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

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dc.contributor.authorDownton, T.
dc.contributor.authorZhou, F.
dc.contributor.authorSegara, D.
dc.contributor.authorJeselsohn, R.
dc.contributor.authorLim, E.
dc.date.issued2022
dc.description.abstractSeveral endocrine therapies are currently available for the treatment of estrogen receptor (ER) positive breast cancer, but the clinical benefit of these agents is limited by endocrine therapy drug resistance. A common mechanism of endocrine therapy resistance is ESR1 mutations. The first-generation selective estrogen receptor degrader (SERD) fulvestrant has activity against ESR1 mutant tumors but requires intramuscular injection and has poor bioavailability that precludes optimal drug dosing. This led to the development of second-generation SERDs which are potent and have improved oral bioavailability and pharmacokinetics. Several of these oral SERDs are now in phase III trials in both the early and advanced ER positive breast cancer settings. This review summarizes the background of oral SERD development, the current status and future perspectives.
dc.description.statementofresponsibilityTeesha Downton, Fiona Zhou, Davendra Segara, Rinath Jeselsohn, Elgene Lim
dc.identifier.citationDrug Design, Development and Therapy, 2022; 16:2933-2948
dc.identifier.doi10.2147/dddt.s380925
dc.identifier.issn1177-8881
dc.identifier.issn1177-8881
dc.identifier.orcidZhou, F. [0000-0003-3113-1671]
dc.identifier.urihttps://hdl.handle.net/2440/146446
dc.language.isoen
dc.publisherDove Medical Press
dc.rights© 2022 Downton et al. This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms. php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
dc.source.urihttps://doi.org/10.2147/dddt.s380925
dc.subjectselective estrogen receptor degraders; breast cancer; estrogen receptor
dc.subject.meshBreast
dc.subject.meshHumans
dc.subject.meshBreast Neoplasms
dc.subject.meshMouth Neoplasms
dc.subject.meshSelective Estrogen Receptor Modulators
dc.subject.meshReceptors, Estrogen
dc.subject.meshEstrogen Receptor alpha
dc.subject.meshFemale
dc.titleOral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status
dc.typeJournal article
pubs.publication-statusPublished online

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