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

General Information of Drug (ID: DMG6OYJ)

Drug Name
Lorcaserin Drug Info
Synonyms APD 356; APD356; AR-10A; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine; 10-chloro-2-methyl-4-azabicyclo[5.4.0]undeca-8,10,12-triene
Indication
Disease Entry ICD 11 Status REF
Obesity 5B81 Approved [1]
Drug abuse 6C4G.1Z Phase 1 [1]
Cross-matching ID
PubChem CID
11658860
ChEBI ID
CHEBI:65353
CAS Number
CAS 616202-92-7
TTD Drug ID
DMG6OYJ
INTEDE Drug ID
DR0979
ACDINA Drug ID
D00376

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Agonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [3]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [3]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [3]
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Approved [3]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [3]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [3]

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 2C receptor (HTR2C) DTT HTR2C 4.233 3.329 3.843 3.888
Cytochrome P450 2A6 (CYP2A6) DME CYP2A6 10.644 6.631 6.598 6.937
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
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 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 Obesity
ICD Disease Classification 5B81
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
5-HT 2C receptor (HTR2C) DTT HTR2C 1.02E-02 -0.45 -0.37
5-HT 2C receptor (HTR2C) DTT HTR2C 2.27E-01 0.27 0.6
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 9.90E-01 3.10E-03 1.75E-02
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 5.35E-01 1.10E-02 1.19E-01
Cytochrome P450 2A6 (CYP2A6) DME CYP2A6 6.24E-01 6.79E-02 2.28E-01
Cytochrome P450 2A6 (CYP2A6) DME CYP2A6 2.82E-01 -4.18E-02 -2.80E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 6.73E-02 6.49E-02 3.07E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 6.45E-01 2.07E-02 1.74E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.39E-01 1.54E-02 4.74E-02
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.64E-02 -8.21E-02 -7.11E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 2.59E-01 6.29E-02 3.14E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 4.84E-01 -8.38E-02 -8.46E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.66E-01 4.25E-02 1.20E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.75E-01 5.15E-02 3.64E-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: 2941).
2 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
3 Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71.