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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]

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. ^ a b c Lee, Clara I; Goodwin, Annabel; Wilcken, Nicholas (3 January 2017). "Fulvestrant for hormone-sensitive metastatic breast cancer". Cochrane Database of Systematic Reviews. 2017 (1): CD011093. doi: 10.1002/14651858.CD011093.pub2. PMC  6464820. PMID  28043088.
  2. ^ a b Lai, Ashton C.; Crews, Craig M. (February 2017). "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. ^ Nalley, Catlin (5 February 2021). "Orally Bioavailable SERD Shows Promise in Certain Breast Cancer Patients". Oncology Times. 43 (3): 35. doi: 10.1097/01.COT.0000734348.58210.24.
  7. ^ Bardia, Aditya; Linden, Hannah M.; Ulaner, Gary A.; Chandarlapaty, Sarat; Gosselin, Alice; Celanovic, Marina; Campone, Mario (20 May 2019). "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. S2CID  190898194.


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