Compounds > sulcardine sulfate
Page last updated: 2024-11-12

sulcardine sulfate

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

Description

sulcardine sulfate: antiarrhythmic agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16043221
CHEMBL ID4594410
SCHEMBL ID19134053
MeSH IDM0558041

Synonyms (13)

Synonym
SCHEMBL19134053
hbi-3000
sulcardine sulfate
unii-4ndn0njz62
343935-61-5
sulcardine sulfate anhydrous
4NDN0NJZ62 ,
benzenesulfonamide, n-((4-hydroxy-3,5-bis(1-pyrrolidinylmethyl)phenyl)methyl)-4-methoxy-, sulfate (1:1)
343935-61-5 (sulfate)
n-(4-hydroxy-3,5-bis(pyrrolidin-1-ylmethyl)benzyl)-4-methoxybenzenesulfonamide sulfate
CHEMBL4594410
n-[[4-hydroxy-3,5-bis(pyrrolidin-1-ylmethyl)phenyl]methyl]-4-methoxybenzenesulfonamide;sulfuric acid
AKOS040749576

Research Excerpts

Overview

Sulcardine sulfate (Sul) is a novel antiarrhythmic agent with promising pharmacological properties. It is currently being evaluated in several clinical trials as an oral formulation. Sulcardine was shown to be safe and tolerated in clinical trials.

ExcerptReferenceRelevance
"Sulcardine sulfate (Sul) is a novel antiarrhythmic agent with promising pharmacological properties, which is currently being evaluated in several clinical trials as an oral formulation. "( Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate.
Bian, Y; Chen, X; Cheng, Y; Kong, D; Li, N; Lu, Y; Ning, C; Ren, C; Su, S; Sun, M; Wang, Y; Zhang, M; Zhang, Y; Zhao, D, 2021)		2.26
"Sulcardine sulfate (sulcardine) is a novel anti-arrhythmic compound, which blocks multiple channels and was shown to be safe and tolerated in clinical trials. "( Characteristics of hERG and hNav1.5 channel blockade by sulcardine sulfate, a novel anti-arrhythmic compound.
Chen, W; Gan, L; Wang, Y, 2019)		2.2
"Sulcardine sulfate is a newly developed candidate drug used to control arrhythmias. "( Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs.
Jia, JY; Li, SJ; Li, XC; Liu, GY; Lu, YL; Wang, YP; Yang, D; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		2.13
"Sulcardine sulfate is a novel antiarrhythmic agent with mechanism of action as a multi-ion channel blocker. "( Multiple Dose Pharmacokinetics and Safety of Sulcardine Sulfate in Healthy Chinese Male Subjects: An Open-Label Phase I Clinical Study.
Jia, JY; Jin, JM; Liu, GY; Liu, Y; Lu, DY; Qian, HJ; Wang, W; Wang, YP; Xin, L; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		2.16
"Sulcardine sulfate (Sul) is a novel anti-arrhythmic agent as a potential treatment for atrial fibrillation and ventricular arrhythmias. "( Pharmacokinetics, safety, and tolerability of sulcardine sulfate: an open-label, single-dose, randomized study in healthy Chinese subjects.
Chen, Q; Hu, CY; Jia, JY; Jin, JM; Li, XN; Liu, GY; Liu, Y; Lu, C; Lu, DY; Qian, HJ; Wang, W; Wang, YP; Yu, C; Zhang, MQ; Zheng, HC, 2017)		2.16

