selurampanel

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

selurampanel: anticonvulsant that antagonizes both AMPA and kainate receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	45381907
CHEMBL ID	3545042
SCHEMBL ID	1660562
MeSH ID	M000597226

Synonyms (23)

Synonym
n-[7-isopropyl-6-(2-methyl-2h-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl]-methanesulfonamide
MCECSFFXUPEPDB-UHFFFAOYSA-N
7wg1mr7dar ,
bgg 492a
selurampanel [inn]
selurampanel
bgg 492
unii-7wg1mr7dar
912574-69-7
bgg492
selurampanel [who-dd]
bgg-492
n-(6-(1-methyl-1h-pyrazol-5-yl)-7-(propan-2-yl)-2,4-dioxo-1,4-dihydroquinazolin-3(2h)-yl)methanesulfonamide
SCHEMBL1660562
CHEMBL3545042
DTXSID00238467
DB12367
AKOS032946688
n-[6-(2-methylpyrazol-3-yl)-2,4-dioxo-7-propan-2-yl-1h-quinazolin-3-yl]methanesulfonamide
Q21098868
SB17404
HY-105860
CS-0026799

Research Excerpts

Overview

Selurampanel (BGG492) is an experimental competitive AMPA antagonist currently in clinical trials.

Excerpt	Reference	Relevance
"Selurampanel (BGG492) is an experimental competitive AMPA antagonist currently in clinical trials."	( BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy. Faught, E, 2014)	1.56

Toxicity

Excerpt	Reference	Relevance
" Adverse events were reported by 80%, 56%, and 60% of BGG492, sumatriptan, and placebo subjects, respectively."	( 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. Brand, R; Campos, V; Diener, HC; Evers, S; Göbel, H; Gomez-Mancilla, B; Hariry, S; Johns, D; Jürgens, TP; Kalkman, HO; Pezous, N; Sommer, C; Sommer, M; Straube, A, 2014)	0.4
" Safety was assessed by recording all adverse events (AEs)."	( 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. Abd-Elaziz, K; Derne, C; Johns, D; Kucher, K; Langguth, B; Pfister, CU; Sverdlov, O; Wagner, F, 2021)	0.88

Bioavailability

Excerpt	Reference	Relevance
" Guided by ionic liquid structure, in vivo profiles ranged from rapid bioavailability and high maximal plasma concentrations to sustained patterns."	( Mapping the pharmaceutical design space by amorphous ionic liquid strategies. Balk, A; Bruhn, H; Dekant, W; Galli, B; Holzgrabe, U; Lühmann, T; Meinel, L; Merget, B; Picard, F; Raccuglia, M; Saedtler, M; Sotriffer, C; Stopper, H; Walid, E; Widmer, T; Wiest, J, 2017)	0.46

Dosage Studied

Excerpt	Relevance	Reference
"To evaluate dose-response relationship of BGG492 as add-on therapy to 1-3 antiepileptic drugs in patients with partial-onset seizures and to investigate safety and tolerability of BGG492."	( BGG492 as an adjunctive treatment in patients with partial-onset seizures: A 12-week, randomized, double-blind, placebo-controlled, phase II dose-titration study with an open-label extension. Brandt, C; Elger, CE; Han, J; Hong, SB; Mancione, L; Strohmaier, C, 2017)	0.46
" In the core study, no statistically significant dose-response trend among the BGG492 treatment groups (100 and 150 mg) was observed at the 4-week double-blind maintenance period (weeks 7-10); however, there was higher percent reduction in total partial seizure frequency in the BGG492 150 mg over placebo groups (37."	( BGG492 as an adjunctive treatment in patients with partial-onset seizures: A 12-week, randomized, double-blind, placebo-controlled, phase II dose-titration study with an open-label extension. Brandt, C; Elger, CE; Han, J; Hong, SB; Mancione, L; Strohmaier, C, 2017)	0.46
"There was no significant dose-response trend in the BGG492 treatment groups (100 and 150 mg); however, higher percent reduction over placebo was observed in the BGG492 150 mg group."	( BGG492 as an adjunctive treatment in patients with partial-onset seizures: A 12-week, randomized, double-blind, placebo-controlled, phase II dose-titration study with an open-label extension. Brandt, C; Elger, CE; Han, J; Hong, SB; Mancione, L; Strohmaier, C, 2017)	0.46

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	8 (88.89)	24.3611
2020's	1 (11.11)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	21.21 (24.57)
Research Supply Index	2.64 (2.92)
Research Growth Index	4.55 (4.65)
Search Engine Demand Index	18.60 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (21.21)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	4 (44.44%)	5.53%
Reviews	3 (33.33%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	2 (22.22%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.	4.4	1	1	sulfonamide; tryptamines	serotonergic agonist; vasoconstrictor agent
pregnanolone Pregnanolone: A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.. 3alpha-hydroxy-5beta-pregnan-20-one : The 3alpha-stereoisomer of 3-hydroxy-5beta-pregnan-20-one.	3.27	1	0	3-hydroxy-5beta-pregnan-20-one; 3alpha-hydroxy steroid	human metabolite; intravenous anaesthetic; sedative
ganaxolone ganaxolone: a selective, high-affinity, steroid modulator of the GABA(A) receptor; structure given in first source; RN given refers to (3alpha,5alpha)-isomer	3.27	1	0	corticosteroid hormone
cannabidivarin cannabidivarin: from Cannabis sativa	3.27	1	0	monoterpenoid

Condition	Indicated	Relationship Strength	Studies	Trials
Pulsatile Tinnitus [description not available]	0	5.85	2	1
Tinnitus A nonspecific symptom of hearing disorder characterized by the sensation of buzzing, ringing, clicking, pulsations, and other noises in the ear. Objective tinnitus refers to noises generated from within the ear or adjacent structures that can be heard by other individuals. The term subjective tinnitus is used when the sound is audible only to the affected individual. Tinnitus may occur as a manifestation of COCHLEAR DISEASES; VESTIBULOCOCHLEAR NERVE DISEASES; INTRACRANIAL HYPERTENSION; CRANIOCEREBRAL TRAUMA; and other conditions.	1	12.85	2	1
Abdominal Epilepsy [description not available]	0	3.53	1	1
Epilepsies, Partial Conditions characterized by recurrent paroxysmal neuronal discharges which arise from a focal region of the brain. Partial seizures are divided into simple and complex, depending on whether consciousness is unaltered (simple partial seizure) or disturbed (complex partial seizure). Both types may feature a wide variety of motor, sensory, and autonomic symptoms. Partial seizures may be classified by associated clinical features or anatomic location of the seizure focus. A secondary generalized seizure refers to a partial seizure that spreads to involve the brain diffusely. (From Adams et al., Principles of Neurology, 6th ed, pp317)	0	3.53	1	1
Drug Refractory Epilepsy [description not available]	0	3.09	1	0
Aura [description not available]	0	3.92	2	0
Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)	1	10.92	2	0
Abdominal Migraine [description not available]	0	4.4	1	1
Acute Disease Disease having a short and relatively severe course.	0	4.4	1	1
Migraine Disorders A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)	1	6.4	1	1
Audiogenic Epilepsy [description not available]	0	4.41	1	1
Epilepsy, Reflex A subtype of epilepsy characterized by seizures that are consistently provoked by a certain specific stimulus. Auditory, visual, and somatosensory stimuli as well as the acts of writing, reading, eating, and decision making are examples of events or activities that may induce seizure activity in affected individuals. (From Neurol Clin 1994 Feb;12(1):57-8)	1	6.41	1	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.15	1	0
Absence Seizure [description not available]	0	2.15	1	0
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	1	4.15	1	0

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