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Oral Serd, a Novel Endocrine Therapy for Estrogen Receptor-Positive Breast Cancer Publisher



Neupane N1 ; Bawek S2 ; Gurusinghe S2 ; Ghaffary EM3 ; Mirmosayyeb O3 ; Thapa S4 ; Falkson C5 ; Oregan R5 ; Dhakal A5
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Authors Affiliations
  1. 1. Department of Internal Medicine, Rochester General Hospital, Rochester, 14621, NY, United States
  2. 2. Department of Internal Medicine, University at Buffalo, Buffalo, 14203, NY, United States
  3. 3. Isfahan Neurosciences Research Center, Isfahan University of Medical Sciences, Isfahan, 8174673461, Iran
  4. 4. Westchester Medical Center, New York Medical College, Valhalla, 10595, NY, United States
  5. 5. Department of Medicine, University of Rochester Medical Center, Rochester, 14642, NY, United States

Source: Cancers Published:2024


Abstract

Breast cancer is the most common cancer among women worldwide, and estrogen receptor-positive (ER+) breast cancer accounts for a significant proportion of cases. While various treatments are available, endocrine therapies are often the first-line treatment for this type of breast cancer. However, the development of drug resistance poses a significant challenge in managing this disease. ESR1 mutations have been identified as a common mechanism of endocrine therapy resistance in ER+ breast cancer. The first-generation selective estrogen receptor degrader (SERD) fulvestrant has shown some activity against ESR1 mutant tumors. However, due to its poor bioavailability and need for intramuscular injection, it may not be the optimal therapy for patients. Second-generation SERDs were developed to overcome these limitations. These newer drugs have improved oral bioavailability and pharmacokinetics, making them more convenient and effective for patients. Several oral SERDs are now in phase III trials for early and advanced ER+ breast cancer. This review summarizes the background of oral SERD development, the current status, and future perspectives. © 2024 by the authors.
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2. Recurrent Hyperactive Esr1 Fusion Proteins in Endocrine Therapy-Resistant Breast Cancer, Annals of Oncology (2018)
3. Frequent Esr1 and Cdk Pathway Copy-Number Alterations in Metastatic Breast Cancer, Molecular Cancer Research (2019)
4. Synthesis, Analysis and Biological Evaluation of Novel Steroidal Estrogenic Prodrugs for the Treatment of Breast Cancer, Pharmaceutical Biology (2004)
5. Clinically Observed Estrogen Receptor Alpha Mutations Within the Ligand-Binding Domain Confer Distinguishable Phenotypes, Oncology (Switzerland) (2018)
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