Toxicity

ExcerptReferenceRelevance
"Pharmacokinetic characteristics of sulcardine sulfate were shown to be non-linear, with the modest accumulation upon repeated dosing, and sulcardine sulfate was safe and well tolerated."( Multiple Dose Pharmacokinetics and Safety of Sulcardine Sulfate in Healthy Chinese Male Subjects: An Open-Label Phase I Clinical Study.
Jia, JY; Jin, JM; Liu, GY; Liu, Y; Lu, DY; Qian, HJ; Wang, W; Wang, YP; Xin, L; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		0.99
" Tolerability was determined by clinical evaluation and adverse event (AE) monitoring."( Pharmacokinetics, safety, and tolerability of sulcardine sulfate: an open-label, single-dose, randomized study in healthy Chinese subjects.
Chen, Q; Hu, CY; Jia, JY; Jin, JM; Li, XN; Liu, GY; Liu, Y; Lu, C; Lu, DY; Qian, HJ; Wang, W; Wang, YP; Yu, C; Zhang, MQ; Zheng, HC, 2017)		0.71

Pharmacokinetics

ExcerptReferenceRelevance
" To elucidate its clinical pharmacokinetic characteristics, a rapid and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the quantification of Sul in human plasma."( Determination of the novel antiarrhythmic drug sulcardine sulfate in human plasma by liquid chromatography tandem mass spectrometry and its application in a clinical pharmacokinetic study.
Gui, Y; Jia, J; Li, S; Liu, G; Liu, Y; Lu, C; Lu, Y; Wang, W; Wang, Y; Yu, C; Zhang, M; Zheng, H, 2016)		0.69
"This study was conducted in healthy Chinese male subjects to investigate the pharmacokinetic profile and safety of sulcardine sulfate after repeated oral dose administration at 200, 400, and 800 mg for 5 days."( Multiple Dose Pharmacokinetics and Safety of Sulcardine Sulfate in Healthy Chinese Male Subjects: An Open-Label Phase I Clinical Study.
Jia, JY; Jin, JM; Liu, GY; Liu, Y; Lu, DY; Qian, HJ; Wang, W; Wang, YP; Xin, L; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		0.92
" This study was conducted to investigate the pharmacokinetic profile, safety, and tolerability of Sul in healthy Chinese subjects."( Pharmacokinetics, safety, and tolerability of sulcardine sulfate: an open-label, single-dose, randomized study in healthy Chinese subjects.
Chen, Q; Hu, CY; Jia, JY; Jin, JM; Li, XN; Liu, GY; Liu, Y; Lu, C; Lu, DY; Qian, HJ; Wang, W; Wang, YP; Yu, C; Zhang, MQ; Zheng, HC, 2017)		0.71
" The objective of this study was to systemically investigate the pharmacokinetic profiles of Sul after intravenous infusion."( Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate.
Bian, Y; Chen, X; Cheng, Y; Kong, D; Li, N; Lu, Y; Ning, C; Ren, C; Su, S; Sun, M; Wang, Y; Zhang, M; Zhang, Y; Zhao, D, 2021)		0.82
" The pharmacokinetic behavior after intravenous administration was linear in rats within the dose range of 30-90 mg/kg, but nonlinear in dogs within 30-60 mg/kg."( Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate.
Bian, Y; Chen, X; Cheng, Y; Kong, D; Li, N; Lu, Y; Ning, C; Ren, C; Su, S; Sun, M; Wang, Y; Zhang, M; Zhang, Y; Zhao, D, 2021)		0.82
"Our study systematically explored the pharmacokinetic characteristics of Sul and successfully developed the PBPK model to predict of its clinical PK."( Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate.
Bian, Y; Chen, X; Cheng, Y; Kong, D; Li, N; Lu, Y; Ning, C; Ren, C; Su, S; Sun, M; Wang, Y; Zhang, M; Zhang, Y; Zhao, D, 2021)		0.82

Bioavailability

ExcerptReferenceRelevance
" The aim of this research was to investigate the pharmacokinetics, bioavailability and excretion characteristics of sulcardine in animals."( Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs.
Jia, JY; Li, SJ; Li, XC; Liu, GY; Lu, YL; Wang, YP; Yang, D; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		0.68
" The oral bioavailability was 34-35 % in rats, while a higher exposure was observed in dogs (bioavailability = 62."( Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs.
Jia, JY; Li, SJ; Li, XC; Liu, GY; Lu, YL; Wang, YP; Yang, D; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		0.68

