Publications (Archive)
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Jump to publications related to:
- Azetukalner (XEN1101)
- NBI-921352 (XEN901) & Nav1.6, Nav1.2/1.6 Inhibitors (partnered with Neurocrine Biosciences, Inc.)
- Other selected Xenon publications
Azetukalner (XEN1101)
Company Poster. “Long-Term Safety and Efficacy of Azetukalner, a Novel, Potent Kv7 Potassium Channel Opener in Adults With Focal Epilepsy: Update From the Ongoing 7-Year Open-Label Extension of X-TOLE” 2024 Annual Meeting of the American Epilepsy Society (AES). December 6-10, 2024
Company Poster. “Is the Mental Health Burden of Epilepsy Under-Recognized in Patients Reporting Focal Onset Seizures? A Patient-Reported Outcomes Study” 2024 Annual Meeting of the American Epilepsy Society (AES). December 6-10, 2024
Company Poster. “A Targeted Literature Review of Comorbidity Burden in Focal Onset Seizures” 2024 Annual Meeting of the American Epilepsy Society (AES). December 6-10, 2024
Company Poster. “Efficacy and Safety of Azetukalner, a Novel, Potent KV7 Potassium Channel Opener in Adults With Moderate to Severe Major Depressive Disorder: Results From the Proof-of-Concept Phase 2 X-NOVA Study” Psych Congress. October 31, 2024
Company Poster. “Azetukalner (XEN1101), a Novel, Potent Kv7 Potassium Channel Opener: Interim Data From an Ongoing, Long‑Term, Open‑Label Extension of a Phase 2b Study (X‑TOLE) in Adults With Focal Onset Seizures.” European Epilepsy Congress. September 7–11, 2024
Company Poster. “Long-term, Quality of Life in Epilepsy Inventory-31 (QOLIE-31) Improvements in Adults With Focal Onset Seizures Treated With Azetukalner (XEN1101) in an Ongoing, Open-Label Extension of a Phase 2b study (X-TOLE).” European Epilepsy Congress. September 7–11, 2024
Company Poster. “Non-seizure Symptoms, Mental Health Comorbidities, and Quality of Life in Patients Reporting Focal Onset Seizures.” European Epilepsy Congress. September 7–11, 2024
Company Poster. “Efficacy and Safety of Azetukalner (XEN1101), a Novel, Kv7 Potassium Channel Opener in Adults With Moderate to Severe Major Depressive Disorder: Results From the Phase 2, Proof-of-Concept X-NOVA Study.” American Society of Clinical Psychopharmacology (ASCP) Annual Meeting. May 28-31, 2024
Oral Presentation. “Interim, Long-term, Safety and Efficacy of XEN1101, a Potent, Selective Potassium Channel Opener: Update from an Ongoing Open-label Extension of a Phase 2b Study (X-TOLE) in Adults with Focal Epilepsy.” American Academy of Neurology Annual Meeting (AAN). April 13–18, 2024
Oral Presentation. “The Impact of Disease Severity on Responder Rates in a Phase 2b Study of XEN1101, a Potent, Selective Potassium Channel Opener, in Adults With Focal Epilepsy (X-TOLE).” American Academy of Neurology Annual Meeting (AAN). April 13–18, 2024
Company Poster. “Interim Long-Term Safety and Efficacy of XEN1101, a Potent, Selective Potassium Channel Opener: Update From an Ongoing, Open-Label Extension of a Phase 2b Study (X-TOLE) in Adults With Focal Epilepsy.” 2023 Annual Meeting of the American Epilepsy Society (AES). December 1-5, 2023
Company Poster. “Long-Term Quality-of-Life Improvements in Adults With Focal Onset Seizures Treated With XEN1101 in an Ongoing Open-Label Extension of a Phase 2b Study (X-TOLE).” 2023 Annual Meeting of the American Epilepsy Society (AES). December 1-5, 2023
Company Poster. “The Impact of Disease Severity on Responder Rates in a Phase 2b Study of XEN1101, a Potent, Selective Potassium Channel Opener, in Adults With Focal Epilepsy (X-TOLE).” 2023 Annual Meeting of the American Epilepsy Society (AES). December 1-5, 2023
Peer-Reviewed Journal Article in JAMA Neurology. French JA, Porter RJ, Perucca E, et al. Efficacy and Safety of XEN1101, a Novel Potassium Channel Opener, in Adults With Focal Epilepsy: A Phase 2b Randomized Clinical Trial. JAMA Neurol. Published online October 09, 2023.
