Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T72065
(Former ID: TTDI01857)
|
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| Target Name |
Voltage-gated sodium channel (Nav)
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
| 2 | Epilepsy/seizure [ICD-11: 8A61-8A6Z] | |||||
| 3 | Ventricular tachyarrhythmia [ICD-11: BC71] | |||||
| BioChemical Class |
Voltage-gated ion channel
|
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 8 Approved Drugs | + | ||||
| 1 | Cenobamate | Drug Info | Approved | Complex partial seizure | [2] | |
| 2 | Eslicarbazepine | Drug Info | Approved | Seizure disorder | [3], [4] | |
| 3 | Flecainide | Drug Info | Approved | Tachyarrhythmias | [5], [6] | |
| 4 | Lacosamide | Drug Info | Approved | Convulsion | [7], [8] | |
| 5 | Procainamide | Drug Info | Approved | Ventricular arrhythmias | [9], [10] | |
| 6 | Propafenone | Drug Info | Approved | Tachyarrhythmias | [11], [12] | |
| 7 | Tetrodotoxin | Drug Info | Approved | Bacterial infection | [13], [14] | |
| 8 | Tocainide | Drug Info | Approved | Ventricular arrhythmias | [15], [16] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Evenamide | Drug Info | Phase 2 | Schizophrenia | [17] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | Barucainide | Drug Info | Terminated | Heart arrhythmia | [18] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Inhibitor | [+] 4 Inhibitor drugs | + | ||||
| 1 | Cenobamate | Drug Info | [19] | |||
| 2 | Eslicarbazepine | Drug Info | [1] | |||
| 3 | Lacosamide | Drug Info | [1] | |||
| 4 | Tetrodotoxin | Drug Info | [1] | |||
| Modulator | [+] 5 Modulator drugs | + | ||||
| 1 | Flecainide | Drug Info | [20] | |||
| 2 | Procainamide | Drug Info | [20] | |||
| 3 | Propafenone | Drug Info | [20] | |||
| 4 | Tocainide | Drug Info | [20] | |||
| 5 | Barucainide | Drug Info | [22] | |||
| Blocker | [+] 1 Blocker drugs | + | ||||
| 1 | Evenamide | Drug Info | [21] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019 | |||||
| REF 3 | 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: 7350). | |||||
| REF 4 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | |||||
| REF 5 | 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). | |||||
| REF 6 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075442. | |||||
| REF 7 | 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: 7472). | |||||
| REF 8 | 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6. | |||||
| REF 9 | 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: 4811). | |||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089257. | |||||
| REF 11 | 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: 2561). | |||||
| REF 12 | New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. | |||||
| REF 13 | 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: 2616). | |||||
| REF 14 | 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. | |||||
| REF 15 | 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: 7309). | |||||
| REF 16 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018257. | |||||
| REF 17 | ClinicalTrials.gov (NCT04461119) Study to Determine the Safety, Tolerability, and Efficacy of Evenamide in Patients With Chronic Schizophrenia. U.S. National Institutes of Health. | |||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000197) | |||||
| REF 19 | Effects of cenobamate (YKP3089), a newly developed anti-epileptic drug, on voltage-gated sodium channels in rat hippocampal CA3 neurons. Eur J Pharmacol. 2019 Jul 15;855:175-182. | |||||
| REF 20 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 21 | Clinical pipeline report, company report or official report of Newron Pharmaceuticals. | |||||
| REF 22 | Barucainide, a novel class Ib antiarrhythmic agent with a slow kinetic property: electrophysiologic observations in isolated canine and rabbit cardiac muscle. Am Heart J. 1990 May;119(5):1050-60. | |||||
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