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

General Information of Drug (ID: DM0NZDT)

Drug Name

PACTIMIBE Drug Info

Synonyms

Pactimibe; 189198-30-9; UNII-D874R9PZ9T; D874R9PZ9T; CHEMBL478858; Pactimibe [INN:BAN]; [7-(2,2-Dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl]acetic acid; (7-(2,2-Dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid; AC1MIXTD; SCHEMBL282098; CTK0H7032; DTXSID80172315; TXIIZHHIOHVWJD-UHFFFAOYSA-N; ZINC1545445; BDBM50263192; DB12971; 2-[7-(2,2-Dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo L-5-yl]acetic acid; AN-30445; 198P309

Indication

Disease Entry	ICD 11	Status	REF
Arteriosclerosis	BD40	Phase 2/3	[1]

Cross-matching ID

PubChem CID: 3081927
CAS Number: CAS 189198-30-9
TTD Drug ID: DM0NZDT
INTEDE Drug ID: DR1871

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Liver carboxylesterase (CES1)	TTMF541	EST1_HUMAN	Inhibitor	[2]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Phase 2/3	[3]

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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
Liver carboxylesterase (CES1)	DTT	CES1	12.04	6.525	5.311	5.909
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327

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

Arteriosclerosis

ICD Disease Classification

BD40

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Liver carboxylesterase (CES1)	DTT	CES1	3.82E-08	1.86	1.9
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	5.05E-04	-1.51E-01	-8.87E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	ClinicalTrials.gov (NCT00151788) Efficacy and Safety of the ACAT Inhibitor CS-505 (Pactimibe) for Reducing the Progression of Carotid Artery Disease. This Study is Also Known as CAPTIVATE.. U.S. National Institutes of Health.
2	Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and b... J Med Chem. 2008 Aug 14;51(15):4823-33.
3	Novel binding mode of the acidic CYP2D6 substrates pactimibe and its metabolite R-125528. Drug Metab Dispos. 2008 Sep;36(9):1938-43.