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

General Information of Drug (ID: DM1S4AG)

Drug Name

Lumiracoxib Drug Info

Synonyms

Joicela; Prexige; Novartis brand of lumiracoxib; COX 189; COX189; COX-189; Lumiracoxib [USAN:INN]; Prexige (Novartis); Prexige (TN); Lumiracoxib (USAN/INN); 2-((2-Chloro-6-fluorophenyl)amino)-5-methylbenzeneacetic acid; 2-((2-Chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid; 2-(2-((2-chloro-6-fluoro-phenyl)amino)-5-methyl-phenyl)acetic acid; 2-[2-(2-chloro-6-fluoroanilino)-5-methylphenyl]acetic acid

Indication

Disease Entry	ICD 11	Status	REF
Chronic renal failure	GB61.Z	Approved	[1]
Knee osteoarthritis	FA01	Approved	[2]
Osteoarthritis	FA00-FA05	Approved	[3]

Therapeutic Class

Antiinflammatory Agents

Cross-matching ID

PubChem CID: 151166
ChEBI ID: CHEBI:73044
CAS Number: CAS 220991-20-8
TTD Drug ID: DM1S4AG
VARIDT Drug ID: DR01172
INTEDE Drug ID: DR0993

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	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Phase 4	[5]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Phase 4	[5]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Phase 4	[5]
UDP-glucuronosyltransferase 1A9 (UGT1A9)	DE85D2P	UD19_HUMAN	Phase 4	[6]

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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 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
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

The Studied Disease

Chronic renal failure

ICD Disease Classification

GB61.Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Prostaglandin G/H synthase 2 (COX-2)	DTT	PTGS2	2.03E-07	1.68	3.86
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	2.43E-01	9.13E-02	3.60E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	5.51E-02	1.95E-01	1.20E+00
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	3.04E-01	-5.14E-02	-1.57E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Adverse effects of cyclooxygenase 2 inhibitors on renal and arrhythmia events: meta-analysis of randomized trials. JAMA. 2006 Oct 4;296(13):1619-32.
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: 2897).
3	Lumiracoxib in the management of osteoarthritis and acute pain. Expert Opin Pharmacother. 2007 Jul;8(10):1551-64.
4	Dissociation of airway inflammation and hyperresponsiveness by cyclooxygenase inhibition in allergen challenged mice. Eur Respir J. 2009 Jul;34(1):200-8.
5	Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor. Clin Pharmacokinet. 2005;44(12):1247-66.
6	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.