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

Stem definition	Drug id	CAS RN
anti-inflammatory agents, ibuprofen derivatives	2652	33005-95-7

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tiaprofenic acid
(RS)-Tiaprofenic acid
(+/-)-Tiaprofenic acid
tiaprofen

Molecular weight: 260.31
Formula: C14H12O3S
CLOGP: 2.54
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 54.37
ALOGS: -3.91
ROTB: 4

Drug dosage:

Dose	Unit	Route
0.60	g	O
0.60	g	R

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	38.42 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.08 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.62 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.10 hours	Lombardo F, Berellini G, Obach RS

Approvals:

None

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
Aspirin-exacerbated respiratory disease	53.02	50.46	9	645	886	63487482

FDA Adverse Event Reporting System (Male)

None

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
Musculoskeletal discomfort	123.01	57.51	32	1005	19803	79723548
Limb discomfort	102.70	57.51	31	1006	32819	79710532
Localised infection	98.60	57.51	31	1006	37544	79705807
Gait inability	84.92	57.51	31	1006	58886	79684465
Liver disorder	78.70	57.51	31	1006	72386	79670965

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M01AE11	MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Propionic acid derivatives
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
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:88188	allergenic drug

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

Disease	Relation	SNOMED_ID	DOID
Pain	indication	22253000
Rheumatoid arthritis	indication	69896004	DOID:7148
Osteoarthritis	indication	396275006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.82	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	7.10		WOMBAT-PK	SCIENTIFIC LITERATURE
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	5.90		WOMBAT-PK	SCIENTIFIC LITERATURE

External reference:

ID	Source
D01325	KEGG_DRUG
C0076653	UMLSCUI
CHEBI:32221	CHEBI
CHEMBL365795	ChEMBL_ID
DB01600	DRUGBANK_ID
C021270	MESH_SUPPLEMENTAL_RECORD_UI
5468	PUBCHEM_CID
3320	INN_ID
1LS1T6R34C	UNII
38253	RXNORM
003468	NDDF
329889002	SNOMEDCT_US
395902007	SNOMEDCT_US

Pharmaceutical products:

None