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

General Information of Drug (ID: DMR0U4V)

Drug Name

XEN-D0103 Drug Info

Synonyms

KCNA voltage-gated potassium channel-5 inhibitor (atrial fibrillation), Xention

Indication

Disease Entry	ICD 11	Status	REF
Atrial fibrillation	BC81.3	Phase 1	[1]

Cross-matching ID

TTD Drug ID: DMR0U4V

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Preclinical Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Voltage-gated potassium channel Kv1.5 (KCNA5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dronedarone	DMA8FS5	Angina pectoris	BA40	Approved	[3]
BMS-919373	DMN28WK	Atrial fibrillation	BC81.3	Phase 2	[4]
IQB-9302	DMET0H4	Pain	MG30-MG3Z	Phase 1	[5]
BMS-394136	DMGDJQR	Arrhythmia	BC9Z	Phase 1	[6]
XEN-D0101	DMU0V45	Atrial fibrillation	BC81.3	Phase 1	[7]
T-226296	DMJ6P9U	Obesity	5B81	Preclinical	[3]
Zatebradine	DMNYKOT	Angina pectoris	BA40	Terminated	[8]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[9]
4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one	DMKMH5L	Discovery agent	N.A.	Investigative	[10]
clofilium	DMQ37OP	Discovery agent	N.A.	Investigative	[11]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated potassium channel Kv1.5 (KCNA5)	TTW0CMT	KCNA5_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT02390258) Fed-Fasted, Single and Multiple Ascending Dose Trial of XEN-D0103. U.S. National Institutes of Health.
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. (Target id: 542).
3	New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
4	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035504)
5	Stereoselective effects of the enantiomers of a new local anaesthetic, IQB-9302, on a human cardiac potassium channel (Kv1.5). Br J Pharmacol. 2001 Jan;132(2):385-92.
6	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
7	Human electrophysiological and pharmacological properties of XEN-D0101: a novel atrial-selective Kv1.5/IKur inhibitor. J Cardiovasc Pharmacol. 2013 May;61(5):408-15.
8	DOI: 10.1161/01.CIR.94.3.562
9	Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. Mol Pharmacol. 1994 Jun;45(6):1227-34.
10	Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92.
11	Mechanism of clofilium block of the human Kv1.5 delayed rectifier potassium channel. Mol Pharmacol. 1995 Jan;47(1):198-205.