Company Poster. “Quality-of-Life Improvements in Adults With Focal Onset Seizures Treated With XEN1101 in an Ongoing, Long-Term, Open-Label Extension of a Phase 2b Study (X-TOLE).” International Epilepsy Congress (IEC). September 2–6, 2023
Company Poster. “XEN1101, a Novel Potassium Channel Modulator: Interim Data From an Ongoing, Long-Term, Open-Label Extension of a Phase 2B Study (X-TOLE) in Adults With Focal Epilepsy.” International Epilepsy Congress (IEC). September 2–6, 2023
Company Oral Presentation. “Design of Two Parallel Randomized, Double-Blind, Placebo-Controlled Phase 3 Studies to Evaluate the Safety and Efficacy of XEN1101 as Adjunctive Therapy in the Treatment of Focal Onset Epilepsy.” International Epilepsy Congress (IEC). September 2–6, 2023
Company Oral Presentation. “A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Study to Evaluate the Safety and Efficacy of XEN1101 as an Adjunctive Therapy in the Treatment of Primary Generalized Tonic-Clonic Seizures.” International Epilepsy Congress (IEC). September 2–6, 2023
Company Oral Presentation. “XEN1101, a Novel Potassium Channel Modulator: Interim Data From an Ongoing, Long-Term, Open-Label Extension of a Phase 2b Study (X-TOLE) in Adults With Focal Epilepsy.” American Academy of Neurology Annual Meeting (AAN). April 22–27, 2023
Company Poster. “A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Study to Evaluate the Safety and Efficacy of XEN1101 as an Adjunctive Therapy in the Treatment of Primary Generalized Tonic-Clonic Seizures.” American Academy of Neurology Annual Meeting (AAN). April 22–27, 2023
Company Poster. “Design of two parallel randomized, double-blind, placebo-controlled phase 3 studies to evaluate the safety and efficacy of XEN1101 as adjunctive therapy in the treatment of focal onset epilepsy.” American Society for Experimental Neurotherapeutics Annual Meeting (ASENT 2023). March 13-15, 2023
Company Poster. “A randomized, double-blind, placebo-controlled, phase 3 study to evaluate the safety and efficacy of XEN1101 as an adjunctive therapy in the treatment of primary generalized tonic-clonic seizures.” American Society for Experimental Neurotherapeutics Annual Meeting (ASENT 2023). March 13-15, 2023
Company Poster. “XEN1101, a novel potassium channel modulator: interim data from an ongoing, long-term, open-label extension of a phase 2b study (X-TOLE) in adults with focal epilepsy.” American Society for Experimental Neurotherapeutics Annual Meeting (ASENT 2023). March 13-15, 2023
Company Poster. “XEN1101, a Novel Potassium Channel Modulator: Interim Data From an Ongoing, Long-Term, Open-Label Extension of a Phase 2B Study (X-TOLE) in Adults With Focal Epilepsy.” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Company Poster. “The Impact of Disease Severity on Efficacy From a Phase 2b Study of XEN1101, a Novel Potassium Channel Opener, in Adults With Focal Epilepsy (X-TOLE).” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Company Poster. “Rapid Onset of Efficacy of XEN1101, a Novel Potassium Channel Opener, in
Adults with Focal Epilepsy: Results from a Phase 2b Study (X-TOLE).” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Xenon Scientific Exhibit Poster. “Phase 2b Efficacy and Safety of XEN1101, a Novel Potassium Channel
Modulator, in Adults with Focal Epilepsy (X-TOLE).” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Xenon Scientific Exhibit Poster. “Design of X-TOLE2 and X-TOLE3: Two Parallel, Randomized, Double-Blind,
Placebo-Controlled Phase 3 Studies to Evaluate the Safety and Efficacy of XEN1101 as Adjunctive
Therapy in the Treatment of Focal Onset Epilepsy.” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Xenon Scientific Exhibit Poster. “X-ACKT: A Randomized, Double-Blind, Placebo-Controlled Phase 3 Study
to Evaluate the Safety and Efficacy of XEN1101 as an Adjunctive Therapy in the Treatment of
