Evidence map›Paper›PMID 34480554›Full record

ReviewEndocrinology2021

Endoxifen, an Estrogen Receptor Targeted Therapy: From Bench to Bedside.

Swaathi Jayaraman, Joel M Reid, John R Hawse, Matthew P Goetz

Erratum issuedOpen access · bronzeAbstract readReview
In one paragraph

Review in Endocrinology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
2.8field-weighted citation impact, top 8% of its field
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

17 citing papers in PubMed, 29 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. A Hypothesized Therapeutic Role of (Z)-Endoxifen in Duchenne Muscular Dystrophy (DMD).Degenerative neurological and neuromuscular disease · 2025
    Article
  6. Article
  7. Review
  8. Article
  9. Article
  10. Article
  11. Tamoxifen evolution.British journal of cancer · 2023
    Review
  12. Article
  13. Review
  14. Review
  15. Review
  16. Review
  17. Article
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

4 authors at 2 institutions in 1 country.

Swaathi JayaramanDepartment of Oncology, Mayo Clinic, Rochester, MN 55905, USA.ORCID 0000-0002-5451-0052
Joel M ReidDepartment of Oncology, Mayo Clinic, Rochester, MN 55905, USA.ORCID 0000-0003-2872-3123
John R HawseDepartment of Biochemistry and Molecular Biology, Mayo Clinic, Rochester, MN 55905, USA.ORCID 0000-0003-3406-470X
Matthew P GoetzDepartment of Oncology, Mayo Clinic, Rochester, MN 55905, USA.ORCID 0000-0002-4383-270X
Mayo Clinic · USMayo Clinic in Arizona · US

Funding

Women's Cancer ProgramP30CA015083 · NCI · MAYO CLINIC ROCHESTER · PI AKHILESH PANDEY · 1985 to 2026
$151.3M
The Role of CHFR in Tumorigenesis and Paclitaxel-Sensitivity in Breast CancerP50CA116201 · NCI · MAYO CLINIC ROCHESTER · PI Fergus Joseph Couch · 2005 to 2026
$49.9M
NCI NIH HHS P30 CA015083NCI NIH HHS P50 CA116201
6 · The paper itself

Abstract

The selective estrogen receptor (ER) modulator, tamoxifen, is the only endocrine agent with approvals for both the prevention and treatment of premenopausal and postmenopausal estrogen-receptor positive breast cancer as well as for the treatment of male breast cancer. Endoxifen, a secondary metabolite resulting from CYP2D6-dependent biotransformation of the primary tamoxifen metabolite, N-desmethyltamoxifen (NDT), is a more potent antiestrogen than either NDT or the parent drug, tamoxifen. However, endoxifen's antitumor effects may be related to additional molecular mechanisms of action, apart from its effects on ER. In phase 1/2 clinical studies, the efficacy of Z-endoxifen, the active isomer of endoxifen, was evaluated in patients with endocrine-refractory metastatic breast cancer as well as in patients with gynecologic, desmoid, and hormone-receptor positive solid tumors, and demonstrated substantial oral bioavailability and promising antitumor activity. Apart from its potent anticancer effects, Z-endoxifen appears to result in similar or even greater bone agonistic effects while resulting in little or no endometrial proliferative effects compared with tamoxifen. In this review, we summarize the preclinical and clinical studies evaluating endoxifen in the context of breast and other solid tumors, the potential benefits of endoxifen in bone, as well as its emerging role as an antimanic agent in bipolar disorder. In total, the summarized body of literature provides compelling arguments for the ongoing development of Z-endoxifen as a novel drug for multiple indications.

Indexed as

AnimalsBone and BonesBreast NeoplasmsCell ProliferationEstrogen AntagonistsFemaleHumansMolecular Targeted TherapyReceptors, EstrogenSelective Estrogen Receptor ModulatorsTamoxifen4-hydroxy-N-desmethyltamoxifenEstrogen AntagonistsReceptors, EstrogenSelective Estrogen Receptor ModulatorsTamoxifenantiestrogenbreast cancerCYP2D6endoxifenhormone therapytamoxifen

Identifiers

PMID34480554
PMCPMC8787422
OpenAlexW3197078919

What OpenQuestion holds

Textmetadata
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.