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.

Klaus Francke, Antje Rottmann, Stefan Klein, Joachim Höchel, Christian Friedrich

Abstract readClinical Trial

In one paragraph

Trial report in International journal of molecular sciences, 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.

ATP-P2X3 Signaling as a Shared Neural Sensitization Pathway in Endometriosis and Irritable Bowel Syndrome: Mechanisms and Therapeutic Implications.Biomedicines · 2026
Review

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

5 authors.

Klaus FranckeResearch and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.

Antje RottmannResearch and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.

Stefan KleinResearch and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.

Joachim HöchelResearch and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.ORCID 0009-0000-8030-0051

Christian FriedrichResearch and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.ORCID 0000-0001-8955-4808

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Hypersensitized P2X3 receptor signaling has been described to play a role in several disorders, including chronic cough. The goal of our in vitro and in vivo studies was to investigate the biotransformation and the influence of CYP3A4 inhibition on the pharmacokinetics of the selective P2X3 antagonist filapixant. Metabolic turnover of filapixant in human liver microsomes and hepatocytes was moderate to high, indicating a complex metabolic pattern with mainly oxidative biotransformation. In recombinant CYP enzymes, depletion of filapixant was observed mainly with CYP3A4 and, to a significantly lesser extent, with CYP1A1, 2D6, 2J2, and 3A5. Drug depletion of [

Indexed as

Cytochrome P-450 CYP3ACytochrome P-450 CYP3A InhibitorsItraconazolePurinergic P2X Receptor AntagonistsAdultDrug InteractionsFemaleHealthy VolunteersHepatocytesHumansMaleMicrosomes, LiverYoung AdultCYP3A4 protein, humanCytochrome P-450 CYP3ACytochrome P-450 CYP3A InhibitorsItraconazolePurinergic P2X Receptor Antagonistsdrug–drug interactionfilapixantitraconazoleP2X3-anatgonistpharmacokinetic

Identifiers

PMID41155469

DOI10.3390/ijms262010177

PMCPMC12564180

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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.