. 13, 2009	FDA	TAKEDA PHARMS USA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.3	acidic
pKa2	0.46	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Xanthine dehydrogenase/oxidase	Enzyme	P47989	XDH_HUMAN	INHIBITOR	Ki	9.22	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		EC50	7.44	WOMBAT-PK
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	7.57	CHEMBL
Flavin reductase (NADPH)	Enzyme	P30043	BLVRB_HUMAN		Kd	5.79	CHEMBL
Xanthine dehydrogenase/oxidase	Enzyme		XDH_BOVIN		IC50	8.52	CHEMBL
Xanthine dehydrogenase/oxidase	Enzyme		XDH_RAT		IC50	8.40	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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