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Novel Endocrine Therapies: Current Status and Future Directions

Elena Brierley-Green1, Niharika Duggirala1, Kelly E McCann1

  • 1Department of Medicine, Division of Hematology-Oncology, UCLA David Geffen School of Medicine, Los Angeles, CA.

Clinical Breast Cancer
|August 22, 2026
PubMed

Insights

Novel oral agents targeting estrogen receptor signaling show promise for ER+/HER2- breast cancer. This review covers selective estrogen receptor degraders (SERDs) and other targeted therapies, exploring their efficacy and tolerability.

Area of Science:

  • Endocrinology
  • Oncology
  • Pharmacology

Background:

  • Estrogen receptor-positive, HER2-negative (ER+/HER2-) breast cancer remains a significant clinical challenge.
  • Endocrine therapy targeting estrogen receptor signaling is a cornerstone of treatment.
  • Recent advancements have introduced novel oral agents with improved mechanisms of action.

Purpose of the Study:

  • To review the latest clinical findings on novel oral agents for ER+/HER2- breast cancer.
  • To explore the mechanisms, efficacy, and tolerability of these emerging therapies.
  • To assess their potential impact on treatment outcomes in both metastatic and early-stage disease.

Main Methods:

  • Review of clinical trials for FDA-approved and emerging oral agents.
  • Analysis of selective estrogen receptor degraders (SERDs), proteolysis-targeting chimeras (PROTACs), and other targeted therapies.
  • Exploration of mechanisms of action, clinical efficacy, and safety profiles.

Main Results:

  • FDA-approved oral SERDs like elacestrant and imlunestrant demonstrate clinical activity.
  • The novel PROTAC vepdegestrant shows promise in early trials.
  • Emerging oral SERDs, PROTACs, complete estrogen receptor antagonists, and SERCAs are under investigation.

Conclusions:

  • Novel oral agents targeting estrogen receptor signaling offer new therapeutic avenues for ER+/HER2- breast cancer.
  • These agents, including SERDs and PROTACs, exhibit varying efficacy and tolerability profiles.
  • Further research is warranted to optimize their use in managing both advanced and early-stage disease.
Keywords:
Endocrine therapyEstrogen-receptor positive breast cancerHormone receptor-positiveNovel SERDsTargeted therapy

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