Details of the Drug Combination

General Information of Drug Combination (ID: DCHD8AX)

Drug Combination Name
Flecainide Pilsicainide
Indication
Disease Entry Status REF
Paroxysmal Atrial Fibrillation Phase 1 [1]
Component Drugs Flecainide   DMSQDLE Pilsicainide   DMZ65K8
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 Flecainide
Disease Entry ICD 11 Status REF
Tachyarrhythmias BC71 Approved [2]
Paroxysmal atrial fibrillation BC81.30 Phase 1 [3]
Atrial fibrillation BC81.3 Investigative [4]
Flecainide Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
E3 ubiquitin-protein ligase COP1 (RFWD2) TT05DLS COP1_HUMAN Modulator [7]
Voltage-gated sodium channel alpha Nav1.9 (SCN11A) TTN9VTF SCNBA_HUMAN Blocker [4]
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Flecainide Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [8]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [8]
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Flecainide Interacts with 14 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Sodium channel protein type 5 subunit alpha (SCN5A) OTGYZWR6 SCN5A_HUMAN Affects Response To Substance [9]
Nuclear protein 1 (NUPR1) OT4FU8C0 NUPR1_HUMAN Increases Expression [6]
Alpha-1-antichymotrypsin (SERPINA3) OT9BP2S0 AACT_HUMAN Increases Expression [6]
Solute carrier family 2, facilitated glucose transporter member 3 (SLC2A3) OT2HZK5M GTR3_HUMAN Decreases Expression [6]
Inhibin beta E chain (INHBE) OTOI2NYG INHBE_HUMAN Increases Expression [6]
Acid ceramidase (ASAH1) OT1DNGXL ASAH1_HUMAN Increases Expression [6]
Lysophospholipase D GDPD3 (GDPD3) OTOHM9QM GDPD3_HUMAN Increases Expression [6]
Protein DEPP1 (DEPP1) OTB36PHJ DEPP1_HUMAN Increases Expression [6]
AP-1 complex subunit sigma-1A (AP1S1) OTQ2H8DN AP1S1_HUMAN Decreases Expression [10]
Nuclear receptor subfamily 0 group B member 2 (NR0B2) OT7UVICX NR0B2_HUMAN Increases Expression [10]
Fibronectin type III domain-containing protein 4 (FNDC4) OTOQK0WK FNDC4_HUMAN Decreases Expression [10]
Protein c-Fos (FOS) OTJBUVWS FOS_HUMAN Increases Expression [11]
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (HCN4) OTPH3RRX HCN4_HUMAN Decreases Activity [12]
Potassium voltage-gated channel subfamily E member 1 (KCNE1) OTZNQUW9 KCNE1_HUMAN Increases ADR [13]
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⏷ Show the Full List of 14 DOT(s)
Indication(s) of Pilsicainide
Disease Entry ICD 11 Status REF
Heart arrhythmia BC65 Approved [5]
Pilsicainide Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Sodium channel unspecific (NaC) TTRK8B9 NOUNIPROTAC Modulator [14]
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Pilsicainide Interacts with 1 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [15]
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References

1 ClinicalTrials.gov (NCT01775891) Efficacy of Pilsicainide After Radiofrequency Ablation of Paroxysmal Atrial Fibrillation
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: 2560).
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
6 A toxicogenomic approach to drug-induced phospholipidosis: analysis of its induction mechanism and establishment of a novel in vitro screening system. Toxicol Sci. 2005 Feb;83(2):282-92.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 Flecainide: current status and perspectives in arrhythmia management. World J Cardiol. 2015 Feb 26;7(2):76-85.
9 Flecainide test in Brugada syndrome: a reproducible but risky tool. Pacing Clin Electrophysiol. 2003 Jan;26(1P2):338-41. doi: 10.1046/j.1460-9592.2003.00045.x.
10 Determination of phospholipidosis potential based on gene expression analysis in HepG2 cells. Toxicol Sci. 2007 Mar;96(1):101-14.
11 Selection of drugs to test the specificity of the Tg.AC assay by screening for induction of the gadd153 promoter in vitro. Toxicol Sci. 2003 Aug;74(2):260-70. doi: 10.1093/toxsci/kfg113. Epub 2003 May 2.
12 Effects of antiarrhythmic drugs on the hyperpolarization-activated cyclic nucleotide-gated channel current. J Pharmacol Sci. 2009 Jun;110(2):150-9. doi: 10.1254/jphs.08312fp. Epub 2009 Jun 5.
13 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
14 A sodium channel blocker, pilsicainide, produces atrial post-repolarization refractoriness through the reduction of sodium channel availability. Tohoku J Exp Med. 2011;225(1):35-42.
15 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.