Trial reportEuropean journal of drug metabolism and pharmacokinetics2026
A Phase 1, Open-Label, Single Ascending Dose Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of ES-481 After Oral Administration in Healthy Volunteers.
Trial report in European journal of drug metabolism and pharmacokinetics, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
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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
1 citing paper in PubMed.
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesES-481 is a potent and selective antagonist of the transmembrane alpha-amino-3-hydroxy-5-methyl-4 isoxazolepropionic acid (AMPA) receptor regulatory protein (TARP)-y8-dependent AMPA receptor being developed for the treatment of drug-resistant epilepsy (DRE). The objective of this study was to determine the pharmacokinetics and tolerability of ES-481 in humans.
methodsThis study was a Phase 1, first-in-human, single-center, open-label, randomized, sentinel design, ascending dose study of ES-481 to evaluate the pharmacokinetics and tolerability of ES-481 in healthy subjects, with single oral doses ranging from 3 mg to 100 mg. There were 10 dosing cohorts, each comprised of 8 subjects. Within each cohort, 6 subjects were randomized to treatment with ES-481 and 2 subjects were randomized to placebo. In all dosing cohorts, a sentinel pair was dosed first, where 1 subject received ES-481 and 1 subject received a placebo. The sentinel subjects were observed for a minimum of 24 h. If no safety concerns were identified after 24 h, then the remaining 6 subjects in each dosing cohort were administered the investigational product (5 subjects administered ES-481 and 1 subject administered a placebo). In one cohort, only 5 subjects were treated with ES-481. A total of 79 subjects were administered the investigational product (ES-481 or placebo) instead of 80. Blood samples were obtained from each subject up to 48<h post-dose. Following quantification of the concentration of ES-481, pharmacokinetic parameters were derived from plasma concentration-time data using a noncompartmental model.
resultsAn approximately proportional increase in AUC parameters and C
conclusionsES-481 doses up to 100 mg were found to be safe and well tolerated. There were no safety findings in this study of concern, and all of the adverse events related to the administration of ES-481 were mild and transient This study describes the pharmacokinetic parameters of ES-481 for the proposed efficacious dose range of 75-100 mg/day of ES-481 for the treatment of DRE.
Indexed as
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Registered trials
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