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

General Information of Drug (ID: DMR6QH0)

Drug Name
Venlafaxine Drug Info
Synonyms
Efectin; Elafax; Venlafaxina; VenlafaxineXR; Venlafaxinum; Venlafaxine ER; Wy 45030; Efectin (TN); Venlafaxina [INN-Spanish];Venlafaxine (Effexor); Venlafaxine (INN); Venlafaxine [BAN:INN]; Venlafaxine [INN:BAN]; Venlafaxinum [INN-Latin]; N,N-dimethyl-2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethylamine; 1-[(1R)-2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol; 1-[2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol; 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol; 1-[2-dimethylamino-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol; 1-{2-(dimethylamino)-1-[4-(methyloxy)phenyl]ethyl}cyclohexanol
Indication
Disease Entry ICD 11 Status REF
Anxiety disorder 6B00-6B0Z Approved [1]
Depression 6A70-6A7Z Approved [2]
Major depressive disorder 6A70.3 Approved [1]
Panic disorder 6B01 Approved [1]
Therapeutic Class
Antidepressants
Cross-matching ID
PubChem CID
5656
ChEBI ID
CHEBI:9943
CAS Number
CAS 93413-69-5
TTD Drug ID
DMR6QH0
VARIDT Drug ID
DR00450
INTEDE Drug ID
DR1679
ACDINA Drug ID
D00725

Molecule(s) Related to This Drug


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

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [5]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [6]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [6]

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
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
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

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
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.66E-01 9.19E-03 4.88E-02
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 5.64E-01 2.36E-02 1.75E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 7.83E-01 2.32E-03 1.53E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 6.06E-01 -2.42E-02 -1.64E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Venlafaxine FDA Label
2 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: 7321).
3 Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92.
4 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
5 The associations between CYP2D6 metabolizer status and pharmacokinetics and clinical outcomes of venlafaxine: a systematic review and meta-analysis. Pharmacopsychiatry. 2019 Sep;52(5):222-231.
6 O- and N-demethylation of venlafaxine in vitro by human liver microsomes and by microsomes from cDNA-transfected cells: effect of metabolic inhibitors and SSRI antidepressants. Neuropsychopharmacology. 1999 May;20(5):480-90.