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A Preoperative Window-of-Opportunity Study of Oral SERD, Imlunestrant, in Newly Diagnosed ER-Positive, HER2-Negative Early Breast Cancer: Results from the EMBER-2 Study.
Clin Cancer Res
December 2024
Medical Oncology Department, Breast Cancer Unit, University Hospital 12 de Octubre, Madrid, Spain.
Article Synopsis
- Imlunestrant is a new pill for treating a type of breast cancer, and researchers looked at how well it works and its safety.
- In a study, women with a specific type of breast cancer took either 400mg or 800mg of the pill for two weeks before surgery, and more tests were done with a 200mg dose.
- The results showed that the 400mg dose worked well and had fewer side effects, making it the best choice for treating patients in this study.
Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review.
Cancer Treat Rev
November 2024
Department of Gynecology and Obstetrics and Multidisciplinary Breast Centre, University Hospitals Leuven, Herestraat 49, 3000 Leuven, Belgium.
Article Synopsis
- Primary and acquired endocrine resistance complicates treatment for hormone receptor positive breast cancer, often due to mutations in estrogen receptor 1 (ESR1) that cause estrogen-independent activation.
- Selective estrogen receptor degraders (SERDs) are a new class of drugs that can degrade the ESR1 receptor, showing promise against this resistance, particularly in oral formulations that are more potent than the original intramuscular drug, fulvestrant.
- Clinical trials, like the EMERALD trial for elacestrant and SERENA-2 for camizestrant, showed improved progression-free survival (PFS), particularly after prior treatments, while other SERDs like giredestrant and amcenestrant did not demonstrate this benefit
Imlunestrant, an Oral Selective Estrogen Receptor Degrader, as Monotherapy and in Combination With Targeted Therapy in Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Phase Ia/Ib EMBER Study.
J Clin Oncol
December 2024
START Center for Cancer Care, San Antonio, TX.
Purpose: Imlunestrant is a next-generation oral selective estrogen receptor (ER) degrader designed to deliver continuous ER target inhibition, including in mutant breast cancer. This phase Ia/b trial determined the recommended phase II dose (RP2D), safety, pharmacokinetics, and efficacy of imlunestrant, as monotherapy and in combination with targeted therapy, in ER-positive (ER+) advanced breast cancer (ABC) and endometrial endometrioid cancer. The ER+/human epidermal growth factor receptor 2-negative (HER2-) ABC experience is reported here.
View Article and Find Full Text PDFPharmacological insights on novel oral selective estrogen receptor degraders in breast cancer.
Eur J Pharmacol
April 2024
Clinical Pharmacology and Pharmacogenetics Unit, Department of Clinical and Experimental Medicine, University of Pisa, Pisa, Italy.
Article Synopsis
- - The treatment landscape for estrogen receptor (ER)-positive breast cancer includes various endocrine therapies like aromatase inhibitors, selective estrogen receptor modulators, and the recently approved selective estrogen receptor degraders (SERDs) like Fulvestrant.
- - Elacestrant is the first oral SERD approved by the FDA for specific cases of advanced breast cancer in postmenopausal women who have already undergone other treatments.
- - Current clinical trials are exploring additional oral SERDs, like amcenestrant and giredestrant, paving the way for new therapeutic options in managing ER-positive breast cancer.
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