Page last updated: 2024-11-12

vernakalant

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Description

vernakalant: an antiarrhythmic agent and mixed ion channel blocker [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9930049
CHEMBL ID2111112
CHEBI ID135956
SCHEMBL ID410062
MeSH IDM0516050

Synonyms (32)

Synonym
HY-14182
CHEBI:135956
vernakalant
vernakalant [inn:ban]
unii-9g468c8b13
3-pyrrolidinol, 1-((1r,2r)-2-(2-(3,4-dimethoxyphenyl)ethoxy)cyclohexyl)-, (3r)-
9g468c8b13 ,
794466-70-9
(3r)-1-((1r,2r)-2-(2-(3,4-dimethoxyphenyl)ethoxy)cyclohexyl)pyrrolidin-3-ol
CS-0276
3-pyrrolidinol,1-[(1r,2r)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]-, (3r)-
SCHEMBL410062
vernakalant [who-dd]
vernakalant [inn]
vernakalant [mi]
DTXSID60229659
CHEMBL2111112
J-513102
vemakalant
AKOS027326205
VBHQKCBVWWUUKN-KZNAEPCWSA-N
(r,r)-1-{2-[2-(3,4-dimethoxy-phenyl)-ethoxy]-cyclohexyl}-pyrrolidin-3-(r)-ol
NCGC00378872-01
A864860
DB06217
(r)-1-((1r,2r)-2-(3,4-dimethoxyphenethoxy)cyclohexyl)pyrrolidin-3-ol
EX-A2465
(3r)-1-[(1r,2r)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol
Q665725
AS-56235
EN300-18166971
AC-35850

Research Excerpts

Overview

Vernakalant is an intravenous anti-arrhythmic drug available in Europe, Canada and some countries in Asia for the restoration of sinus rhythm in acute onset atrial fibrillation. It has proven effectiveness and safety compared to placebo and amiodarone in randomized clinical trials.

