Evidence map›Paper›PMID 40825714›Full record

ArticleBritish journal of clinical pharmacology2025

Effect of vepdegestrant, a PROTAC oestrogen receptor degrader, on dabigatran and rosuvastatin pharmacokinetics in healthy participants.

Derek Z Yang, Li Zhou, Jennifer A Winton, Kyle T Matschke, Constantino Kantaridis, Kristine Doyle, Kimberly C Lee, Naihan Chen, Yuanyuan Zhang, Weiwei Tan

Abstract readClinical Trial, Phase I
PubMed Full text at PMC Publisher
In one paragraph

Article in British 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 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing 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

7 citing papers in PubMed.

  1. A Relative Bioavailability Study of Vepdegestrant Tablets in Healthy Adult Participants.European journal of drug metabolism and pharmacokinetics · 2026
    Trial
  2. Article
  3. Article
  4. Review
  5. Review
  6. Article
  7. 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

10 authors.

Derek Z YangPfizer, Inc., San Diego, CA, USA.
Li ZhouPfizer, Inc., San Diego, CA, USA.
Jennifer A WintonPfizer, Inc., Groton, CT, USA.
Kyle T MatschkePfizer, Inc., Collegeville, PA, USA.
Constantino KantaridisPfizer, Inc., Brussels, Belgium.
Kristine DoylePfizer, Inc., New Haven, CT, USA.
Kimberly C LeePfizer, Inc., Groton, CT, USA.
Naihan ChenPfizer, Inc., Beijing, China.
Yuanyuan ZhangArvinas Operations, Inc., New Haven, CT, USA.
Weiwei TanPfizer, Inc., San Diego, CA, USA.ORCID https://orcid.org/0000-0001-8915-1152

Funding

Arvinas Estrogen Receptor, Inc.Pfizer, Inc.
6 · The paper itself

Abstract

aimsTo evaluate the effects of vepdegestrant, a PROteolysis TArgeting Chimera (PROTAC) oestrogen receptor degrader, on the pharmacokinetics of dabigatran (a P-glycoprotein [P-gp] substrate) and rosuvastatin (a breast cancer resistance protein [BCRP] substrate).

methodsIn two phase 1, open-label, two-period, fixed-sequence studies, healthy adult participants received a single oral dose of dabigatran etexilate 75 mg or rosuvastatin 10 mg alone and with a single dose of vepdegestrant 200 mg. Serial plasma samples were collected after dosing, and pharmacokinetic parameters for dabigatran and rosuvastatin were estimated by standard noncompartmental analysis.

resultsCoadministration of the P-gp substrate dabigatran etexilate with vepdegestrant increased dabigatran area under the concentration-time curve (AUC) from time 0 to infinity by 98% and maximum plasma concentration (C

conclusionsCoadministration with vepdegestrant doubled dabigatran exposure and resulted in a minor increase (11%) in rosuvastatin exposure in humans.

Indexed as

AntithrombinsDabigatranPyridinesPyrimidinesRosuvastatin CalciumSulfonamidesAdministration, OralAdultArea Under CurveATP Binding Cassette Transporter, Subfamily G, Member 2Drug InteractionsFemaleHealthy VolunteersHumansHydroxymethylglutaryl-CoA Reductase InhibitorsMaleABCG2 protein, humanAntithrombinsATP Binding Cassette Transporter, Subfamily G, Member 2DabigatranHydroxymethylglutaryl-CoA Reductase InhibitorsNeoplasm ProteinsPyridinesPyrimidinesRosuvastatin CalciumSulfonamidesbreast cancerdrug interactionsdrug transportersp‐glycoproteinpharmacokinetics

Identifiers

PMID40825714
PMCPMC12648365

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.