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

General Information of Drug (ID: DM3IWS8)

Drug Name

Laquinimod Drug Info

Synonyms

Laquinimod; 248281-84-7; 5-CHLORO-N-ETHYL-4-HYDROXY-1-METHYL-2-OXO-N-PHENYL-1,2-DIHYDROQUINOLINE-3-CARBOXAMIDE; ABR-215062; ABR 215062; 5-Chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid ethyl-phenyl-amide; UNII-908SY76S4G; CIVENTICHEM CV-4057; Laquinimod (ABR-215062); 908SY76S4G; N-Ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide; 5-chloro-n-ethyl-2-hydroxy-1-methyl-4-oxo-n-phenyl-1,4-dihydroquinoline-3-carboxamide; C19H17ClN2O3

Indication

Disease Entry	ICD 11	Status	REF
Lupus	4A40	Phase 3	[1]
Multiple sclerosis	8A40	Phase 3	[2]
Huntington disease	8A01.10	Phase 2	[3]
Primary progressive multiple sclerosis	8A40.1	Phase 2	[2]

Cross-matching ID

PubChem CID: 54677946
ChEBI ID: CHEBI:134738
CAS Number: CAS 248281-84-7
TTD Drug ID: DM3IWS8
INTEDE Drug ID: DR0918

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Nuclear factor NF-kappa-B (NFKB)	TTSXVID	NFKB1_HUMAN; NFKB2_HUMAN; TF65_HUMAN; RELB_HUMAN; REL_HUMAN	Modulator	[4]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Phase 3	[5]

------------------------------------------------------------------------------------

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Nuclear factor NF-kappa-B (NFKB)	DTT	NFKB1	5.38	4.436	4.89	5.698
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

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

Lupus

ICD Disease Classification

4A40

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Nuclear factor NF-kappa-B (NFKB)	DTT	NFKB1; NFKB2; RELA; RELB; REL	5.39E-01	0.16	0.27
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	7.29E-03	-3.47E-02	-1.80E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	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: 7639).
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Reduced astrocytic NF- B activation by laquinimod protects from cuprizone-induced demyelination. Acta Neuropathol. 2012 Sep;124(3):411-24.
5	Oral laquinimod treatment in multiple sclerosis. Neurologia. 2011 Mar;26(2):111-7.