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

General Information of Drug (ID: DM4V8WF)

Drug Name

Cenicriviroc Drug Info

Synonyms

Cenicriviroc; 497223-25-3; TBR-652; TAK-652; Cenicriviroc mesylate; UNII-15C116UA4Y; TAK652; 15C116UA4Y; TBR652; Cenicriviroc (USAN/INN); SCHEMBL3157768; SCHEMBL3157748; CHEMBL2110727; MolPort-044-723-655; MolPort-044-649-359; EX-A1608; BDBM50422828; AKOS027250788; CS-6148; DB11758; SB16976; HY-14882; AS-35184; D09878; UNII-15C116UA4Y component PNDKCRDVVKJPKG-WHERJAGFSA-N; 1-Benzazocine-5-carboxamide, 8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-N-[4-[[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-, (5E)-

Indication

Disease Entry	ICD 11	Status	REF
Human immunodeficiency virus infection	1C62	Phase 2	[1]
Human immunodeficiency virus-1 infection	1C62	Phase 2	[2]

Cross-matching ID

PubChem CID: 11285792
ChEBI ID: CHEBI:149636
CAS Number: CAS 497223-25-3
TTD Drug ID: DM4V8WF
INTEDE Drug ID: DR1848

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
C-C chemokine receptor type 2 (CCR2)	TTFZYTO	CCR2_HUMAN	Antagonist	[2]
C-C chemokine receptor type 5 (CCR5)	TT2CEJG	CCR5_HUMAN	Modulator	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Phase 2	[4]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Phase 2	[4]

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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 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
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

Human immunodeficiency virus infection

ICD Disease Classification

1C62

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.78E-01	-3.38E-03	-5.71E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	9.85E-01	2.24E-02	7.33E-02

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: 801).
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	The dual CCR5 and CCR2 inhibitor cenicriviroc does not redistribute HIV into extracellular space: implications for plasma viral load and intracellular DNA decline. J Antimicrob Chemother. 2015 Mar;70(3):750-6.
4	Pharmacokinetics, safety, and CCR2/CCR5 antagonist activity of cenicriviroc in participants with mild or moderate hepatic impairment. Clin Transl Sci. 2016 Jun;9(3):139-48.