Selective estrogen receptor degrader

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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 (brand name Faslodex).[1] As of November 2016 other SERDs under development include 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]

Investigational[]

See also: List of investigational sex-hormonal agents § Estrogenics

Fulvestrant requires large-volume and frequently painful intramuscular injections.[3] In response, pharmaceutical companies are currently developing oral SERDs. Among products in development are:[4]

  • : Roche
  • (SAR439859): Sanofi
  • : AstraZeneca
  • : G1 Therapeutics
  • : Novartis
  • : Eli Lilly
  • Elacestrant: Radius Health
  • : Zentalis
  • : Inventisbio
  • : Jiangsu Hengrui Medicine

The oral SERDs target ER-positive/HER2-negative breast cancer and are tested as monotherapy and in combination with other drugs such as the CDK inhibitor palbociclib (Ibrance).[5][6][7]

See also[]

  • Aromatase inhibitor
  • Estrogen deprivation therapy

References[]

  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. PMC 6464820. 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 (2): 101–114. doi:10.1038/nrd.2016.211. PMC 5684876. PMID 27885283.
  3. ^ "Injection-Site Pain With Large-Volume Intramuscular Injection of Fulvestrant Can Be Minimized". PracticeUpdate. Retrieved 2020-12-28.
  4. ^ "A blockbuster breast cancer niche has Roche and Sanofi in the lead". Evaluate.com. 2020-02-19. Retrieved 2020-12-28.
  5. ^ "Rintodestrant | oral selective estrogen receptor degrader (SERD) | G1 Therapeutics, Inc". www.g1therapeutics.com. Retrieved 2021-01-09.
  6. ^ "Orally Bioavailable SERD Shows Promise in Certain Breast Cancer Patients". know.lww.com. Retrieved 2021-01-09.
  7. ^ Bardia, Aditya; Linden, Hannah M.; Ulaner, Gary A.; Chandarlapaty, Sarat; Gosselin, Alice; Celanovic, Marina; Campone, Mario (2019-05-20). "Phase 1/2 dose-escalation and expansion study investigating SAR439859 +/- palbociclib in postmenopausal women with estrogen receptor-positive (ER+)/HER2- metastatic breast cancer". Journal of Clinical Oncology. 37 (15_suppl): TPS1105. doi:10.1200/JCO.2019.37.15_suppl.TPS1105. ISSN 0732-183X.


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