ExcerptReferenceRelevance
"Vernakalant is a novel drug used to treat atrial fibrillation (AF)."( Effectiveness and Safety Profiles of Vernakalant for Cardioversion of Acute-onset Atrial Fibrillation: A Systematic Review and Meta-analysis.
Guan, Y; Li, J; Sun, B; Wang, X; Wu, D; Yu, C; Zhao, C, 2023
)
1.9
"Vernakalant appears to be a good choice when AF is manifested postoperatively or exists with ischemic heart disease and valvular states. "( Effectiveness and Safety Profiles of Vernakalant for Cardioversion of Acute-onset Atrial Fibrillation: A Systematic Review and Meta-analysis.
Guan, Y; Li, J; Sun, B; Wang, X; Wu, D; Yu, C; Zhao, C, 2023
)
2.63
"Vernakalant is a novel, relatively atrial-selective antiarrhythmic agent. "( Systematic Review and Meta-analysis Appraising Efficacy and Safety of Vernakalant for Cardioversion of Recent-Onset Atrial Fibrillation.
Guo, X; Ma, W; Sun, G; Wang, J; Wang, Q, 2020
)
2.23
"Vernakalant is an intravenous anti-arrhythmic drug available in Europe, Canada and some countries in Asia for the restoration of sinus rhythm in acute onset atrial fibrillation. "( Vernakalant hydrochloride for the treatment of atrial fibrillation: evaluation of its place in clinical practice.
Henney, NC; Lip, GY; Penson, PE; Qin, S; Ritchie, LA, 2020
)
3.44
"Vernakalant is a novel, rapid drug, which is used intravenously, with proven effectiveness and safety compared to placebo and amiodarone in randomized clinical trials."( Flecainide versus vernakalant for conversion of recent-onset atrial fibrillation.
Caro, M; Conde, D; Corrales Barboza, A; Costabel, JP; Ferro, A; Lambardi, F; Lavalle Cobo, A; Trivi, M, 2013
)
1.45
"Vernakalant is a novel, safe, and effective drug used intravenously and has proved to be more rapid in converting recent-onset AF to sinus rhythm compared with placebo and amiodarone."( Propafenone versus vernakalant for conversion of recent-onset atrial fibrillation.
Aragon, M; Conde, D; Corrales Barbosa, A; Costabel, JP; Giniger, A; Klein, A; Lambardi, F; Trivi, M, 2013
)
1.44
"Vernakalant is a new, safe and effective drug used intravenously, which has proved to be more rapid in converting recent onset atrial fibrillation (AF) to sinus rhythm compared to placebo, amiodarone, propafenone, and flecainide in clinical studies. "( Vernakalant: Perception of state of health in patients with a recent-onset atrial fibrillation.
Aragon, M; Conde, D; Costabel, JP; Lambardi, F; Trivi, M, 2014
)
3.29
"Vernakalant is a novel atrial-selective antiarrhythmic drug able to convert recent-onset atrial fibrillation (AF) with reportedly low proarrhythmic risk. "( Predictors of successful cardioversion with vernakalant in patients with recent-onset atrial fibrillation.
Carlson, J; Holmqvist, F; Juhlin, T; Mochalina, N; Öhlin, B; Platonov, PG, 2015
)
2.12
"Vernakalant is an available drug for the treatment of recent-onset atrial fibrillation, producing conversion between 55% and 87% of the patients treated. "( Predictors of conversion of recent-onset atrial fibrillation treated with vernakalant.
Aragón, M; Ariznavarreta, P; Campos, R; Conde, D; Costabel, JP; Lambardi, F; Urdapilleta, M; Vergara, JM, 2015
)
2.09
"Vernakalant is a novel antiarrhythmic that acts selectively in the atrium, and inhibits potassium currents, with minor blockade of IKr currents in the ventricle."( [Vernakalant for the conversion of atrial fibrillation of recent onset].
Baranchuk, A; Conde, D; Seoane, L, 2015
)
2.05
"Vernakalant hydrochloride is a rapid-acting antiarrhythmic drug licensed in the EU since 2010 for the conversion of recent-onset atrial fibrillation with proven efficacy and safety when compared with placebo and amiodarone in randomized clinical trials."( Chemical cardioversion of recent-onset atrial fibrillation in the emergency department using vernakalant hydrochloride achieves safe and rapid restoration of sinus rhythm and facilitates same day discharge.
Gilligan, P; Mahon, P; Sheahan, R; Stoneman, P, 2017
)
2.12
"Vernakalant (RSD1235) is an investigational drug that converts atrial fibrillation rapidly and safely in patients intravenously [Roy et al., J. "( Modeling of high-affinity binding of the novel atrial anti-arrhythmic agent, vernakalant, to Kv1.5 channels.
Eldstrom, J; Fedida, D, 2009
)
2.02
"Vernakalant is a promising novel antiarrhythmic intravenous drug for the rapid conversion of atrial fibrillation to sinus rhythm. "( [Vernakalant: a novel antiarrhythmic drug for the rapid conversion of atrial fibrillation to sinus rhythm].
Eschenhagen, T; Hirt, MN, 2010
)
2.71
"Vernakalant is a new antiarrhythmic drug that acts selectively in the atrium, targeting atrial specific channels: the Kv1.5 channel which carries IK(ur), and the Kir3.1/3.4 channel which carries IK(Ach). "( Vernakalant: a new drug to treat patients with acute onset atrial fibrillation.
Frishman, WH; Tian, D,
)
3.02
"Vernakalant is a relatively atrial-selective antiarrhythmic agent that has been shown to successfully convert atrial fibrillation (AF) to normal sinus rhythm for some patients whose onset of dysrhythmia occurred less than 7 days previously. "( Vernakalant hydrochloride: A novel atrial-selective agent for the cardioversion of recent-onset atrial fibrillation in the emergency department.
Butterfield, NN; Calder, LA; Clement, CM; Dickinson, G; Perry, JJ; Stiell, IG; Vaillancourt, C, 2010
)
3.25
"Vernakalant is a novel anti-arrhythmic drug, recently approved for the cardioversion of recent-onset atrial fibrillation. "( Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant.
Cialdella, P; Pedicino, D; Santangeli, P, 2011
)
2.05
