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

Stem definition	Drug id	CAS RN
	2013	21256-18-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: oxaprozin alvo oxaprozin potassium WY 21743	An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE. Molecular weight: 293.32 Formula: C18H15NO3 CLOGP: 2.95 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 63.33 ALOGS: -3.96 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

oxaprozin
alvo
oxaprozin potassium
WY 21743

An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.

Molecular weight: 293.32
Formula: C18H15NO3
CLOGP: 2.95
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 63.33
ALOGS: -3.96
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.90	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	98 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	88.64 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1.60 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Oct. 29, 1992	FDA	GD SEARLE

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
Drug hypersensitivity	522.83	21.64	250	2305	310437	63176030
General symptom	34.96	21.64	10	2545	2798	63483669
Emotional distress	25.40	21.64	16	2539	32533	63453934

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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
Drug hypersensitivity	89.64	28.87	37	523	80492	34875879

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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
Drug hypersensitivity	574.78	23.25	245	2262	298671	79443210
General symptom	38.43	23.25	10	2497	2524	79739357
Emotional distress	28.59	23.25	17	2490	39952	79701929

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	M01AE12	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Propionic acid derivatives
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
FDA CS	M0001335	Anti-Inflammatory Agents, Non-Steroidal
FDA EPC	N0000175722	Nonsteroidal Anti-inflammatory Drug
FDA MoA	N0000000160	Cyclooxygenase Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D000894	Anti-Inflammatory Agents, Non-Steroidal
MeSH PA	D018501	Antirheumatic Agents

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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
Rheumatoid arthritis	indication	69896004	DOID:7148
Osteoarthritis	indication	396275006
Juvenile rheumatoid arthritis	indication	410795001
Ankylosing spondylitis	off-label use	9631008	DOID:7147
Peptic ulcer	contraindication	13200003	DOID:750
Myocardial infarction	contraindication	22298006	DOID:5844
Hypertensive disorder	contraindication	38341003	DOID:10763
Gastrointestinal ulcer	contraindication	40845000
Chronic heart failure	contraindication	48447003
Disorder of cardiovascular system	contraindication	49601007	DOID:1287

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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	4.51	acidic
pKa2	0.69	Basic

Orange Book patent data (new drug applications)

None

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
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	4.44	IUPHAR	CHEMBL
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	6.07	DRUG MATRIX	CHEMBL
fMet-Leu-Phe receptor	GPCR	P21462	FPR1_HUMAN				WOMBAT-PK
Retinoic acid receptor RXR-alpha	Nuclear hormone receptor	P19793	RXRA_HUMAN		EC50	4.79	CHEMBL
Retinoic acid receptor RXR-beta	Nuclear hormone receptor	P28702	RXRB_HUMAN		EC50	4.60	CHEMBL
Retinoic acid receptor RXR-gamma	Nuclear hormone receptor	P48443	RXRG_HUMAN		EC50	4.40	CHEMBL
Bifunctional epoxide hydrolase 2	Enzyme	P34913	HYES_HUMAN	INHIBITOR	IC50	5.30	IUPHAR
Complement C5	Secreted	P01031	CO5_HUMAN		Kd	6.19	CHEMBL
Serine hydroxymethyltransferase, mitochondrial	Enzyme	P34897	GLYM_HUMAN		IC50	5.71	CHEMBL
Nuclear receptor subfamily 4 group A member 2	Nuclear other	P43354	NR4A2_HUMAN		IC50	4.40	CHEMBL

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External reference:

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ID	Source
004113	NDDF
108518005	SNOMEDCT_US
174064-08-5	SECONDARY_CAS_RN
32613	RXNORM
3458	INN_ID
386031002	SNOMEDCT_US
4020735	VUID
4020735	VANDF
41102	MMSL
427736002	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Daypro	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1381	TABLET, FILM COATED	600 mg	ORAL	NDA	30 sections
Daypro	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1381	TABLET, FILM COATED	600 mg	ORAL	NDA	30 sections
Daypro	HUMAN PRESCRIPTION DRUG LABEL	1	55289-453	TABLET, FILM COATED	600 mg	ORAL	NDA	30 sections
Daypro	HUMAN PRESCRIPTION DRUG LABEL	1	55289-453	TABLET, FILM COATED	600 mg	ORAL	NDA	30 sections
Oxaprozin	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0924	TABLET, FILM COATED	600 mg	ORAL	ANDA	28 sections
Oxaprozin	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0924	TABLET, FILM COATED	600 mg	ORAL	ANDA	28 sections
Oxaprozin	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0141	TABLET	600 mg	ORAL	ANDA	29 sections
Oxaprozin	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0141	TABLET	600 mg	ORAL	ANDA	29 sections
Oxaprozin	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0141	TABLET	600 mg	ORAL	ANDA	29 sections
OXAPROZIN	HUMAN PRESCRIPTION DRUG LABEL	1	16590-178	TABLET	600 mg	ORAL	ANDA	24 sections

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