Primary Generalized Tonic-Clonic Seizures.” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Xenon Scientific Exhibit Poster. “A Novel Molecular Mechanism for the Treatment of Major Depressive
Disorder: A Phase 2, Proof-of-Concept Study of the Potassium Channel Opener XEN1101 in Subjects
With Major Depressive Disorder.” 2022 Annual Meeting of the American Epilepsy Society (AES). December 4, 2022
Company Presentation. “Overview: Novel Kv7 Mechanism of Action for Depression.” 5th Neuropsychiatric
and Psychedelic Drug Development Summit. October 31, 2022
Company Poster. “Rapid Onset of Efficacy of XEN1101, a Novel Potassium Channel Opener, in Adults with Focal Epilepsy: Results from a Phase 2b Study (X-TOLE).” 14th European Epilepsy Congress. July 9-13, 2022
Company Poster. “The Impact of Disease Severity on Efficacy from a Phase 2b Study of XEN1101, a Novel Potassium Channel Opener, in Adults with Focal Epilepsy (X-TOLE).” 14th European Epilepsy Congress. July 9-13, 2022
Company Poster. “Phase 2b Efficacy and Safety of XEN1101, a Novel Potassium Channel Opener, in Adults With Focal Onset Seizures (X-TOLE).” 14th European Epilepsy Congress. July 9-13, 2022
Company Poster. “A novel molecular mechanism for the treatment of major depressive disorder: a phase 2, proof-of-concept study of the potassium channel opener XEN1101 in subjects with moderate to severe MDD.” APA 2022 (American Psychiatric Association Annual Meeting). May 21-25, 2022
Company Presentation. “An Overview of XEN1101 and XEN496.” EILAT XVI Conference:
New Antiepileptic Drugs and Devices. May 23, 2022
Company Poster. “Phase 2b Efficacy and Safety of XEN1101, a Novel Potassium Channel Modulator, In Adults With Focal Epilepsy (X-TOLE).” AAN 2022 (Annual Meeting of the American Academy of Neurology). Encore Poster from ASENT 2022.
Company Poster. “Phase 2b Efficacy and Safety of XEN1101, a Novel Potassium Channel Modulator, In Adults With Focal Epilepsy (X-TOLE).” ASENT 2022 (virtual meeting of the American Society for Experimental Neurotherapeutics).
Company Poster. “The Impact of Disease Severity on Efficacy from a Phase 2b Study of XEN1101, a Novel Potassium Channel Opener, in Adults with Focal Epilepsy (X-TOLE).” ASENT 2022 (virtual meeting of the American Society for Experimental Neurotherapeutics).
Company Poster. “Phase 2b Efficacy and Safety of XEN1101, a Novel Potassium Channel Modulator, In Adults With Focal Epilepsy (X-TOLE).” 2021 Annual Meeting of the American Epilepsy Society (AES). December 4, 2021
Company Poster. “Electronic Seizure Diary Compliance In An Adult Focal Epilepsy Clinical Trial.” 2021 Annual Meeting of the American Epilepsy Society (AES). December 5, 2021
Company Symposium. “The Unmet Need in Epilepsy: The Therapeutic Potential of Potassium Channel Modulators.” 2021 Annual Meeting of the American Epilepsy Society (AES). December 3, 2021
Company Poster. “XEN1101, a Differentiated Kv7 Potassium Channel Modulator, Impacts Depression and Anhedonia.” 2021 Annual Meeting of the American Epilepsy Society (AES). December 5, 2021
Company Presentation. ASENT 2021 (Virtual meeting of the American Society for Experimental Neurotherapeutics): “Addressing an Unmet Medical Need in Adult Focal Epilepsy with XEN1101, a Novel KV7 Modulator.” February 22-25, 2021
Company Presentation. ASENT 2021 (Virtual meeting of the American Society for Experimental Neurotherapeutics): “Depression and Anhedonia: Acute Preclinical Efficacy for XEN1101, a Differentiated KV7 Potassium Channel Modulator.” February 22-25, 2021
Company Presentation. ASENT 2021 (Virtual meeting of the American Society for Experimental Neurotherapeutics): “Anticonvulsant Effects of the Differentiated KV7 Channel Potentiator XEN1101 in Combination with Commonly Used Anti-Seizure Drugs.” February 22-25, 2021
