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

Stem definition	Drug id	CAS RN
anti-inflammatory, indometacin derivatives	1440	53-86-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: indomethacin hydrochloride indomethacin HCl indocin indomethacin indometacine indomethacine indometacin indomethacin sodium	A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Additional data needed to determine whether in vitro activity against SARS-CoV-2 corresponds with clinical efficacy in the treatment of COVID-19. Molecular weight: 357.79 Formula: C19H16ClNO4 CLOGP: 4.18 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 68.53 ALOGS: -5.17 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

indomethacin hydrochloride
indomethacin HCl
indocin
indomethacin
indometacine
indomethacine
indometacin
indomethacin sodium

A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Additional data needed to determine whether in vitro activity against SARS-CoV-2 corresponds with clinical efficacy in the treatment of COVID-19.

Molecular weight: 357.79
Formula: C19H16ClNO4
CLOGP: 4.18
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 68.53
ALOGS: -5.17
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.10	g	O
0.10	g	P
0.10	g	R
0.10	g	O
0.10	g	R

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	7.99 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	15 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.40 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.10 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
June 10, 1965	FDA

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
Oligohydramnios	420.57	12.06	134	21589	6232	63461067
Premature delivery	179.68	12.06	118	21605	30163	63437136
Neck deformity	158.19	12.06	49	21674	2072	63465227
Ankylosing spondylitis	150.72	12.06	73	21650	10401	63456898
Neck mass	140.14	12.06	51	21672	3552	63463747
Bone density abnormal	113.46	12.06	43	21680	3355	63463944
Oesophageal spasm	106.01	12.06	40	21683	3083	63464216
Oesophageal pain	95.97	12.06	39	21684	3662	63463637
Exposure during pregnancy	83.31	12.06	172	21551	155375	63311924
Premature baby	81.75	12.06	63	21660	20672	63446627

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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	155.06	12.89	64	13437	5540	34937890
Ductus arteriosus premature closure	102.01	12.89	23	13478	238	34943192
Gout	54.71	12.89	51	13450	19202	34924228
Sacroiliitis	47.93	12.89	19	13482	1479	34941951
Hepatitis B virus test positive	47.38	12.89	13	13488	314	34943116
Drug ineffective	43.59	12.89	313	13188	456438	34486992
Arthralgia	43.21	12.89	154	13347	169887	34773543
Exostosis	42.29	12.89	25	13476	4698	34938732
Tendon disorder	41.86	12.89	21	13480	2854	34940576
Ankle fracture	40.02	12.89	23	13478	4102	34939328

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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
Ankylosing spondylitis	288.77	11.78	123	29245	12082	79702938
Neck deformity	148.81	11.78	46	29322	1791	79713229
Neck mass	119.66	11.78	49	29319	4355	79710665
Oesophageal spasm	109.66	11.78	43	29325	3413	79711607
Bone density abnormal	103.93	11.78	40	29328	3020	79712000
Oesophageal pain	97.48	11.78	42	29326	4237	79710783
Drug ineffective	83.01	11.78	679	28689	1080234	78634786
Sacroiliitis	63.72	11.78	30	29338	3724	79711296
Corneal perforation	61.35	11.78	19	29349	744	79714276
Lymphoedema	60.23	11.78	44	29324	12369	79702651

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01EB03	CARDIOVASCULAR SYSTEM CARDIAC THERAPY OTHER CARDIAC PREPARATIONS Other cardiac preparations
ATC	M01AB01	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Acetic acid derivatives and related substances
ATC	M01AB51	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Acetic acid derivatives and related substances
ATC	M02AA23	MUSCULO-SKELETAL SYSTEM TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN Antiinflammatory preparations, non-steroids for topical use
ATC	S01BC01	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFLAMMATORY AGENTS Antiinflammatory agents, non-steroids
ATC	S01CC02	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION Antiinflammatory agents, non-steroids and antiinfectives in combination
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:35544	cyclooxygenase inhibitors
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:35845	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
Ankylosing spondylitis	indication	9631008	DOID:7147
Tendinitis	indication	34840004	DOID:971
Tenosynovitis	indication	67801009	DOID:970
Rheumatoid arthritis	indication	69896004	DOID:7148
Patent ductus arteriosus	indication	83330001	DOID:13832
Bursitis	indication	84017003	DOID:2965
Gout	indication	90560007	DOID:13189
Bursitis of shoulder	indication	239961006
Osteoarthritis	indication	396275006
Synovitis	indication	416209007	DOID:2703

