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

Stem definition	Drug id	CAS RN
selective cyclo-oxygenase inhibitors	568	169590-42-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: celecoxib celebrex celecox celocoxib onsenal	A pyrazole derivative and selective CYCLOOXYGENASE 2 INHIBITOR that is used to treat symptoms associated with RHEUMATOID ARTHRITIS; OSTEOARTHRITIS and JUVENILE ARTHRITIS, as well as the management of ACUTE PAIN. Molecular weight: 381.37 Formula: C17H14F3N3O2S CLOGP: 4.57 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 77.98 ALOGS: -4.88 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

celecoxib
celebrex
celecox
celocoxib
onsenal

A pyrazole derivative and selective CYCLOOXYGENASE 2 INHIBITOR that is used to treat symptoms associated with RHEUMATOID ARTHRITIS; OSTEOARTHRITIS and JUVENILE ARTHRITIS, as well as the management of ACUTE PAIN.

Molecular weight: 381.37
Formula: C17H14F3N3O2S
CLOGP: 4.57
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 77.98
ALOGS: -4.88
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.20	g	O

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	17.49 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.00 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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Approvals:

Date	Agency	Company	Orphan
Dec. 31, 1998	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	1672.90	10.11	3409	210774	307278	62967561
Rheumatoid arthritis	545.77	10.11	1988	212195	251831	63023008
Arthralgia	447.14	10.11	3366	210817	566344	62708495
Musculoskeletal stiffness	443.07	10.11	1500	212683	183118	63091721
Drug ineffective	386.33	10.11	5281	208902	1039484	62235355
Death	367.01	10.11	434	213749	373947	62900892
Ankylosing spondylitis	332.99	10.11	279	213904	10195	63264644
Toxicity to various agents	280.08	10.11	253	213930	246997	63027842
Fibromyalgia	256.47	10.11	722	213461	79698	63195141
Loss of personal independence in daily activities	245.08	10.11	804	213379	96486	63178353

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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
Ankylosing spondylitis	447.87	10.63	214	63406	5390	34887921
Drug hypersensitivity	297.72	10.63	529	63091	80000	34813311
Psoriatic arthropathy	253.36	10.63	241	63379	19557	34873754
Arthralgia	177.13	10.63	694	62926	169347	34723964
Pain	162.89	10.63	770	62850	203905	34689406
Toxicity to various agents	130.71	10.63	104	63516	200258	34693053
Death	129.94	10.63	338	63282	397711	34495600
Arthritis	118.31	10.63	208	63412	31138	34862173
Musculoskeletal stiffness	107.18	10.63	252	63368	46428	34846883
Rheumatoid arthritis	102.99	10.63	220	63400	38018	34855293

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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	1885.90	9.87	3195	224705	295721	79220767
Rheumatoid arthritis	730.01	9.87	1746	226154	206724	79309764
Arthralgia	613.34	9.87	3234	224666	568569	78947919
Ankylosing spondylitis	596.39	9.87	394	227506	11811	79504677
Musculoskeletal stiffness	499.22	9.87	1357	226543	173651	79342837
Drug ineffective	497.69	9.87	4985	222915	1075928	78440560
Toxicity to various agents	456.93	9.87	324	227576	421216	79095272
Death	448.08	9.87	578	227322	565936	78950552
Psoriatic arthropathy	406.83	9.87	769	227131	77230	79439258
Pain	366.10	9.87	3334	224566	700468	78816020

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C08CA51	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives
ATC	L01XX33	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
ATC	M01AH01	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Coxibs
ATC	N02AJ16	NERVOUS SYSTEM ANALGESICS OPIOIDS Opioids in combination with non-opioid analgesics
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:50629	COX-2 inhibitor
CHEBI has role	CHEBI:176497	geroprotectors
FDA CS	M0001335	Anti-Inflammatory Agents, Non-Steroidal
FDA EPC	N0000175722	Nonsteroidal Anti-inflammatory Drug
FDA MoA	N0000000160	Cyclooxygenase Inhibitors

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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
Ankylosing spondylitis	indication	9631008	DOID:7147
Rheumatoid arthritis	indication	69896004	DOID:7148
Dysmenorrhea	indication	266599000
Osteoarthritis	indication	396275006
Juvenile rheumatoid arthritis	indication	410795001
Acute postoperative pain	indication	107401000119105
Alcoholism	contraindication	7200002
Peptic ulcer	contraindication	13200003	DOID:750
Myocardial infarction	contraindication	22298006	DOID:5844
Dehydration	contraindication	34095006

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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	9.79	acidic

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
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	10376527	May 27, 2036	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	10722456	May 27, 2036	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	10799517	May 27, 2036	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	9572819	May 27, 2036	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	9795620	May 27, 2036	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	9949990	May 27, 2036	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
56MG;44MG	SEGLENTIS	KOWA PHARMS	N213426	Oct. 15, 2021	RX	TABLET	ORAL	10238668	April 19, 2030	A METHOD FOR TREATMENT OF PAIN IN ADULTS USING TRAMADOL HYDROCHLORIDE AND CELECOXIB
56MG;44MG	SEGLENTIS	KOWA PHARMS	N213426	Oct. 15, 2021	RX	TABLET	ORAL	10548909	April 19, 2030	A METHOD FOR TREATMENT OF PAIN IN ADULTS USING TRAMADOL HYDROCHLORIDE AND CELECOXIB
56MG;44MG	SEGLENTIS	KOWA PHARMS	N213426	Oct. 15, 2021	RX	TABLET	ORAL	11478488	April 19, 2030	A METHOD FOR TREATMENT OF PAIN IN ADULTS USING TRAMADOL HYDROCHLORIDE AND CELECOXIB
EQ 10MG BASE;200MG	CONSENSI	PURPLE BIOTECH	N210045	May 31, 2018	DISCN	TABLET	ORAL	9662315	May 22, 2029	TREATMENT OF ADULT PATIENTS FOR WHOM TREATMENT WITH BOTH AMLODIPINE FOR HYPERTENSION AND CELECOXIB FOR OSTEOARTHRITIS ARE APPROPRIATE

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
25MG/ML	ELYXYB	SCILEX HLDG	N212157	May 5, 2020	DISCN	SOLUTION	ORAL	May 5, 2023	NEW PRODUCT
56MG;44MG	SEGLENTIS	KOWA PHARMS	N213426	Oct. 15, 2021	RX	TABLET	ORAL	Oct. 15, 2024	NEW PRODUCT

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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	7.24	WOMBAT-PK	CHEMBL
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN		IC50	7.30	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	4.85	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.48	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.14	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.16	DRUG MATRIX
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Ki	4.92	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	6.18	WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	6	DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	4.86	DRUG MATRIX

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External reference:

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ID	Source
CEL	PDB_CHEM_ID
007731	NDDF
116081000	SNOMEDCT_US
14020	MMSL
140587	RXNORM
174627	MMSL
2662	PUBCHEM_CID
2892	IUPHAR_LIGAND_ID
370187009	SNOMEDCT_US
4021143	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1515	CAPSULE	50 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1515	CAPSULE	50 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1520	CAPSULE	100 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1520	CAPSULE	100 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1525	CAPSULE	200 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1525	CAPSULE	200 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1530	CAPSULE	400 mg	ORAL	NDA	31 sections
CELEBREX	HUMAN PRESCRIPTION DRUG LABEL	1	0025-1530	CAPSULE	400 mg	ORAL	NDA	31 sections
Celecoxib	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7165	CAPSULE	100 mg	ORAL	ANDA	30 sections
Celecoxib	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7165	CAPSULE	100 mg	ORAL	ANDA	30 sections

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