Etacstil

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Etacstil
Identifiers
  • (2E)-3-{4-[(1Z)-1,2-Diphenyl-1-buten-1-yl]phenyl}acrylic acid
JSmol)
  • CC/C(=C(\c1ccccc1)/c2ccc(cc2)/C=C/C(=O)O)/c3ccccc3
  • InChI=1S/C25H22O2/c1-2-23(20-9-5-3-6-10-20)25(21-11-7-4-8-12-21)22-16-13-19(14-17-22)15-18-24(26)27/h3-18H,2H2,1H3,(H,26,27)/b18-15+,25-23-
  • Key:HJQQVNIORAQATK-DDJBQNAASA-N

Etacstil (developmental code names GW-5638, DPC974) is an orally active, nonsteroidal, combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was developed for the treatment of estrogen receptor-positive breast cancer.[1][2][3] It was shown to overcome antiestrogen (tamoxifen, aromatase inhibitor, fulvestrant) resistance in breast cancer by altering the shape of the estrogen receptor, thus exhibiting SERD properties.[4][5][6][7][8] Etacstil is a tamoxifen derivative and one of the first drugs to overcome tamoxifen-resistance. It is the predecessor of GW-7604,[3][9][10] of which etacstil is a prodrug (GW-7604 being the 4-hydroxy metabolite of etacstil).[11] This is analogous to the case of tamoxifen being a prodrug of afimoxifene (4-hydroxytamoxifen).[11]

Etacstil was developed in the early 1990s by

Bristol Myers-Squibb (BMS) acquired Dupont, and for non-scientific, corporate reasons, closed the trial and abandoned the release of etacstil and its metabolite GW-7604.[6][9][12]

After many dormant years, a recent resurgence of interest in SERDs has led to the development of brilanestrant, a structural analogue of etacstil.[9]

See also

References

  1. ISBN 9781592597680
    .
  2. ^ "GW 5638 Profile". AdisInsight. Springer Nature Switzerland AG.
  3. ^
    doi:10.1621/B4A9CIQ78V
    .
  4. PMID 11306468
    .
  5. ^ "GW5638 uniquely alters the shape of the estrogen receptor". The Ben May Department for Cancer Research. The University of Chicago. 2015. Archived from the original on 10 October 2015.
  6. ^ a b "Tamoxifen-like drug suggests new ways to selectively block estrogen". The University of Chicago Medical Center. 12 May 2005. Archived from the original on 2018-03-27. Retrieved 2016-10-25.
  7. PMID 12060645
    .
  8. S2CID 35414830
    .
  9. ^
    PMID 26162914
    .
  10. PMID 11159857
    .
  11. ^
    PMID 11159857
    .
  12. ^ a b "Osteoporosis Drug Bazedoxifene Stops Growth Of Breast Cancer Cells". Medical News Today. 17 June 2013. Archived from the original on 8 January 2014.
  13. PMID 8201587
    .
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