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Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
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Accelerating drug development in breast cancer: New frontiers for ER inhibition

Emanuela Ferraro1, Elaine M Walsh2, Jacqueline J Tao3

  • 1Breast Medicine Service, Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, NY, USA.

Cancer Treatment Reviews
|July 15, 2022
PubMed

Insights

Targeting estrogen receptor (ER) signaling is key for hormone receptor-positive breast cancer. Newer oral ER inhibitors and combination therapies offer improved efficacy and administration for better treatment outcomes.

Area of Science:

  • Oncology
  • Endocrinology
  • Pharmacology

Background:

  • Estrogen receptor (ER) signaling drives proliferation, tumorigenesis, and progression in breast cancers.
  • Hormone receptor-positive (HR+) breast cancer is successfully managed with endocrine therapy targeting ER signaling.
  • Established agents include selective estrogen receptor modulators (SERMs), selective estrogen receptor degraders (SERDs), and aromatase inhibitors (AIs).

Purpose of the Study:

  • To review the clinical development of SERDs and novel ER inhibitors.
  • To examine combination strategies for overcoming ER pathway escape.
  • To assess advantages of newer oral ER inhibitors and discuss future directions.

Main Methods:

  • Review of clinical development of SERDs and novel ER inhibitors.
  • Assessment of combination strategies involving CDK4/6 and PI3K inhibitors.
  • Evaluation of newer oral ER inhibitors' pharmacokinetic and efficacy profiles.

Main Results:

  • SERDs and novel ER inhibitors are advancing in clinical development.
  • Combination strategies show promise in overcoming endocrine resistance.
  • Newer oral ER inhibitors offer improved bioavailability, therapeutic index, administration, and efficacy.

Conclusions:

  • Targeting ER signaling remains a cornerstone in HR+ breast cancer treatment.
  • Novel oral ER inhibitors and combination therapies represent significant advancements.
  • Future research directions focus on optimizing these strategies for enhanced patient outcomes.
Keywords:
Breast cancerEstrogen receptor inhibitorsSERDs

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