Evidence mapPaperPMID 41476196Full record

ArticleJournal of translational medicine2025

Synergistic antiarrhythmic mechanism of I

Miaomiao Ju, Suhua Qiu, Yi Wang, Wenting Wu, Jinglei Sun, Chenxia Shi, Qingzhong Jia, Yanfang Xu

Abstract read
In one paragraph

Article in Journal of translational medicine, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Miaomiao JuDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Suhua QiuDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Yi WangDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Wenting WuDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Jinglei SunDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Chenxia ShiDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Qingzhong JiaDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China.
Yanfang XuDepartment of Pharmacology, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, China. yanfangxu@hebmu.edu.cn.

Funding

Hebei Provincial Department of Science and Technology 236Z7750G
6 · The paper itself

Abstract

backgroundArrhythmias represent a leading cause of mortality among individuals with cardiovascular diseases. Considering the failure of antiarrhythmic drugs targeting single-ion channels in clinical trials, this study aims to evaluate the pharmacodynamics of various combinations of single-channel blockers to identify safer and more effective therapeutic regimens.

methodsThe antiarrhythmic effects of inhibitors alone and pairwise combination strategies targeting late sodium current (INa-L), hERG potassium current (IKr), ryanodine receptor 2 (RyR2), and L-type calcium current (ICa-L) inhibitors via a checkerboard dosing approach were evaluated in human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). Comprehensive evaluation based on synergy scoring, efficacy, and toxicity (SynergyFinder) was performed to identify the preferred combination with high efficacy and low toxicity. The effectiveness of the preferred combination was further validated in isolated perfused guinea pig hearts. In addition, an analysis of the effects of the preferred combination on calcium sparks and Ca2+/calmodulin-dependent protein kinase II (CaMKII) was conducted.

resultsA combination regimen of the INa-L inhibitor GS967 and the RyR2 inhibitor Dantrolene, which exhibited highly effective, low-toxicity synergistic antiarrhythmic properties, was identified through checkerboard high-throughput screening. An alternative combination of the INa-L blocker Eleclazine and the RyR2 inhibitor TMDJ-035 showed similar therapeutic efficacy, indicating that the effectiveness of the preferred combination stems from target-mediated effects. The combination further demonstrated significant efficacy in multiple hiPSC-CM arrhythmia models and an ex vivo guinea pig heart reperfusion arrhythmia model. Mechanistic studies revealed that the dual-target inhibition strategy corrected pathological calcium sparks and calcium cycling dysfunction, downregulated the CaMKII-RyR2 phosphorylation cascade, thereby restoring electrical signaling.

conclusionsThe combination of INa-L and RyR2 inhibitors exerts safer and more effective antiarrhythmic effects. This combinational therapeutic strategy provides a theoretical basis for developing novel antiarrhythmic regimens based on dual-target regulation, demonstrating significant translational medical potential and warranting further clinical evaluation.

Indexed as

Anti-Arrhythmia AgentsCalciumCalcium-Calmodulin-Dependent Protein Kinase Type 2Calcium SignalingRyanodine Receptor Calcium Release ChannelSignal TransductionAnimalsArrhythmias, CardiacCalcium Channel BlockersDrug SynergismGuinea PigsHumansInduced Pluripotent Stem CellsMyocytes, CardiacAnti-Arrhythmia AgentsCalciumCalcium-Calmodulin-Dependent Protein Kinase Type 2Calcium Channel BlockersRyanodine Receptor Calcium Release ChannelArrhythmiashiPSC-CMsI Na-LRyR2

Identifiers

PMID41476196
PMCPMC12866562

What Socratic holds

Textmetadata
LicenceCC BY-NC-ND
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.