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

General Information of Drug (ID: DMV26S8)

Drug Name

Levomilnacipran Drug Info

Synonyms

Fetzima; UNII-UGM0326TXX; Levomilnacipran HCl; 96847-54-0; UGM0326TXX; CHEMBL99946; F-2695; (1S,2R)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide; (1S,2R)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide; Levomilnacipran [USAN:INN]; Milnacipram; AC1OCEN8; F 2695; Levomilnacipran (USAN/INN); ZINC506; SCHEMBL1414867; GTPL7435; GJJFMKBJSRMPLA-DZGCQCFKSA-N; CHEBI:136040; BDBM50032379; SB17447; DB08918; f2-695; D10072

Indication

Disease Entry	ICD 11	Status	REF
Fibromyalgia	MG30.01	Approved	[1]
Major depressive disorder	6A70.3	Approved	[2]

Cross-matching ID

PubChem CID: 6917779
ChEBI ID: CHEBI:136040
CAS Number: CAS 96847-54-0
TTD Drug ID: DMV26S8
VARIDT Drug ID: DR00049
INTEDE Drug ID: DR0945
ACDINA Drug ID: D00362

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Norepinephrine transporter (NET)	TTAWNKZ	SC6A2_HUMAN	Modulator	[3]
Serotonin transporter (SERT)	TT3ROYC	SC6A4_HUMAN	Modulator	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[5]
Cytochrome P450 2J2 (CYP2J2)	DERSX5P	CP2J2_HUMAN	Approved	[]

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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
Norepinephrine transporter (NET)	DTT	SLC6A2	2.459	3.426	3.322	3.35
Serotonin transporter (SERT)	DTT	SLC6A4	6.278	5.469	6.075	6.966
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

ICD Disease Classification

06 Mental, behavioural or neurodevelopmental disorder

Disease Class

ICD-11: 6A20 Schizophrenia

The Studied Tissue

Pre-frontal cortex

The Studied Disease

Major depressive disorder [ICD-11:6A20]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Norepinephrine transporter (NET)	DTT	SLC6A2	7.05E-01	7.02E-03	0.07
Serotonin transporter (SERT)	DTT	SLC6A4	1.17E-01	0.07	0.59
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.83E-01	4.69E-02	1.89E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	3.17E-01	-6.95E-02	-2.88E-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: 7435).
2	Levomilnacipran FDA Label
3	Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
4	P-glycoprotein differentially affects escitalopram, levomilnacipran, vilazodone and vortioxetine transport at the mouse blood-brain barrier inivo. Neuropharmacology. 2016 Apr;103:104-11.
5	The role of levomilnacipran in the management of major depressive disorder: a comprehensive review. Curr Neuropharmacol. 2016;14(2):191-9.