Company Presentation. ASENT 2021 (Virtual meeting of the American Society for Experimental Neurotherapeutics): “KV7 Modulators in Epilepsy and Depression.” February 22-25, 2021
Company Poster. Virtual 2020 American Epilepsy Society (AES) Annual Meeting: “Pre-clinical In Vitro and In Vivo Comparison of the Kv7 Activator XEN1101 with Ezogabine.” December 4-8, 2020
Company Presentation. 2020 Epilepsy Pipeline Conference: “KV7 Potassium Channel Modulators for the Treatment of Epilepsy.” (Includes overview of both XEN1101 and XEN496.) August 27, 2020
Company Presentation. Eilat XV Conference: “New Anti-Epileptic Drugs and Devices.” (Includes overview of both XEN1101 and XEN496.) July 28, 2020
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting: “Use of Transcranial Magnetic Stimulation Data in the Design of a Dose Ranging Finding Efficacy, Safety, Tolerability and Pharmacokinetics Study of XEN1101 in Patients with Focal Epilepsy.” December 6-10, 2019
Company Poster. 2018 American Epilepsy Society (AES) Annual Meeting: “A First-in-Human Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Pharmacodynamics of a Novel Small Molecule KV7.2/7.3 Positive Allosteric Modulator (XEN1101) in Healthy Subjects.” December 3, 2018
Company Poster. 2018 American Epilepsy Society (AES) Annual Meeting: “A Phase 1 Study Utilizing Transcranial Magnetic Stimulation to Assess the Pharmacodynamic Effects of a Novel Potassium Channel Opener (XEN1101) on Human Cortical Excitability.” December 3, 2018
King’s College London Presentation. 13th European Congress on Epileptology: “A First-in-Human Phase I Study to Assess the Pharmacodynamic Profile of a Novel Potassium Channel Opener (XEN1101) on Human Cortical Excitability with TMS-EEG and TMS-EMG.” August 29, 2018
Company Presentation. Eilat XIV Meeting: “XEN1101: A Novel, Next- Generation KCNQ2 Modulator for the Treatment of Epilepsy.” May 15, 2018
Company Presentation. Epilepsy Foundation Pipeline Conference: “XEN1101, a Novel Modulator of Kv7.2/3 for the Treatment of Epilepsy.” February 22-23, 2018
NBI-921352 (XEN901): Partnered Program with Neurocrine Biosciences
Includes Selective Nav1.6 and Dual Nav1.2/1.6 Inhibitors
Company Poster. Virtual 2020 American Epilepsy Society (AES) Annual Meeting: “An Online Survey of Caregivers for Patients with SCN8A Developmental and Epileptic Encephalopathy (SCN8A-DEE) or SCN8A-Related Epilepsy.” December 4-8, 2020
Company Poster. Virtual 2020 American Epilepsy Society (AES) Annual Meeting: “Potential Drug-Drug Interactions Between NBI-921352/XEN901 (a Novel Nav1.6 Selective Sodium Channel Blocker) and a Strong Inducer of CYP3A4 (Phenytoin) in Healthy Volunteers.” December 4-8, 2020
Company Poster. Virtual 2020 American Epilepsy Society (AES) Annual Meeting: “Pharmacokinetics, Food Effect, and Relative Bioavailability of Two Formulations of NBI-921352/XEN901 (Novel Nav1.6-Selective Sodium Channel Blocker) in Healthy Adults: Pediatric Granules and Adult Tablets.” December 4-8, 2020
Company Poster. 2020 American Academy of Neurology (AAN) Meeting: “Relative Bioavailability, Pharmacokinetic and Food Effect Assessment of Two Immediate-Release Formulations of the NaV1.6-Selective Sodium Channel Blocker NBI-921352/XEN901: Pediatric Granules and Adult Tablets.” May 2020
Company Poster. 2020 American Academy of Neurology (AAN) Meeting: “Assessment of Potential Pharmacokinetic and Pharmacodynamic Interactions between NBI-921352/XEN901, a Novel NaV1.6-Selective Sodium Channel Blocker, and Phenytoin (a Non-selective NaV Blocker) in Adult Healthy Subjects.” May 2020
Company Poster. 2020 American Academy of Neurology (AAN) Meeting: “An Online Survey of Caregivers of Patients with SCN8A-Related Epilepsy.” May 2020
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting–Genetic Epilepsies Scientific Exhibit: “A Phase 1 Study in Healthy Subjects to Assess the Safety, Tolerability and Pharmacokinetics of XEN901, a Novel, Selective Nav1.6 Sodium Channel Inhibitor for the Treatment of SCN8A-Related Epilepsy.” December 8, 2019