"Vernakalant is a novel antiarrhythmic agent that has demonstrated clinical efficacy for the treatment of atrial fibrillation. "( Vernakalant selectively prolongs atrial refractoriness with no effect on ventricular refractoriness or defibrillation threshold in pigs.
Bechard, J; Gibson, JK; Huang, J; Ideker, RE; Killingsworth, CR; McAfee, DA; Schneidkraut, MJ; Wheeler, JJ, 2011
)
3.25
"Vernakalant hydrochloride is a novel antiarrhythmic drug for the rapid conversion of atrial fibrillation to sinus rhythm and prevention of relapse. "( Disposition and mass balance of [14C]vernakalant after single intravenous and oral doses in healthy volunteers.
Alak, A; Keirns, J; Mao, ZL; Wheeler, JJ, 2011
)
2.08
"Vernakalant is a new antiarrhythmic drug which is used for rapid conversion of atrial fibrillation. "( [Vernakalant--a new drug for pharmacological conversion of atrial fibrillation].
Hinneburg, I, 2011
)
2.72
"Vernakalant hydrochloride is a novel, predominantly atrial-selective antiarrhythmic drug that effectively and rapidly terminates atrial fibrillation (AF). "( Population pharmacokinetics of vernakalant hydrochloride injection (RSD1235) in patients with atrial fibrillation or atrial flutter.
Gao, Y; Kastrissios, H; Keirns, J; Mao, ZL; Townsend, RW; Wheeler, JJ, 2012
)
2.11
"Vernakalant is a relatively atrial-selective antiarrhythmic drug approved for the conversion of recent onset atrial fibrillation in Europe and is under regulatory review in the United States. "( Atrial selective effects of intravenously administered vernakalant in conscious beagle dogs.
Bechard, J; Pourrier, M, 2011
)
2.06
"Vernakalant hydrochloride is a novel, relatively atrial-selective antiarrhythmic agent that rapidly converts atrial fibrillation (AF) to sinus rhythm (SR). "( Population pharmacokinetic-pharmacodynamic analysis of vernakalant hydrochloride injection (RSD1235) in atrial fibrillation or atrial flutter.
Gao, Y; Keirns, JJ; Kshirsagar, S; Mao, Z; Townsend, R; Wheeler, JJ, 2011
)
2.06
"Vernakalant (VER) is a relatively atrial-selective antiarrhythmic drug capable of blocking potassium and sodium currents in a frequency- and voltage-dependent manner. "( Comparison of electrophysiological and antiarrhythmic effects of vernakalant, ranolazine, and sotalol in canine pulmonary vein sleeve preparations.
Antzelevitch, C; Gibson, JK; Lynch, JJ; Pourrier, M; Sicouri, S, 2012
)
2.06
"Vernakalant is a novel, relatively atrial-selective antiarrhythmic drug. "( Vernakalant: conversion of atrial fibrillation in patients with ischemic heart disease.
Beatch, GN; Butterfield, NN; Camm, AJ; Dickinson, G; Torp-Pedersen, C, 2013
)
3.28
"Vernakalant is an emergent antiarrhythmic drug that, in preclinical studies, has demonstrated high efficacy in restoring sinus rhythm and safety in patients with rapid recent-onset atrial fibrillation. "( Efficacy and safety of vernakalant in recent-onset atrial fibrillation after the European medicines agency approval: systematic review and meta-analysis.
Botta, G; Buccelletti, F; Carroccia, A; Franceschi, F; Gentiloni Silveri, N; Iacomini, P; Marsiliani, D, 2012
)
2.13
"Vernakalant is a novel, relatively atrial-selective antiarrhythmic agent for conversion of atrial fibrillation (AF) to sinus rhythm. "( Efficacy and safety of vernakalant in patients with atrial flutter: a randomized, double-blind, placebo-controlled trial.
Beatch, GN; Camm, AJ; Dickinson, G; Ip, J; Juul-Moller, S; Toft, E; Torp-Pedersen, C; Vijayaraman, P; Wyse, DG, 2012
)
2.13
"Vernakalant is an atrial-selective drug specifically designed to block sodium channels at the atrial level, and its intravenous formulation has recently been recommended for approval by the Food and Drug Administration for pharmacological conversion of AF."( [New antiarrhythmic drugs for the treatment of atrial fibrillation].
Botto, GL; Campana, C; Mariconti, B; Pentimalli, F; Russo, G, 2012
)
1.1
"Vernakalant is a newly developed antiarrhythmic drug against atrial fibrillation (AF). "( The new antiarrhythmic drug vernakalant: ex vivo study of human atrial tissue from sinus rhythm and chronic atrial fibrillation.
Christ, T; Endig, S; Fedida, D; Gibson, JK; Knaut, M; Lynch, JJ; Matschke, K; Pourrier, M; Ravens, U; Rozmaritsa, N; Wettwer, E, 2013
)
2.13
"Vernakalant is a new antiarrhythmic agent recently approved in Europe for the rapid cardioversion of recent-onset atrial fibrillation. "( A new antiarrhythmic drug in the treatment of recent-onset atrial fibrillation: vernakalant.
Bonadei, I; Curnis, A; D'Aloia, A; Gelsomino, S; Lorusso, R; Salghetti, F; Vizzardi, E, 2013
)
2.06
"Vernakalant is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more "atrial-selective" than available agents."( The effect of vernakalant (RSD1235), an investigational antiarrhythmic agent, on atrial electrophysiology in humans.
Beatch, GN; Cvitkovic, SS; Dorian, P; Korley, V; Mangat, I; Pinter, A, 2007
)
2.14
"Vernakalant (RSD1235) is an investigational drug recently shown to convert atrial fibrillation rapidly and safely in patients (J Am Coll Cardiol 44:2355-2361, 2004). "( The molecular basis of high-affinity binding of the antiarrhythmic compound vernakalant (RSD1235) to Kv1.5 channels.
Eldstrom, J; Ezrin, A; Fedida, D; Gibson, K; Pourrier, M; Wang, Z; Xu, H, 2007
)
2.01
"Vernakalant is a sodium and ultra-rapid potassium channel blocker with atrial selective effects. "( Vernakalant in the management of atrial fibrillation.
Cheng, JW, 2008
)
3.23
"Vernakalant is a new atrial-selective antiarrhythmic agent. "( Vernakalant in the management of atrial fibrillation.
Cheng, JW, 2008
)
3.23

