Evaluation of the androgen receptor in patients with ERα-positive early breast cancer treated with adjuvant tamoxifen ± fluoxymesterone

Breast Cancer Res. 2025 Mar 19;27(1):40. doi: 10.1186/s13058-025-01992-0.

Abstract

Background: Our goal was to evaluate the impact of level of androgen receptor (AR) expression on outcomes in women with estrogen receptor α (ER) positive breast cancer. We sought to corroborate our preclinical findings that AR-agonists were efficacious in patients with ER-positive tumors that also expressed high levels of AR.

Methods: Tissue microarrays (TMAs) were prepared from primary tumor blocks from patients entered on a prospective randomized adjuvant trial of tamoxifen (Tam) alone or combined with fluoxymesterone (Flu), an AR-agonist, (NCCTG 89-30-52). TMAs were stained for ER and AR and expression examined in decile increments (0-100%) of positive invasive tumor nuclei. The primary endpoint was relapse-free survival (RFS).

Results: 301 (59%) of the 514 patients had sufficient tissue to determine ER and AR expression, where nuclear staining of > 70% was considered "enriched" and nuclear staining of ≤ 70% was considered "poor/moderate". Eleven (4%) of these patients had poor/moderate ER staining and were excluded from these analyses. The proportion of the ER-enriched tumors that also had AR-enriched expression levels was 56.3% in the Tam arm and 51.8% in the Tam + Flu arm. Within the AR-enriched patients, the cumulative incidence of RFS events showed an advantage for Tam + Flu over Tam alone that reached significance (Gray's test p = 0.0472).

Conclusions: Our findings suggest that an AR-agonist may be of value in AR-enriched, ER-enriched breast cancers and should be studied in future trials because of the availability of new, more tolerable AR-agonists.

Keywords: Androgen receptor; Estrogen receptor; Fluoxymesterone; Tamoxifen.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Agents, Hormonal / therapeutic use
  • Antineoplastic Combined Chemotherapy Protocols* / therapeutic use
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / metabolism
  • Breast Neoplasms* / mortality
  • Breast Neoplasms* / pathology
  • Chemotherapy, Adjuvant
  • Estrogen Receptor alpha* / genetics
  • Estrogen Receptor alpha* / metabolism
  • Female
  • Humans
  • Middle Aged
  • Receptors, Androgen* / genetics
  • Receptors, Androgen* / metabolism
  • Tamoxifen / administration & dosage
  • Tamoxifen / therapeutic use
  • Tissue Array Analysis
  • Treatment Outcome

Substances

  • Receptors, Androgen
  • Tamoxifen
  • Estrogen Receptor alpha
  • ESR1 protein, human
  • AR protein, human
  • Antineoplastic Agents, Hormonal