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Review

Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective

1
Hospital Clínico de València, Instituto de Investigación INCLIVA, 46010 Valencia, Spain
2
Centro de Investigación Biomédica en Red de Oncología, CIBERONC-ISCIII, 28029 Madrid, Spain
3
Departamento de Fisiología, Universidad de València, 46010 Valencia, Spain
*
Authors to whom correspondence should be addressed.
Academic Editor: Roberta Tarallo
Int. J. Mol. Sci. 2021, 22(15), 7812; https://doi.org/10.3390/ijms22157812
Received: 29 June 2021 / Revised: 15 July 2021 / Accepted: 19 July 2021 / Published: 22 July 2021
Estrogen receptor-positive (ER+) is the most common subtype of breast cancer. Endocrine therapy is the fundamental treatment against this entity, by directly or indirectly modifying estrogen production. Recent advances in novel compounds, such as cyclin-dependent kinase 4/6 inhibitors (CDK4/6i), or phosphoinositide 3-kinase (PI3K) inhibitors have improved progression-free survival and overall survival in these patients. However, some patients still develop endocrine resistance after or during endocrine treatment. Different underlying mechanisms have been identified as responsible for endocrine treatment resistance, where ESR1 gene mutations are one of the most studied, outstanding from others such as somatic alterations, microenvironment involvement and epigenetic changes. In this scenario, selective estrogen receptor degraders/downregulators (SERD) are one of the weapons currently in research and development against aromatase inhibitor- or tamoxifen-resistance. The first SERD to be developed and approved for ER+ breast cancer was fulvestrant, demonstrating also interesting activity in ESR1 mutated patients in the second line treatment setting. Recent investigational advances have allowed the development of new oral bioavailable SERDs. This review describes the evolution and ongoing studies in SERDs and new molecules against ER, with the hope that these novel drugs may improve our patients’ future landscape. View Full-Text
Keywords: SERD; breast cancer; endocrine therapy; hormone therapy; luminal breast cancer SERD; breast cancer; endocrine therapy; hormone therapy; luminal breast cancer
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MDPI and ACS Style

Hernando, C.; Ortega-Morillo, B.; Tapia, M.; Moragón, S.; Martínez, M.T.; Eroles, P.; Garrido-Cano, I.; Adam-Artigues, A.; Lluch, A.; Bermejo, B.; Cejalvo, J.M. Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective. Int. J. Mol. Sci. 2021, 22, 7812. https://doi.org/10.3390/ijms22157812

AMA Style

Hernando C, Ortega-Morillo B, Tapia M, Moragón S, Martínez MT, Eroles P, Garrido-Cano I, Adam-Artigues A, Lluch A, Bermejo B, Cejalvo JM. Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective. International Journal of Molecular Sciences. 2021; 22(15):7812. https://doi.org/10.3390/ijms22157812

Chicago/Turabian Style

Hernando, Cristina, Belén Ortega-Morillo, Marta Tapia, Santiago Moragón, María T. Martínez, Pilar Eroles, Iris Garrido-Cano, Anna Adam-Artigues, Ana Lluch, Begoña Bermejo, and Juan M. Cejalvo 2021. "Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective" International Journal of Molecular Sciences 22, no. 15: 7812. https://doi.org/10.3390/ijms22157812

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