Effects

Vernakalant has a high affinity to ion channels specifically involved in repolarization of atrial tissue. It has minimal effects in the ventricles and thus, is thought to have a low proarrhythmic potential.

Vernakalant has been reported to be effective in the conversion of POAF. It has been approved in Europe and South America, but not in the United States and Canada.

ExcerptReferenceRelevance
"Vernakalant has a unique pharmacological profile of multi-ion channel activity and atrial-specificity that distinguishes it from other anti-arrhythmic drugs."( Vernakalant hydrochloride for the treatment of atrial fibrillation: evaluation of its place in clinical practice.
Henney, NC; Lip, GY; Penson, PE; Qin, S; Ritchie, LA, 2020
)
2.72
"Vernakalant has a high affinity to ion channels specifically involved in repolarization of atrial tissue and has minimal effects in the ventricles and thus, is thought to have a low proarrhythmic potential."( Pharmacological cardioversion of atrial fibrillation with vernakalant: evidence in support of the ESC Guidelines.
Camm, AJ; Graydon, R; Savelieva, I, 2014
)
1.37
"Vernakalant has been reported to be effective in the conversion of POAF."( Conversion of Atrial Fibrillation after Cardiosurgical Procedures by Vernakalant® as an Atrial Repolarization Delaying Agent (ARDA).
Aubin, H; Boeken, U; Dalyanoglu, H; Korbmacher, B; Lichtenberg, A; Makimoto, H; Mehdiani, A; Minol, JP; Müller, A; Sipahi, NF, 2018
)
1.44
"Vernakalant has been approved in Europe and South America, but it has not been approved in the United States and Canada."( Is vernakalant better or not, compared with other treatments for conversion of acute atrial fibrillation?
Conde, D, 2013
)
1.73
"Vernakalant has been demonstrated more effective than both placebo and amiodarone for the rapid conversion of atrial fibrillation, without significant adverse events."( Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant.
Cialdella, P; Pedicino, D; Santangeli, P, 2011
)
1.32

Treatment

Vernakalant treated patients were older (59.3 ± 12.5 vs. propafenone and flecainide) Treatment with vernakalants resulted in a significantly greater improvement in patient perception of state of health at hour 2.

ExcerptReferenceRelevance
"Vernakalant treated patients were older (59.3 ± 12.5 vs."( Intravenous vernakalant in comparison with intravenous flecainide in the cardioversion of recent-onset atrial fibrillation.
Hartikainen, J; Heikkola, A; Hyppölä, H; Lekkala, M; Pohjantähti-Maaroos, H; Sinisalo, E, 2019
)
1.61
"Treatment with vernakalant resulted in a significantly greater improvement in patient perception of state of health at hour 2 compared with propafenone and flecainide."( Vernakalant: Perception of state of health in patients with a recent-onset atrial fibrillation.
Aragon, M; Conde, D; Costabel, JP; Lambardi, F; Trivi, M, 2014
)
2.18

Toxicity

Vernakalant is effective and safe for restoring sinus rhythm in the hospital emergency department. dysgeusia, paraesthesia and sneezing were most common treatment-emergent adverse events. Three serious adverse events occurred that were considered to be related to study drug.