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting–Genetic Epilepsies Scientific Exhibit: “An Online Survey of Caregivers of Patients with SCN8A-Related Epilepsy.” December 8, 2019
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting: “XEN393, A Novel Selective Dual Inhibitor of Nav1.2/Nav1.6 Channels Prevents Electrically-Induced Seizures in Mice and Rats.” December 6-10, 2019
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting: “Nav1.6 Selective and Nav1.2/Nav1.6 Dual Inhibitors Reduce Action Potential Firing in Mouse Cortical Pyramidal Neurons While Sparing Inhibitory Interneuron Firing.” December 6-10, 2019
Company Poster. 2018 American Epilepsy Society (AES) Annual Meeting: “A First in Human Phase 1 Study to Assess the Safety, Tolerability and Pharmacokinetics of a Novel NaV1.6 Selective Small Molecule Sodium Channel Inhibitor (XEN901) in Healthy Subjects.” December 3, 2018
Company Poster. 2018 American Epilepsy Society (AES) Annual Meeting: “Repeat Dosing of Novel Selective Inhibitors of NaV1.6 Enhances Efficacy in the Mouse Maximal Electroshock Model.” December 3, 2018
Company Poster. 2018 American Epilepsy Society (AES) Annual Meeting: “Efficacy of Sodium Channel Inhibitors as Anticonvulsants in the Rat MES Assay is
Predictive of the Therapeutic Plasma Concentration in Humans.” December 3, 2018
Company Poster. 2018 American Epilepsy Society (AES) Annual Meeting: “Preclinical Safety Margins of the Potent and NaV1.6 Selective Inhibitor, XEN901, in Relation to Non-Selective Sodium Channel Blockers.” December 3, 2018
Company Presentation. Eilat XIV Meeting: “XEN901: A Novel, Highly Selective NaV1.6 Inhibitor for the Treatment of Epilepsy.” May 15, 2018
Company Poster. American Epilepsy Society Meeting: “Selective Inhibitors Suggest NaV1.6 Activity Is the Primary Driver of Efficacy for Voltage-Gated Sodium Channel Targeted AED’s.” December 2017
Company Poster. Society of General Physiologists Annual Meeting: “Selective antagonists of NaV1.6 prevent electrically induced seizures in a mouse model of EIEE13.” September 2016.
Related and supporting publications:
Veeramah et al. “De Novo Pathogenic SCN8A Mutation Identified by Whole-Genome Sequencing of a Family Quartet Affected by Infantile Epileptic Encephalopathy and SUDEP.” 2012 The American Journal of Human Genetics PubMed PMID: 22365152
Ohba et al. “Early onset epileptic encephalopathy caused by de novo SCN8A mutations.” 2014 Epilepsia PubMed PMID: 24888894
Meisler et al. “SCN8A encephalopathy: Research progress and prospects.” 2016 Epilepsia PubMed PMID: 27270488
Hammer et al. “SCN8A-Related Epilepsy with Encephalopathy.” GeneReviews PubMed PMID 27559564
Other Selected Publications
Company Poster. “NaV 1.1 Potentiators Modulate Brain Rhythms Measured Through Quantitative Electrocorticography (qECoG) in a Dravet Mouse Model” 2024 Annual Meeting of the American Epilepsy Society (AES). December 6-10, 2024
Company Poster. “Selective Potentiation of NaV1.1 Channels in Dravet Mice Restores Interneuron Function and Improves Motor Function” 2024 Annual Meeting of the American Epilepsy Society (AES). December 6-10, 2024
Company Poster. “A Selective Nav1.1 Potentiator Enhances Interneuron Excitability to Normalize Motor Performance in a Dravet Syndrome Mouse Model.” 2023 Annual Meeting of the American Epilepsy Society (AES). December 1-5, 2023
Company Poster. “Molecularly Selective Nav1.1 Potentiators Increases PV+ Fast-Spiking
Interneuron Excitability and Restore Motor Performance in a Mouse Model of Dravet Syndrome.” 2022 Annual Meeting of the American Epilepsy Society (AES). December 5, 2022
Company Poster (Virtual). “Nav1.1 Selective Potentiators Normalize Inhibition/Excitation Imbalance and Prevent Seizures in a Mouse Model of Dravet Syndrome.” 2021 Annual Meeting of the American Epilepsy Society (AES). December 3-7, 2021
