vernakalant: an antiarrhythmic agent and mixed ion channel blocker
ID Source | ID |
---|---|
PubMed CID | 9930049 |
CHEMBL ID | 2111112 |
CHEBI ID | 135956 |
SCHEMBL ID | 410062 |
MeSH ID | M0516050 |
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 |
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.
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Class | Description |
---|---|
alcohol | A compound in which a hydroxy group, -OH, is attached to a saturated carbon atom. |
phenols | Organic 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 10.6840 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 15 (11.03) | 29.6817 |
2010's | 108 (79.41) | 24.3611 |
2020's | 13 (9.56) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (49.75) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 18 (12.95%) | 5.53% |
Reviews | 46 (33.09%) | 6.00% |
Case Studies | 4 (2.88%) | 4.05% |
Observational | 4 (2.88%) | 0.25% |
Other | 67 (48.20%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |