Selective estrogen receptor degrader
Not to be confused with Selective estrogen receptor modulator.
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]
See also
References
- 1 2 3 Lee, CI; Goodwin, A; Wilcken, N (3 January 2017). "Fulvestrant for hormone-sensitive metastatic breast cancer.". The Cochrane database of systematic reviews. 1: CD011093. PMID 28043088. doi:10.1002/14651858.CD011093.pub2.
- 1 2 Lai, AC; Crews, CM (25 November 2016). "Induced protein degradation: an emerging drug discovery paradigm.". Nature Reviews. Drug Discovery. PMID 27885283. doi:10.1038/nrd.2016.211.
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