Dosage Studied

ExcerptRelevanceReference
" More than 90 % of dosed sulcardine was recovered, and approximately 20-40 % of the dose excreted into urine as the original form, and the remaining was found in feces and bile, most of which (about 40 %) was transformed into metabolites."( Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs.
Jia, JY; Li, SJ; Li, XC; Liu, GY; Lu, YL; Wang, YP; Yang, D; Yu, C; Zhang, MQ; Zheng, HC; Zhu, F, 2017)		0.68
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (88.89)24.3611
2020's1 (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: 12.06

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

MetricThis Compound (vs All)
Research Demand Index12.06 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (22.22%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (77.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
flecainide
Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		2.0810aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
ranolazine
Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina.		2.0610aromatic amide;
monocarboxylic acid amide;
monomethoxybenzene;
N-alkylpiperazine;
secondary alcohol
uk 68798
[no description available]		2.0610aromatic ether;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
potassium channel blocker
ouabain
Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.		2.071011alpha-hydroxy steroid;
14beta-hydroxy steroid;
5beta-hydroxy steroid;
alpha-L-rhamnoside;
cardenolide glycoside;
steroid hormone		anti-arrhythmia drug;
cardiotonic drug;
EC 2.3.3.1 [citrate (Si)-synthase] inhibitor;
EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
ion transport inhibitor;
plant metabolite
aconitine
Aconitine: A C19 norditerpenoid alkaloid (DITERPENES) from the root of ACONITUM; DELPHINIUM and larkspurs. It activates VOLTAGE-GATED SODIUM CHANNELS. It has been used to induce ARRHYTHMIAS in experimental animals and it has anti-inflammatory and anti-neuralgic properties.. aconitine : A diterpenoid that is 20-ethyl-3alpha,13,15alpha-trihydroxy-1alpha,6alpha,16beta-trimethoxy-4-(methoxymethyl)aconitane-8,14alpha-diol having acetate and benzoate groups at the 8- and 14-positions respectively.		2.0710
ConditionIndicatedRelationship StrengthStudiesTrials
Extrasystole, Ventricular
[description not available]		02.0810
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.4820
Cardiovascular Stroke
[description not available]		02.0810
Injury, Myocardial Reperfusion
[description not available]		02.0810
Cardiac Arrest, Sudden
[description not available]		02.0810
Atrioventricular Nodal Re-Entrant Tachycardia
[description not available]		02.0810
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		02.0810
Ventricular Fibrillation
A potentially lethal cardiac arrhythmia that is characterized by uncoordinated extremely rapid firing of electrical impulses (400-600/min) in HEART VENTRICLES. Such asynchronous ventricular quivering or fibrillation prevents any effective cardiac output and results in unconsciousness (SYNCOPE). It is one of the major electrocardiographic patterns seen with CARDIAC ARREST.		02.0810
Death, Sudden, Cardiac
Unexpected rapid natural death due to cardiovascular collapse within one hour of initial symptoms. It is usually caused by the worsening of existing heart diseases. The sudden onset of symptoms, such as CHEST PAIN and CARDIAC ARRHYTHMIAS, particularly VENTRICULAR TACHYCARDIA, can lead to the loss of consciousness and cardiac arrest followed by biological death. (from Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine, 7th ed., 2005)		02.0810
Tachycardia, Ventricular
An abnormally rapid ventricular rhythm usually in excess of 150 beats per minute. It is generated within the ventricle below the BUNDLE OF HIS, either as autonomic impulse formation or reentrant impulse conduction. Depending on the etiology, onset of ventricular tachycardia can be paroxysmal (sudden) or nonparoxysmal, its wide QRS complexes can be uniform or polymorphic, and the ventricular beating may be independent of the atrial beating (AV dissociation).		02.0810
Arrhythmia
[description not available]		02.0710
Arrhythmias, Cardiac
Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.		02.0710