Evidence map›Paper›PMID 39558800›Full record

ArticleJournal of clinical pharmacology2025

In Vitro Evaluation of CYP-Mediated Metabolism of Fezolinetant and Pharmacokinetic Interaction Between Fezolinetant and Fluvoxamine in Healthy Postmenopausal Smokers and Nonsmokers.

Megumi Iwai, Jace Nielsen, Mayuko Miyagawa, Melanie Patton, Peter L Bonate, Xuegong Wang, Tomasz Wojtkowski, Angela Sinn, Jiayin Huang

Abstract readClinical Trial, Phase I
In one paragraph

Article in Journal of clinical pharmacology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Trial
  2. Clinical Pharmacokinetics, Mass Balance and Metabolism of Fezolinetant in Postmenopausal Women.European journal of drug metabolism and pharmacokinetics · 2026
    Article
  3. Article
  4. Article
  5. 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

9 authors.

Megumi IwaiAstellas Pharma Global Development, Inc., Northbrook, IL, USA.
Jace NielsenAstellas Pharma Global Development, Inc., Northbrook, IL, USA.
Mayuko MiyagawaAstellas Pharma, Inc., Tokyo, Japan.
Melanie PattonAstellas Pharma Global Development, Inc., Northbrook, IL, USA.
Peter L BonateAstellas Pharma Global Development, Inc., Northbrook, IL, USA.
Xuegong WangAstellas Pharma Global Development, Inc., Northbrook, IL, USA.
Tomasz WojtkowskiAstellas Pharma Global Development, Inc., Northbrook, IL, USA.
Angela SinnParexel International GmbH, Berlin, Germany.
Jiayin HuangAmgen, Inc., Thousand Oaks, CA, USA.

Funding

Astellas Pharma
6 · The paper itself

Abstract

Fezolinetant is an oral, nonhormonal, neurokinin 3 receptor antagonist treatment option for moderate to severe vasomotor symptoms associated with menopause. An in vitro study using human recombinant cytochrome P450 (CYP) enzymes and human liver microsomes showed that fezolinetant is metabolized to its major but inactive metabolite, ES259564, predominantly through CYP1A2, with minor contributions from CYP2C9 and CYP2C19. The clinical impact of CYP1A2 inhibition and induction on single-dose pharmacokinetics of fezolinetant was assessed in an open-label, single-sequence, phase 1 study in healthy postmenopausal women, where the impact of fluvoxamine, a strong CYP1A2 inhibitor, and smoking, a moderate CYP1A2 inducer, were evaluated. In total, 18 participants, 9 of whom were smokers, were enrolled. Fezolinetant pharmacokinetics were evaluated after a single 30-mg dose on Day 1 and Day 7. Fluvoxamine 50 mg was administered as a single dose on Days 3 and 10 and twice daily from Days 4 to 9. Fluvoxamine increased geometric mean ratio of fezolinetant maximum plasma concentrations (C

Indexed as

FluvoxaminePostmenopauseAgedArea Under CurveCytochrome P-450 CYP1A2Cytochrome P-450 CYP1A2 InhibitorsDrug InteractionsFemaleHumansMicrosomes, LiverMiddle AgedNon-SmokersSmokersSmokingCYP1A2 protein, humanCytochrome P-450 CYP1A2Cytochrome P-450 CYP1A2 InhibitorsFluvoxamineCYP1A2drug–drug interactionfezolinetantinductioninhibitionsmoking

Identifiers

PMID39558800
PMCPMC11937985

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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 OpenQuestion graph.