Evidence map›Paper›PMID 41246975›Full record

ArticleClinical and translational science2025

A Phase 1 Study to Assess the Effect of Fruquintinib on the Pharmacokinetics of P-gp and BCRP Substrates in Healthy Subjects.

Martha Gonzalez, Zhao Yang, William R Schelman, Xiaofei Zhou, Neeraj Gupta, Caly Chien

Registry-linked trialAbstract readClinical Trial, Phase I
In one paragraph

Article in Clinical and translational science, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05368805 (A Phase 1, Open-label, 2-part, 2-period Fixed-sequence Study to Evaluate the Effect of Fruquintinib on the Pharmacokinetics of Dabigatran Etexilate), which is not on this 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.

NCT05368805 phase1completednot on this map

A Phase 1, Open-label, 2-part, 2-period Fixed-sequence Study to Evaluate the Effect of Fruquintinib on the Pharmacokinetics of Dabigatran Etexilate (A P-GP Substrate) and Rosuvastatin (A BCRP Substrate) in Healthy Subjects

TypeinterventionalSponsorHutchmedRan2022 to 2022Enrolled32ConditionsMetastatic Colorectal CancerArmsFruquintinib, Dabigatran Etexilate, Rosuvastatin
3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. 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

6 authors.

Martha GonzalezHUTCHMED International Corporation, Florham Park, New Jersey, USA.
Zhao YangHUTCHMED International Corporation, Florham Park, New Jersey, USA.
William R SchelmanHUTCHMED International Corporation, Florham Park, New Jersey, USA.
Xiaofei ZhouTakeda Development Center Americas, Inc. (TDCA), Cambridge, Massachusetts, USA.ORCID 0000-0003-0319-1327
Neeraj GuptaTakeda Development Center Americas, Inc. (TDCA), Cambridge, Massachusetts, USA.ORCID 0000-0002-5500-5218
Caly ChienHUTCHMED International Corporation, Florham Park, New Jersey, USA.ORCID 0009-0002-7054-9536

Funding

HUTCHMED International Corporation and Takeda Pharmaceuticals U.S.A. Inc.
6 · The paper itself

Abstract

Fruquintinib, a highly selective, oral inhibitor of all three vascular endothelial growth factor receptors (-1, -2, and -3), is approved for previously treated metastatic colorectal cancer. This phase 1, two-part, two-period, fixed-sequence study (NCT05368805) evaluated the potential inhibitory effect of fruquintinib (5 mg) on the pharmacokinetics (PK) of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) substrates. In Part A, 20 healthy subjects received a single oral dose of dabigatran etexilate (P-gp substrate) 150 mg on Day 1 and Day 5, with fruquintinib co-administered on Day 5. In Part B, 12 healthy subjects received a single oral dose of rosuvastatin (BCRP substrate) 10 mg on Day 1 and Day 5, with fruquintinib co-administered on Day 5. Plasma samples were collected to evaluate the PK of dabigatran and rosuvastatin over 96 h, and to measure fruquintinib and its major metabolite M11 concentrations over 192 h. Co-administration of dabigatran etexilate with fruquintinib resulted in a ~10% decrease in the systemic exposure of dabigatran; geometric mean ratios (GMRs) and 90% CIs were 0.90 (0.66-1.23) for C

Indexed as

ATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2BenzofuransNeoplasm ProteinsQuinazolinesAdministration, OralAdultArea Under CurveDabigatranDrug InteractionsFemaleHealthy VolunteersHumansMaleMiddle AgedRosuvastatin CalciumABCG2 protein, humanATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2BenzofuransDabigatranNeoplasm ProteinsQuinazolinesRosuvastatin Calciumdabigatran etexilatedrug–drug interactionfruquintinibpharmacokineticsrosuvastatin

Identifiers

PMID41246975
PMCPMC12621112

What Socratic holds

Textmetadata
LicenceCC BY-NC
Read underepoch 390

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 Socratic graph.