Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMRKXPT)

Drug Name

Ketoprofen Drug Info

Synonyms

Actron; Alrheumat; Alrheumum; Alrheumun; Aneol; Capisten; Dexal; Epatec; Fastum; Kefenid; Ketoprofene; Ketoprofeno; Ketoprofenum; Ketopron; Ketoprophene; Lertus; Menamin; Meprofen; Orudis; Orugesic; Oruvail; Oscorel; Profenid; Toprec; Toprek; Benzoylhydratropic Acid; Orudis KT; K 1751; RP 19583; RP19583; RU 4733; Arthril (TN); Fastum (TN); Fastum Gel (TN); Iso-K; Keto (TN); Ketoflam (TN); Ketomex (TN); Ketonal (TN); Ketoprofenas (TN); Ketoprofene (TN); Ketoprofene [INN-French]; Ketoprofeno [INN-Spanish]; Ketoprofenum (TN); Ketoprofenum [INN-Latin]; Ketorin (TN); Ketospray (TN); Lasonil (TN); M-Benzoylhydratropic acid; Oki (TN); Orudis (TN); Oruvail (TN); RP-19583; Racemic-Ketoprofen; Zon (TN); Bi-Profnid (TN); RP, 19,583; Ketoprofen (JP15/USP/INN); Ketoprofen [USAN:INN:BAN:JAN]; Orudis, Oruvail, Ketoflam, Orudis KT, Ketoprofen; Acide (benzoyl-3-phenyl)-2-propionique; Acide (benzoyl-3-phenyl)-2-propionique [French]; L'Acide (benzoyl-3-phenyl)-2-propionique; (+-)-m-Benzoylhydratropic acid; 2-(3-Benzoylphenyl)propanoic acid; 2-(3-Benzoylphenyl)propionic acid; 2-(m-Benzoylphenyl)propionic acid; 2-[3-(benzoyl)phenyl]propanoic acid; 2-[3-(phenylcarbonyl)phenyl]propanoic acid; 2-[3-Benzoylphenyl]propionic acid; 3-Benzoylhydratropic acid

Indication

Disease Entry	ICD 11	Status	REF
Bursitis		Approved	[1]
Dysmenorrhea	GA34.3	Approved	[1]
Musculoskeletal pain	MG30	Approved	[2]
Pain	MG30-MG3Z	Phase 3	[3]
Migraine	8A80	Phase 2	[4]
Osteoarthritis	FA00-FA05	Phase 1	[4]

Therapeutic Class

Analgesics

Cross-matching ID

PubChem CID: 3825
ChEBI ID: CHEBI:6128
CAS Number: CAS 22071-15-4
TTD Drug ID: DMRKXPT
VARIDT Drug ID: DR00690
INTEDE Drug ID: DR0907
ACDINA Drug ID: D00343

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostaglandin G/H synthase 2 (COX-2)	TTVKILB	PGH2_HUMAN	Inhibitor	[5]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[6]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Approved	[7]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

ICD Disease Classification

15 Disease of the musculoskeletal system/connective tissue

Disease Class

ICD-11: FA20 Rheumatoid arthritis

The Studied Tissue

Synovial tissue

The Studied Disease

Osteoarthritis [ICD-11:FA20]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Prostaglandin G/H synthase 2 (COX-2)	DTT	PTGS2	3.32E-01	1.67	0.74
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	4.11E-01	5.03E-03	2.97E-02
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	7.34E-03	-2.37E-01	-1.13E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Ketoprofen FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4795).
3	Ketoprofen-induced cyclooxygenase inhibition in renal medulla and platelets of rats treated with caffeine. Pharmacology. 2001;63(4):234-9.
4	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5	Probing the skin permeation of fish oil/EPA and ketoprofen-3. Effects on epidermal COX-2 and LOX. Prostaglandins Leukot Essent Fatty Acids. 2007 Jun;76(6):357-62.
6	Clinical pharmacokinetics of ketoprofen enantiomers in wild type of Cyp 2c8 and Cyp 2c9 patients with rheumatoid arthritis. Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):167-73.
7	Association between the UGT1A1*28 allele and hyperbilirubinemia in HIV-positive patients receiving atazanavir: a meta-analysis. Biosci Rep. 2019 May 2;39(5). pii: BSR20182105.