selurampanel (BGG492) / Novartis - LARVOL DELTA

Current and future pharmacotherapy options for drug-resistant epilepsy. (PubMed, Expert Opin Pharmacother) - "Current pharmacotherapy options for drug-resistant epilepsy include perampanel, brivaracetam and the newly approved cenobamate for focal epilepsies; cannabidiol (Epidiolex) for Lennox-Gastaut Syndrome (LGS), Dravet and Tuberous Sclerosis Complex (TSC); fenfluramine for Dravet syndrome and ganaxolone for seizures in Cyclin-dependent kinase-like 5 (CDKL5) deficiency disorder...For adult focal epilepsies, padsevonil and carisbamate are at a more advanced Phase III stage of clinical development followed by compounds at Phase II like selurampanel, XEN1101 and JNJ-40411813. For specific epilepsy syndromes, XEN 496 is under Phase III development for potassium voltage-gated channel subfamily Q member 2 developmental and epileptic encephalopathy (KCNQ2-DEE), carisbamate is under Phase III development for LGS and Ganaxolone under Phase III development for TSC. Finally, in preclinical models several molecular targets including inhibition of glycolysis, neuroinflammation and sodium..."

Journal • CNS Disorders • Epilepsy • Genetic Disorders • Immunology • Inflammation

Efficacy and safety of single- and repeated-selurampanel dosing for 2 weeks in patients with chronic subjective tinnitus: Results of a randomized, double-blind, placebo-controlled, cross-over, proof-of-concept phase IIa study. (PubMed, Prog Brain Res) - P2 | "In conclusion, BGG492 showed reduction of both tinnitus loudness and annoyance after a single dose and reduction of tinnitus handicap after 2 weeks of treatment in patients with chronic subjective tinnitus, thereby supporting further clinical investigation of AMPA receptor antagonists with an improved benefit/risk ratio. A dose of 100mg TID BGG492 showed higher efficacy but somewhat lower tolerability compared to 50mg TID."

Clinical • Journal • P2a data • Otorhinolaryngology

Efficacy of BGG492 in individuals with refractory partial seizures undergoing inpatient evaluation for epilepsy surgery -

P2, N=37;

Randomized, multicenter trial to assess the efficacy, safety and tolerability of a single dose of a novel AMPA receptor antagonist BGG492 for the treatment of acute migraine attacks (Cephalalgia) - PMID: 23963355; P2, N=75; NCT00892203; Sponsor: Novartis; PMID: 23963355; "Improvement from severe/moderate to mild/no headache pain (primary response)...58%, 58%, and 54% of BGG492-treated subjects at 2, 3, and 4 hours post-dose (p =0.2, 0.5, and 0.5 vs placebo), respectively, compared with 68%, 84%, and 92% sumatriptan-treated subjects, and 40%, 48%, and 44% in the placebo group."

P2 data • Migraine

An update: emerging drugs for tinnitus. (PubMed, Expert Opin Emerg Drugs) - "Areas covered: In this editorial results from recent Phase 3 and Phase 2a trials investigating the NMDA receptor antagonist AM-101 from Auris Medical, the AMPA receptor antagonist BGG492 from Novartis and the Kv3 modulator AUT00063 from Autifony Therapeutics will be discussed. Expert opinion: In spite of huge advances in pathophysiologic knowledge and research methodology in the last decades, pharmaceutical research in tinnitus still represents a high-risk field. Important research directions include the identification of potential therapeutic targets and the development of objective outcome measurements to facilitate translational research."

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