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Drugs of the Future
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Drugs Fut 2016, 41(6): 361
ISSN 0377-8282
Copyright 2016 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2016.041.06.2482681
 
 
The role of selective estrogen receptor destabilizers (SERDs) in breast cancer therapy
Weatherman, R.V.
 
 
Hormonal therapy for the treatment of estrogen receptor-positive breast cancer represents one of the prominent successes of targeted cancer therapy. Selective estrogen receptor destabilizers (SERDs) are a class of hormonal therapy drugs that bind to estrogen receptor and cause its rapid degradation. Clinically, the most prominent SERD is fulvestrant, which is approved as a second-line therapy for advanced breast cancer. By being mechanistically distinct from the other two major hormonal therapy drug classes, selective estrogen receptor modulators (SERMs) and aromatase inhibitors, SERDs represent a third option of endocrine therapy that can potentially be effective even when the other therapies have failed. This review will compare SERDs to the other therapies targeted at estrogen signaling, discuss the development of new SERDs and highlight mechanistic and clinical evidence supporting the use of SERDs as a second-line and potentially first-line therapeutic, either alone or in combination with other agents.


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