Company Poster. Virtual 2020 American Epilepsy Society (AES) Annual Meeting: “Early Data from a Phase 2 Open Label Study of XEN007 (Flunarizine) for Treatment Resistant Absence Seizures.” December 4-8, 2020
Company Poster. Virtual 2020 American Epilepsy Society (AES) Annual Meeting: “Selective Potentiation of Inhibitory Networks Prevents Seizures in a Mouse Model of Dravet Syndrome.” December 4-8, 2020
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting: “Small Molecule Potentiators of Nav1.1. Increase Action Potential Firing in Fast Spiking Cortical Inhibitory Interneurons from a Mouse Model of Dravet Syndrome.” December 6-10, 2019
Company Poster. 2019 American Epilepsy Society (AES) Annual Meeting– Genetic Epilepsies Scientific Exhibit: “Selective Sodium Channel Inhibitors and Potentiators; Pharmacology in Cortical Slices from Wild-Type and Dravet Mice.” December 6-10, 2019
Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS. “Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.” PubMed PMID: 29737846
Chernov-Rogan T, Li T, Lu G, Verschoof H, Khakh K, Jones SW, Beresini MH, Liu C, Ortwine DF, McKerrall SJ, Hackos DH, Sutherlin D, Cohen CJ, Chen J. “Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors.” Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801 PubMed PMID: 29311306
Winquist RJ, Cohen CJ. “Integration of biological/pathophysiological contexts to help clarify genotype-phenotype mismatches in monogenetic diseases. Childhood epilepsies associated with SCN2A as a case study. Biochem Pharmacol.” 2018 May;151:252-262. PubMed PMID: 29307654
Focken T, Liu S, Chahal N, Dauphinais M, Grimwood ME, Chowdhury S, Hemeon I, Bichler P, Bogucki D, Waldbrook M, Bankar G, Sojo LE, Young C, Lin S, Shuart N, Kwan R, Pang J, Chang JH, Safina BS, Sutherlin DP, Johnson JP Jr, Dehnhardt CM, Mansour TS, Oballa RM, Cohen CJ, Robinette CL. “Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.” ACS Med Chem Lett. 2016 Jan 19;7(3):277-82. PubMed PMID: 26985315
Huang, J, Vanoye CG, Cutts A, Goldberg YP, Dib-Hajj SD, Cohen CJ, Waxman SG, George AL Jr. “Sodium channel Nav1.9 mutations associated with insensitivity to pain dampen neuronal excitability.” J Clin Invest. 2017 June 30; 127(7):2805-2814. PubMed PMID: 28530638
Ahuja S, Mukund S, Deng L, Khakh K, Chang E, Ho H, Shriver S, Young C, Lin S, Johnson JP Jr, Wu P, Li J, Coons M, Tam C, Brillantes B, Sampang H, Mortara K, Bowman KK, Clark KR, Estevez A, Xie Z, Verschoof H, Grimwood M, Dehnhardt C, Andrez JC, Focken T, Sutherlin DP, Safina BS, Starovasnik MA, Ortwine DF, Franke Y, Cohen CJ, Hackos DH, Koth CM, Payandeh J. “Structural basis of NaV7 inhibition by an isoform-selective small-molecule antagonist.” Science. 2015 Dec 18;350(6267) PubMed PMID: 26680203
Sun S, Jia Q, Zenova AY, Chafeev M, Zhang Z, Lin S, Kwan R, Grimwood ME, Chowdhury S, Young C, Cohen CJ, Oballa RM. “The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Nav1.7.” Bioorg Med Chem Let 2014 August, 24(2):4397-4401. PubMed PMID: 25176194
Goldberg YP, Pimstone SN, Namdari R, Price N, Cohen C, Sherrington RP, Hayden MR. “Human Mendelian pain disorders: a key to discovery and validation of novel analgesics.” Clin Genet. 2012 Oct;82(4):367-73. PubMed PMID: 22845492
Goldberg YP, MacFarlane J, MacDonald ML, Thompson J, Dube MP, Mattice M, Fraser R, Young C, Hossain S, Pape T, Payne B, Radomski C, Donaldson G, Ives E, Cox J, Younghusband HB, Green R, Duff A, Boltshauser E, Grinspan GA, Dimon JH, Sibley BG, Andria G, Toscano E, Kerdraon J, Bowsher D, Pimstone SN, Samuels ME, Sherrington R, Hayden MR. “Loss-of-function mutations in the Nav1.7 gene underlie congenital indifference to pain in multiple human populations.” Clin. Genet. 71(4):311-319, Apr. 2007. PubMed PMID: 17470132
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