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

General Information of Drug (ID: DMTZRCW)

• Drug Name: Aryl carboxamide derivative 1 Drug Info
• Synonyms: PMID25539043-Compound-WO2010137351Example37
• Cross-matching ID: TTD Drug ID: DMTZRCW

Molecule-Related Drug Atlas

Drug(s) Targeting Voltage-gated sodium channel alpha Nav1.7 (SCN9A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
XEN-402	DMR69CG	Osteoarthritis	FA00-FA05	Phase 2	[2]
PF-05089771	DMD74BJ	Chronic pain	MG30	Phase 2	[3]
BIIB074	DMLV1ET	Bipolar disorder	6A60	Phase 2	[4]
DSP-2230	DM0WTMD	Neuropathic pain	8E43.0	Phase 1	[4]
BIIB095	DMUC6EP	Pain	MG30-MG3Z	Phase 1	[4]
GDC0310	DMUNFEP	Chronic pain	MG30	Phase 1	[5]
DSP-3905	DMYHU24	Neuropathic pain	8E43.0	Phase 1	[4]
PF-05241328	DM2NTBL	Pain	MG30-MG3Z	Phase 1	[6]
DWJ-208	DMQKDJZ	Cancer related pain	MG30	Phase 1	[4]
RG7893	DM1R4MQ	Pain	MG30-MG3Z	Phase 1	[7]

Drug(s) Targeting Voltage-gated sodium channel alpha Nav1.5 (SCN5A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mephenytoin	DM5UGDK	Epilepsy	8A60-8A68	Approved	[8]
Mexiletine	DMCTE9R	Ventricular tachycardia	BC71	Approved	[9]
Fosphenytoin	DMOX3LB	Epilepsy	8A60-8A68	Approved	[8]
Disopyramide	DM5SYZP	Ventricular arrhythmias	BC71	Approved	[9]
Lomerizine	DME0TC8	Migraine	8A80	Approved	[10]
Tetrodotoxin	DMWMPRG	Bacterial infection	1A00-1C4Z	Approved	[11]
Dyclonine	DMU6OFP	Pain	MG30-MG3Z	Approved	[12]
Moricizine	DMOMBJW	Arrhythmia	BC9Z	Approved	[13]
Ethotoin	DMXWOCP	Complex partial seizure	8A68.0	Approved	[14]
Prilocaine	DMI7DZ2	Pain	MG30-MG3Z	Approved	[12]

Drug(s) Targeting Voltage-gated sodium channel alpha Nav1.3 (SCN3A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lidoflazine	DMV23GL	Angina pectoris	BA40	Approved	[15]
Aryl carboxamide derivative 2	DM146TA	N. A.	N. A.	Patented	[1]
Pyrimidine derivative 1	DMN9VQM	N. A.	N. A.	Patented	[1]
Pyrrolo-pyridinone derivative 6	DMXGNP8	N. A.	N. A.	Patented	[1]
Pyrrolo-pyridinone derivative 5	DMK2FSY	N. A.	N. A.	Patented	[1]
Sipatrigine	DMMQ4GC	Neurological disorder	6B60	Discontinued in Phase 2	[16]
U-92032	DMTYO3P	N. A.	N. A.	Terminated	[17]
PD-85639	DMNUKB4	N. A.	N. A.	Terminated	[15]
Batrachotoxin	DMYH9SU	Discovery agent	N.A.	Investigative	[18]
Veratridine	DMUF8JZ	Discovery agent	N.A.	Investigative	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated sodium channel alpha Nav1.3 (SCN3A)	TTAXZ0K	SCN3A_HUMAN	Inhibitor	[1]
Voltage-gated sodium channel alpha Nav1.5 (SCN5A)	TTZOVE0	SCN5A_HUMAN	Inhibitor	[1]
Voltage-gated sodium channel alpha Nav1.7 (SCN9A)	TT4G2JS	SCN9A_HUMAN	Inhibitor	[1]

References

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• [2] Treatment of Na(v)1.7-mediated pain in inherited erythromelalgia using a novel sodium channel blocker. Pain. 2012 Jan;153(1):80-5.
• [3] Primary erythromelalgia: a review. Orphanet J Rare Dis. 2015 Sep 30;10:127.
• [4] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9.
• [7] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041740)
• [8] Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68.
• [9] Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9.
• [10] Medicinal chemistry of neuronal voltage-gated sodium channel blockers. J Med Chem. 2001 Jan 18;44(2):115-37.
• [11] Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81.
• [12] Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine. Pharmacol Biochem Behav. 1998 Feb;59(2):305-12.
• [13] From first class to third class: recent upheaval in antiarrhythmic therapy--lessons from clinical trials. Am J Cardiol. 1996 Aug 29;78(4A):28-33.
• [14] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [15] Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. J Med Chem. 1994 Jan 21;37(2):268-74.
• [16] Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. J Med Chem. 2002 Aug 15;45(17):3755-64.
• [17] Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a ... J Med Chem. 2000 Sep 7;43(18):3372-6.
• [18] 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: 580).