Details of the Drug Combination

General Information of Drug Combination (ID: DC3Q0DF)

Drug Combination Name
Lorcaserin Varenicline
Indication
Disease Entry Status REF
Obesity Phase 2 [1]
Component Drugs Lorcaserin   DMG6OYJ Varenicline   DMMUOLJ
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Lorcaserin
Disease Entry ICD 11 Status REF
Obesity 5B81 Approved [2]
Drug abuse 6C4G.1Z Phase 1 [2]
Lorcaserin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Agonist [5]
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Lorcaserin Interacts with 6 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [6]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [6]
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Metabolism [6]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [6]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Metabolism [6]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [6]
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⏷ Show the Full List of 6 DME(s)
Indication(s) of Varenicline
Disease Entry ICD 11 Status REF
Drug dependence N.A. Approved [3]
Smoking dependence 6C4A.2 Approved [4]
Varenicline Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2) TTL1ATN ACHA4_HUMAN; ACHB2_HUMAN Modulator [7]
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Varenicline Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Substrate [8]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [9]
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Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Tobacco Use Disorder DCJ8CV6 N. A. Phase 1 [10]
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References

1 ClinicalTrials.gov (NCT02412631) Addressing Post Cessation Weight Gain
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: 2941).
3 Varenicline FDA Label
4 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: 5459).
5 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
6 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.
7 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
8 Effect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: an in vitro-in vivo study. Clin Pharmacol Ther. 2008 Apr;83(4):567-76.
9 Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J Med Chem. 2013 Sep 26;56(18):7232-42.
10 ClinicalTrials.gov (NCT02393547) Lorcaserin for Preventing Weight Gain Among Smokers