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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:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	3.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
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

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Approvals:

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

FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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Drug Use | Suggest Off label Use Form| |View source of the data|

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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

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🐶 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)

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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

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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

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External reference:

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ID	Source
012966	NDDF
101V0R1N2E	UNII
134018	PUBCHEM_CID
161190	MMSL
232999	MMSL
26212	MMSL
4025245	VUID
4025245	VANDF
441610003	SNOMEDCT_US
441743008	SNOMEDCT_US

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Pharmaceutical products:

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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

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