Trial reportBritish journal of clinical pharmacology2022
First-in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics.
Trial report in British journal of clinical pharmacology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02817100 (Randomized, Placebo-controlled, Double-blind, Parallel Group Study to Investigate the Safety, Tolerability and Pharmacokinetics of Increasing Single Oral Doses), which is not on this map. Cited by 10 papers.
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.
Randomized, Placebo-controlled, Double-blind, Parallel Group Study to Investigate the Safety, Tolerability and Pharmacokinetics of Increasing Single Oral Doses (10 - 1500 mg, Tablets) of BAY1817080 Including the Effect of Food and Itraconazole on the Relative Bioavailability of BAY1817080 in Healthy Men
Who cites it
10 citing papers in PubMed, 23 citations in OpenAlex.
- Investigation of the Relevance of CYP3A4 Inhibition on the Pharmacokinetics of the Novel P2X3 Antagonist Filapixant: Results of In Vitro Explorations and a Fixed-Sequence Clinical Trial with Itraconazole in Healthy Volunteers.International journal of molecular sciences · 2025Trial
- P2X3 Receptor Antagonist Eliapixant in Phase I Clinical Trials: Safety and Inter-ethnic Comparison of Pharmacokinetics in Healthy Chinese and Japanese Participants.Clinical pharmacokinetics · 2024Trial
- Trial
- First-in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics.British journal of clinical pharmacology · 2022Trial
- Spinal P2XPurinergic signalling · 2026Article
- Molecular insights into P2X signalling cascades in acute kidney injury.Purinergic signalling · 2024Review
- Drugs Targeting Cough Receptors: New Therapeutic Options in Refractory or Unexplained Chronic Cough.Drugs · 2024Review
- Mass Balance and Metabolic Pathways of Eliapixant, a P2X3 Receptor Antagonist, in Healthy Male Volunteers.European journal of drug metabolism and pharmacokinetics · 2024Article
- Diclofenac and other non-steroidal anti-inflammatory drugs (NSAIDs) are competitive antagonists of the human P2X3 receptor.Frontiers in pharmacology · 2023Article
- Engineering Nanoscale Drug Delivery Systems for Pain.Wiley interdisciplinary reviews. Nanomedicine and nanobiotechnologyReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsNeuronal hypersensitisation due to adenosine triphosphate-dependent P2X3 receptor signalling plays a significant role in several disorders including chronic cough and endometriosis. This first-in-human study of eliapixant (BAY 1817080) investigated the tolerability, safety and pharmacokinetics (PK) of single doses of eliapixant, including the effect of food and coadministration with a CYP3A inhibitor on eliapixant relative bioavailability.
methodsIn this randomised, double-blind phase I study (NCT02817100), 88 healthy male subjects received single ascending doses of immediate-release eliapixant (10-800 mg) tablets or placebo under fasted conditions, with food (low-fat continental or high-fat American breakfast) or with itraconazole (fasted state). PK parameters, dose proportionality, adverse events and taste assessments (taste strips; dysgeusia questionnaire) were evaluated.
resultsEliapixant had a long half-life (23.5-58.9 h [fasted state]; 32.8-43.8 h [high-fat breakfast]; 38.9-46.0 h [low-fat breakfast]). Less than dose-proportional increases in maximum plasma concentrations (C
conclusionThe PK profile, particularly the long half-life, and favourable tolerability with no taste-related adverse events, supports the further development of eliapixant in disorders with underlying P2X3 receptor-mediated neuronal hypersensitisation.
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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.