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

General Information of Drug (ID: DMGX5Q0)

Drug Name

Gepirone Drug Info

Synonyms

83928-76-1; 4,4-Dimethyl-1-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)piperidine-2,6-dione; Gepironum [Latin]; Gepirone [INN]; Gepirona [Spanish]; UNII-JW5Y7B8Z18; BMY-13805; JW5Y7B8Z18; CHEMBL284092; Gepironum; AK115965; Gepirona; Travivo; 2,6-Piperidinedione, 4,4-dimethyl-1-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-; BMY 13805; gepiron ER; MJ 13805-1; ORG-13011(Gepirone); AC1L1IK6; AC1Q6F8Q; 4,4-dimethyl-1-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-2,6-piperidinedione; 3,3-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]glutarimide; 4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione

Indication

Disease Entry	ICD 11	Status	REF
Major depressive disorder	6A70.3	Approved	[1]
Depression	6A70-6A7Z	Terminated	[2]

Cross-matching ID

PubChem CID: 55191
ChEBI ID: CHEBI:135990
CAS Number: CAS 83928-76-1
TTD Drug ID: DMGX5Q0
INTEDE Drug ID: DR0769

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	Agonist	[2]

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

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Phase 2	[3]

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

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 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Phase 2	[4]

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

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
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
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

Major depressive disorder

ICD Disease Classification

6A70.3

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
5-HT 1A receptor (HTR1A)	DTT	HTR1A	2.18E-01	-0.11	-0.51
P-glycoprotein 1 (ABCB1)	DTP	P-GP	1.08E-01	-2.87E-01	-5.57E-01
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.05E-01	1.60E-01	1.37E+00
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.40E-01	1.04E-01	7.11E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	7.43E-01	2.19E-03	1.72E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	3.18E-03	2.30E-01	2.71E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	8.32E-01	4.74E-02	1.73E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 021164
2	Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
3	Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
4	Metabolism of the newest antidepressants: comparisons with related predecessors. IDrugs. 2004 Feb;7(2):143-50.