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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	4.45	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
20MG	TIVORBEX	GENUS	N204768	Feb. 24, 2014	DISCN	CAPSULE	ORAL	9089471	April 23, 2030	TREATMENT OF PAIN
40MG	TIVORBEX	GENUS	N204768	Feb. 24, 2014	DISCN	CAPSULE	ORAL	9089471	April 23, 2030	TREATMENT OF PAIN

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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
50MG	INDOMETHACIN	ZYDUS	A216184	Aug. 2, 2023	RX	SUPPOSITORY	RECTAL	Jan. 30, 2024	COMPETITIVE GENERIC THERAPY

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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 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	7.21	WOMBAT-PK	CHEMBL
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	6.33	WOMBAT-PK	CHEMBL
Multidrug resistance-associated protein 1	Transporter	P33527	MRP1_HUMAN		IC50	4.92	CHEMBL
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN		EC50	9.85	CHEMBL
Prostaglandin D2 receptor 2	GPCR	Q9Y5Y4	PD2R2_HUMAN		Ki	6.53	WOMBAT-PK
Dehydrogenase/reductase SDR family member 9	Enzyme	Q9BPW9	DHRS9_HUMAN		IC50	4.85	CHEMBL
Aldose reductase	Enzyme	P15121	ALDR_HUMAN		IC50	5.22	CHEMBL
Aldo-keto reductase family 1 member C2	Enzyme	P52895	AK1C2_HUMAN		IC50	4.44	CHEMBL
Aldo-keto reductase family 1 member C3	Enzyme	P42330	AK1C3_HUMAN		IC50	7	CHEMBL
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN	AGONIST	Kd	7.38	IUPHAR

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External reference:

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ID	Source
IMN	PDB_CHEM_ID
002373	NDDF
002374	NDDF
1294612	RXNORM
1524	INN_ID
1909	IUPHAR_LIGAND_ID
2387	MMSL
2393	MMSL
3715	PUBCHEM_CID
373513008	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
INDOCIN	HUMAN PRESCRIPTION DRUG LABEL	1	42211-101	SUSPENSION	25 mg	ORAL	NDA	28 sections
INDOCIN	HUMAN PRESCRIPTION DRUG LABEL	1	42211-102	SUPPOSITORY	50 mg	RECTAL	ANDA	29 sections
Indomethacin	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1113	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	13 sections
Indomethacin	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1113	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	ANDA	13 sections
INDOMETHACIN	HUMAN PRESCRIPTION DRUG LABEL	1	0713-0176	SUPPOSITORY	50 mg	RECTAL	ANDA	14 sections
Indomethacin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-083	CAPSULE	50 mg	ORAL	ANDA	27 sections
Indomethacin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-919	CAPSULE, EXTENDED RELEASE	75 mg	ORAL	ANDA	12 sections
Indomethacin	Human Prescription Drug Label	1	10544-935	CAPSULE, EXTENDED RELEASE	75 mg	ORAL	ANDA	24 sections
INDOMETHACIN	HUMAN PRESCRIPTION DRUG LABEL	1	10702-016	CAPSULE, EXTENDED RELEASE	75 mg	ORAL	ANDA	28 sections
INDOMETHACIN	HUMAN PRESCRIPTION DRUG LABEL	1	16590-130	CAPSULE	50 mg	ORAL	ANDA	24 sections

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