Selective estrogen receptor degrader

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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.[1] 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.[1]

As of 2016 the only marketed SERD was fulvestrant.[1] As of November 2016 other SERDs under development includes brilanestrant and elacestrant.[2] The clinical success of fulvestrant led to efforts to discover and develop a parallel drug class of selective androgen receptor degraders (SARDs).[2]

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  1. ^ a b c 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.
  2. ^ a b 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.