Evidence map›Paper›PMID 39565495›Full record

ArticleInternational journal of clinical oncology2025

Safety and pharmacokinetics of vepdegestrant in Japanese patients with ER+ advanced breast cancer: a phase 1 study.

Hiroji Iwata, Yoichi Naito, Masaya Hattori, Akiyo Yoshimura, Kan Yonemori, Mana Aizawa, Yuko Mori, Junichiro Yoshimitsu, Yoshiko Umeyama, Toru Mukohara

Registry-linked trialAbstract readClinical Trial, Phase IMulticenter Study
PubMed Full text at PMC Publisher
In one paragraph

Article in International journal of clinical oncology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05463952 (A PHASE I, OPEN-LABEL STUDY TO EVALUATE THE SAFETY, TOLERABILITY AND PHARMACOKINETICS OF ARV-471), which is not on this 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.

NCT05463952 phase1active not recruitingnot on this map

A phase i, open-label study to evaluate the safety, tolerability and pharmacokinetics of arv-471 (pf-07850327), a single agent in japanese participants with er+/her2-locally advanced or metastatic breast cancer

TypeinterventionalSponsorPfizerRan2022 to 2025Enrolled6ConditionsBreast NeoplasmsArmsvepdegestrant
3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Trial
  2. Article
  3. Review
  4. Review
  5. Review
  6. Review
  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.

Hiroji IwataDepartment of Breast Oncology, Aichi Cancer Center Hospital, 1-1 Kanokoden, Chikusa-ku, Nagoya, Aichi, 464-8681, Japan. hiwata0422@gmail.com.
Yoichi NaitoDepartment of Medical Oncology, National Cancer Center Hospital East, 6-5-1 Kashiwanoha, Kashiwa, Chiba, 277-8577, Japan.
Masaya HattoriDepartment of Breast Oncology, Aichi Cancer Center Hospital, 1-1 Kanokoden, Chikusa-ku, Nagoya, Aichi, 464-8681, Japan.
Akiyo YoshimuraDepartment of Breast Oncology, Aichi Cancer Center Hospital, 1-1 Kanokoden, Chikusa-ku, Nagoya, Aichi, 464-8681, Japan.
Kan YonemoriDepartment of Medical Oncology, National Cancer Center Hospital, 5-1-1 Tsukiji Chuo-ku, Tokyo, 104-0045, Japan.
Mana AizawaDepartment of Biometrics and Data Management, Pfizer R&D Japan, 3-22-7 Yoyogi, Shibuya-ku, Tokyo, 151-8589, Japan.
Yuko MoriDepartment of Clinical Research, Pfizer R&D Japan, 3-22-7 Yoyogi, Shibuya-ku, Tokyo, 151-8589, Japan.
Junichiro YoshimitsuDepartment of Clinical Research, Pfizer R&D Japan, 3-22-7 Yoyogi, Shibuya-ku, Tokyo, 151-8589, Japan.
Yoshiko UmeyamaDepartment of Clinical Research, Pfizer R&D Japan, 3-22-7 Yoyogi, Shibuya-ku, Tokyo, 151-8589, Japan.
Toru MukoharaDepartment of Medical Oncology, National Cancer Center Hospital East, 6-5-1 Kashiwanoha, Kashiwa, Chiba, 277-8577, Japan.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundVepdegestrant (ARV-471) is an oral PROteolysis TArgeting Chimera (PROTAC) estrogen receptor (ER) degrader.

methodsThis phase 1 study (NCT05463952) investigated safety, pharmacokinetics, and antitumor activity of vepdegestrant in Japanese patients with ER-positive (ER+)/human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer at the 200-mg once daily (QD) recommended phase 3 dose. Eligible patients had ER+/HER2- advanced breast cancer resistant to standard therapy, with no standard therapy available, or had received two or more prior endocrine therapies in any setting. The primary endpoint was dose-limiting toxicities (DLTs) in cycle 1; secondary endpoints included safety, pharmacokinetics, and antitumor activity.

resultsSix female patients (median age, 58 [range: 47-62] years) were treated. For advanced disease, three (50.0%) patients received three or more prior regimens and five (83.3%) patients received prior cyclin-dependent kinase 4/6 inhibitors. At data cutoff, median treatment duration was 9.8 (range: 6-28) weeks; two patients remained on treatment. No DLTs were observed. Four (66.7%) patients experienced adverse events; none led to dose reduction or discontinuation. Four (66.7%) patients had treatment-related adverse events; all were grade 1 except anemia (grade 2). Geometric mean maximum plasma concentration and 24-h area under the plasma concentration-time curve of vepdegestrant were 630.9 ng/mL and 10,400 ng∙hr/mL after a single dose and 1056 ng/mL and 18,310 ng∙hr/mL after multiple doses. Two (33.3%) patients demonstrated stable disease at week 24.

conclusionVepdegestrant 200 mg QD was well tolerated in Japanese patients with ER+/HER2- advanced breast cancer with no notable differences in pharmacokinetics from Western patients. CLINICAL

trial registrationClinicalTrials.gov: NCT05463952 (date of registration: July 19, 2022).

Indexed as

Breast NeoplasmsReceptors, EstrogenAntineoplastic AgentsEast Asian PeopleErb-b2 Receptor Tyrosine KinasesFemaleHumansJapanMiddle AgedAntineoplastic AgentsERBB2 protein, humanErb-b2 Receptor Tyrosine KinasesReceptors, EstrogenAdvanced breast cancerEstrogen receptor–positiveHuman epidermal growth factor receptor 2–negativeJapanese patientsSafetyVepdegestrant

Identifiers

PMID39565495
PMCPMC11700046

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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.