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Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status

Teesha Downton1,2, Fiona Zhou1,2, Davendra Segara1

  • 1Garvan Institute of Medical Research, Sydney, NSW, Australia.

Drug Design, Development and Therapy
|September 9, 2022
PubMed

Insights

New oral SERDs offer improved treatment options for ER-positive breast cancer resistant to endocrine therapy. These drugs target ESR1 mutations, overcoming limitations of older injectable therapies.

Area of Science:

  • Oncology
  • Endocrinology
  • Pharmacology

Background:

  • Endocrine therapies are standard for ER-positive breast cancer.
  • Drug resistance, often due to ESR1 mutations, limits treatment efficacy.
  • Fulvestrant, a first-generation SERD, has limitations including injection and poor bioavailability.

Purpose of the Study:

  • To review the development of oral selective estrogen receptor degraders (SERDs).
  • To summarize the current status of oral SERDs in clinical trials.
  • To discuss future perspectives for oral SERD therapy in breast cancer.

Main Methods:

  • Literature review of preclinical and clinical studies on oral SERDs.
  • Analysis of pharmacokinetic and pharmacodynamic data.
  • Evaluation of clinical trial outcomes for oral SERDs in ER-positive breast cancer.

Main Results:

  • Second-generation oral SERDs demonstrate potent activity against ESR1 mutations.
  • These agents show improved oral bioavailability and pharmacokinetics compared to fulvestrant.
  • Several oral SERDs are advancing through Phase III trials for early and advanced breast cancer.

Conclusions:

  • Oral SERDs represent a significant advancement in treating endocrine-resistant ER-positive breast cancer.
  • Improved dosing and efficacy are expected with oral SERD formulations.
  • Ongoing trials will define the role of oral SERDs in breast cancer management.
Keywords:
breast cancerestrogen receptorselective estrogen receptor degraders

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