ExcerptReferenceRelevance
" The molecular structure of existing agents such as amiodarone is being modified in an attempt to improve safety and reduce adverse effects."( Vernakalant: pharmacology electrophysiology, safety and efficacy.
Banchs, JE; Gonzalez, MD; Naccarelli, GV; Penny-Peterson, E; Samii, S; Stevenson, R; Wolbrette, DL, 2008
)
1.79
" Serious adverse events or events leading to discontinuation of study drug were uncommon."( A randomized active-controlled study comparing the efficacy and safety of vernakalant to amiodarone in recent-onset atrial fibrillation.
Beatch, G; Camm, AJ; Capucci, A; Hohnloser, SH; Mangal, B; Torp-Pedersen, C; Van Gelder, IC, 2011
)
0.6
" Both vernakalant and amiodarone were safe and well tolerated in this study."( A randomized active-controlled study comparing the efficacy and safety of vernakalant to amiodarone in recent-onset atrial fibrillation.
Beatch, G; Camm, AJ; Capucci, A; Hohnloser, SH; Mangal, B; Torp-Pedersen, C; Van Gelder, IC, 2011
)
1.08
" Dysgeusia and sneezing were the most common treatment-related adverse events, consistent with previous reports."( Efficacy and safety of vernakalant in patients with atrial flutter: a randomized, double-blind, placebo-controlled trial.
Beatch, GN; Camm, AJ; Dickinson, G; Ip, J; Juul-Moller, S; Toft, E; Torp-Pedersen, C; Vijayaraman, P; Wyse, DG, 2012
)
0.69
" Even though electrical cardioversion is proven to be safe and effective, the need for anesthesia makes alternative strategies more attractive."( Safety and efficacy of pharmacological cardioversion of atrial fibrillation using intravenous vernakalant, a new antiarrhythmic drug with atrial selectivity.
Blomström, P; Blomström-Lundqvist, C, 2012
)
0.6
"Vernakalant is shown to have good conversion rates, an apparently safe antiarrhythmic profile and is well tolerated in patients with a history of ischemic heart disease."( Safety and efficacy of pharmacological cardioversion of atrial fibrillation using intravenous vernakalant, a new antiarrhythmic drug with atrial selectivity.
Blomström, P; Blomström-Lundqvist, C, 2012
)
2.04
" Initially, a longer-acting oral formulation of vernakalant was shown to be effective and safe in preventing AF recurrence after cardioversion in a Phase IIb study."( Safety and efficacy of vernakalant for acute cardioversion of atrial fibrillation: an update.
Dobrev, D; Tsuji, Y, 2013
)
0.96
" In the vernakalant arm, dysgeusia, paraesthesia and sneezing were the most common treatment-emergent adverse events, and three serious adverse events occurred that were considered to be related to study drug."( Safety and efficacy of vernakalant for the conversion of atrial fibrillation to sinus rhythm; a phase 3b randomized controlled trial.
Beatch, GN; Mangal, B, 2016
)
1.18
" Vernakalant was generally well tolerated; the incidence of treatment-emergent adverse events was similar between the groups."( Efficacy and Safety of Vernakalant for Cardioversion of Recent-onset Atrial Fibrillation in the Asia-Pacific Region: A Phase 3 Randomized Controlled Trial.
Beatch, GN; Bhirangi, K; Juul-Moller, S; Rustige, J, 2017
)
1.68
" However, although it showed a safe profile in terms of side effects in this analysis, we are still hesitant about this conclusion and few safety issues should be addressed within specific patients' subgroups."( Efficacy and safety of intravenous vernakalant for the rapid conversion of recent-onset atrial fibrillation: A meta-analysis.
Akel, T; Lafferty, J, 2018
)
0.76
" Adverse events were reported for 30 patients."( [Vernakalant in hospital emergency practice: safety and effectiveness].
Carbajosa Dalmau, J; Cosín-Sales, J; Hernández-Sori, N; Jacob, J; Llorens, P; Martín-Martínez, A; Noceda, J; Peiró-Gómez, A; Pérez-Durá, MJ; Ruescas-Gómez, L; Urtubia-Palacios, A,
)
1.04
"Vernakalant is effective and safe for restoring sinus rhythm in the hospital emergency department."( [Vernakalant in hospital emergency practice: safety and effectiveness].
Carbajosa Dalmau, J; Cosín-Sales, J; Hernández-Sori, N; Jacob, J; Llorens, P; Martín-Martínez, A; Noceda, J; Peiró-Gómez, A; Pérez-Durá, MJ; Ruescas-Gómez, L; Urtubia-Palacios, A,
)
2.48
" Despite its good efficacy profile and rapid onset of action, there was still controversial evidence regarding vernakalant-related adverse events."( Systematic Review and Meta-analysis Appraising Efficacy and Safety of Vernakalant for Cardioversion of Recent-Onset Atrial Fibrillation.
Guo, X; Ma, W; Sun, G; Wang, J; Wang, Q, 2020
)
1

