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

General Information of Drug (ID: DMH7IPW)

Drug Name

Sarizotan Drug Info

Synonyms

Sarizotan [INN]; EMD 128130; N-((3,4-Dihydro-2H-1-benzopyran-2-yl)methyl)-5-(4-fluorophenyl)-3-pyridinemethanamine; (-)-3-((((R)-2-Chromanylmethyl)amino)methyl)-5-(p-fluorophenyl)pyridine; 1-(3,4-dihydro-2H-chromen-2-yl)-N-[[5-(4-fluorophenyl)pyridin-3-yl]methyl]methanamine

Indication

Disease Entry	ICD 11	Status	REF
Rett syndrome	LD90.4	Phase 2/3	[1]
Parkinson disease	8A00.0	Discontinued in Phase 2	[2]

Cross-matching ID

PubChem CID: 6918388
CAS Number: CAS 351862-32-3
TTD Drug ID: DMH7IPW
INTEDE Drug ID: DR1872

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 1A receptor (HTR1A)	TTSQIFT	5HT1A_HUMAN	Modulator	[3]
Dopamine D2 receptor (D2R)	TTEX248	DRD2_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 2/3	[4]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Phase 2/3	[4]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Phase 2/3	[4]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Phase 2/3	[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
5-HT 1A receptor (HTR1A)	DTT	HTR1A	4.661	5.289	3.053	3.472
Dopamine D2 receptor (D2R)	DTT	DRD2	5.345	5.634	5.789	5.901
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
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

Rett syndrome

ICD Disease Classification

LD90.4

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
5-HT 1A receptor (HTR1A)	DTT	HTR1A	1.49E-05	-0.22	-0.58
Dopamine D2 receptor (D2R)	DTT	DRD2	2.50E-02	-0.08	-0.49
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	1.82E-04	-1.35E-01	-5.84E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	7.36E-01	1.62E-02	1.08E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.90E-01	-9.81E-03	-5.96E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.04E-02	6.29E-02	3.54E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
3	Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.Curr Med Chem.2014;21(4):437-57.
4	In vitro characterization of sarizotan metabolism: hepatic clearance, identification and characterization of metabolites, drug-metabolizing enzyme identification, and evaluation of cytochrome p450 inhibition. Drug Metab Dispos. 2010 Jun;38(6):905-16.