Selective estrogen receptor degrader
A selective estrogen receptor degrader or downregulator (SERD) is a type of drug which binds to the estrogen receptor (ER) and, in the process of doing so, causes the ER to be degraded and thus downregulated. They are used to treat estrogen receptor-sensitive or progesterone receptor-sensitive breast cancer, along with older classes of drugs like selective estrogen receptor modulators (SERMs) and aromatase inhibitors.
As of 2016 the only marketed SERD was fulvestrant. As of November 2016 other SERDs under development includes brilanestrant and elacestrant. The clinical success of fulvestrant led to efforts to discover and develop a parallel drug class of selective androgen receptor degraders (SARDs).
- Lee, CI; Goodwin, A; Wilcken, N (3 January 2017). "Fulvestrant for hormone-sensitive metastatic breast cancer". The Cochrane Database of Systematic Reviews. 1: CD011093. doi:10.1002/14651858.CD011093.pub2. PMID 28043088.
- Lai, AC; Crews, CM (25 November 2016). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews. Drug Discovery. 16: 101–114. doi:10.1038/nrd.2016.211. PMC 5684876. PMID 27885283.
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