Chemistry: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 (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

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]

  • Giredestrant: Roche
  • Amcenestrant (SAR439859): Sanofi
  • Camizestrant (AZD9833): AstraZeneca
  • Rintodestrant ( G1T48 ) : G1 Therapeutics
  • LSZ102: Novartis
  • Imlunestrant (LY3484356): Eli Lilly
  • Elacestrant: Radius Health
  • ZN-c5: Zentalis
  • Taragarestrant (D-0502): Inventisbio
  • SHR9549: Jiangsu Hengrui Medicine
  • Vepdegestrant ( ARV-471 ): Oral estrogen receptor PROTAC protein degrader for breast cancer by Arvinas Pharmaceuticals.
  • ZB716 ( Fulvestrant boronic acid ).

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

References

  1. ↑ 1.0 1.1 1.2 Lee, CI; Goodwin, A; Wilcken, N (3 January 2017). "Fulvestrant for hormone-sensitive metastatic breast cancer.". The Cochrane Database of Systematic Reviews 1 (1): CD011093. doi:10.1002/14651858.CD011093.pub2. PMID 28043088. 
  2. ↑ 2.0 2.1 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. PMID 27885283. 
  3. ↑ "Injection-Site Pain With Large-Volume Intramuscular Injection of Fulvestrant Can Be Minimized" (in en). https://www.practiceupdate.com/content/injection-site-pain-with-large-volume-intramuscular-injection-of-fulvestrant-can-be-minimized/52698. 
  4. ↑ "A blockbuster breast cancer niche has Roche and Sanofi in the lead" (in en). 2020-02-19. https://www.evaluate.com/vantage/articles/news/corporate-strategy/blockbuster-breast-cancer-niche-has-roche-and-sanofi-lead. 
  5. ↑ "Rintodestrant | oral selective estrogen receptor degrader (SERD) | G1 Therapeutics, Inc.". https://www.g1therapeutics.com/pipeline/rintodestrant/. 
  6. ↑ "Orally Bioavailable SERD Shows Promise in Certain Breast Cancer Patients". http://know.lww.com/nsclc/sabcsarticles/bioavailable-serd.html. 
  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. https://ascopubs.org/doi/abs/10.1200/JCO.2019.37.15_suppl.TPS1105. 




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