Pharmacokinetics

ExcerptReferenceRelevance
" Key pharmacokinetic parameters analyzed were the maximum plasma concentration and the area under the plasma concentration-time curve."( Pharmacokinetics of novel atrial-selective antiarrhythmic agent vernakalant hydrochloride injection (RSD1235): influence of CYP2D6 expression and other factors.
Beatch, GN; Clohs, L; Keirns, J; Mao, ZL; Wheeler, JJ, 2009
)
0.59
" Plasma vernakalant concentration data from 5 phase 2 and 3 clinical trials of vernakalant in patients with AF or atrial flutter and a phase 1 study in healthy volunteers were used to construct a population pharmacokinetic model."( Population pharmacokinetics of vernakalant hydrochloride injection (RSD1235) in patients with atrial fibrillation or atrial flutter.
Gao, Y; Kastrissios, H; Keirns, J; Mao, ZL; Townsend, RW; Wheeler, JJ, 2012
)
1.1
" This analysis integrates pharmacokinetic (PK) and safety data from 5 clinical trials of patients with AF or atrial flutter (AFL)."( Population pharmacokinetic-pharmacodynamic analysis of vernakalant hydrochloride injection (RSD1235) in atrial fibrillation or atrial flutter.
Gao, Y; Keirns, JJ; Kshirsagar, S; Mao, Z; Townsend, R; Wheeler, JJ, 2011
)
0.62

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Vernakalant holds considerable promise for the treatment of recent-onset AF. Given its relatively short half-life, continuous dosing may be required in order to maintain sinus rhythm. Plasma, urine, and fecal samples were collected for 7 days after dosing.

ExcerptRelevanceReference
" Thus, vernakalant holds considerable promise for the treatment of recent-onset AF; however, given its relatively short half-life, continuous dosing may be required in order to maintain sinus rhythm following conversion from AF."( Vernakalant, a mixed sodium and potassium ion channel antagonist that blocks K(v)1.5 channels, for the potential treatment of atrial fibrillation.
Billman, GE, 2010
)
2.26
" Plasma, urine, and fecal samples were collected for 7 days after dosing to measure vernakalant and its metabolites and to estimate mass balance of total [(14)C] recovery."( Disposition and mass balance of [14C]vernakalant after single intravenous and oral doses in healthy volunteers.
Alak, A; Keirns, J; Mao, ZL; Wheeler, JJ, 2011
)
0.87
" Patients received the recommended dosage of Vernakalant and were clinically observed and monitored (heart rate, invasive blood pressure, pulse oximetry, central venous pressure) in 1-minute-intervals for 20 minutes before- and 120 minutes after the first dose of Vernakalant."( Hemodynamic effects of Vernakalant in cardio-surgical ICU-patients treated for recent-onset postoperative atrial fibrillation.
Domanovits, H; Edlinger-Stanger, M; Holaubek, C; Niederdöckl, J; Niessner, A; Schnaubelt, S; Schütz, N; Simon, A; Spiel, AO; Steinlechner, B; Sulzgruber, P, 2020
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
alcoholA compound in which a hydroxy group, -OH, is attached to a saturated carbon atom.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (136)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's15 (11.03)29.6817
2010's108 (79.41)24.3611
2020's13 (9.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.75

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index49.75 (24.57)
Research Supply Index5.06 (2.92)
Research Growth Index5.05 (4.65)
Search Engine Demand Index79.51 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (49.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials18 (12.95%)5.53%
Reviews46 (33.09%)6.00%
Case Studies4 (2.88%)4.05%
Observational4 (2.88%)0.25%
Other67 (48.20%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]