ArticleFrontiers in pharmacology2012
Cardiac Safety Implications of hNav1.5 Blockade and a Framework for Pre-Clinical Evaluation.
Article in Frontiers in pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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.
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.
Who cites it
17 citing papers in PubMed, 48 citations in OpenAlex.
- Predicting QRS and PR interval prolongations in humans using nonclinical data.British journal of pharmacology · 2017Trial
- Article
- Discovery of NaJournal of natural products · 2025Article
- Article
- Nanomedicine and voltage-gated sodium channel blockers in pain management: a game changer or a lost cause?Drug delivery and translational research · 2024Review
- Current state of the epilepsy drug and device pipeline.Epilepsia · 2024Review
- An orally active entry inhibitor of influenza A viruses protects mice and synergizes with oseltamivir and baloxavir marboxil.Science advances · 2024Article
- Unmasking of Brugada syndrome by lamotrigine in a patient with pre-existing epilepsy: A case report with review of the literature.Frontiers in cardiovascular medicine · 2022Article
- Ventricular voltage-gated ion channels: Detection, characteristics, mechanisms, and drug safety evaluation.Clinical and translational medicine · 2021Review
- Mechanisms of flecainide induced negative inotropy: An in silico study.Journal of molecular and cellular cardiology · 2021Article
- Discovery of aryl sulfonamide-selective Nav1.7 inhibitors with a highly hydrophobic ethanoanthracene core.Acta pharmacologica Sinica · 2020Article
- Article
- Dynamic all-optical drug screening on cardiac voltage-gated ion channels.Scientific reports · 2018Article
- Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaMedChemComm · 2017Article
- Sulfonamides as Selective NaACS medicinal chemistry letters · 2016Article
- Reporting sodium channel activity using calcium flux: pharmacological promiscuity of cardiac Nav1.5.Molecular pharmacology · 2015Article
- Reducing safety-related drug attrition: the use of in vitro pharmacological profiling.Nature reviews. Drug discovery · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The human cardiac sodium channel (hNav1.5, encoded by the SCN5A gene) is critical for action potential generation and propagation in the heart. Drug-induced sodium channel inhibition decreases the rate of cardiomyocyte depolarization and consequently conduction velocity and can have serious implications for cardiac safety. Genetic mutations in hNav1.5 have also been linked to a number of cardiac diseases. Therefore, off-target hNav1.5 inhibition may be considered a risk marker for a drug candidate. Given the potential safety implications for patients and the costs of late stage drug development, detection, and mitigation of hNav1.5 liabilities early in drug discovery and development becomes important. In this review, we describe a pre-clinical strategy to identify hNav1.5 liabilities that incorporates in vitro, in vivo, and in silico techniques and the application of this information in the integrated risk assessment at different stages of drug discovery and development.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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 OpenQuestion graph.