Английская Википедия:Etacstil
Шаблон:Short description Шаблон:Infobox drug
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 Duke University, Glaxo Wellcome, and later, Dupont.[12][13] In 2001, 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
Шаблон:Estrogen receptor modulators
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite web
- ↑ 3,0 3,1 Шаблон:Cite journal
- ↑ Antiestrogen GW5638 induces a unique structural change in the ER. The biological significance of this conformational change was revealed in studies that demonstrated that tamoxifen-resistant breast tumor explants are not cross-resistant to GW5638. Because of these properties, this drug is currently being developed as a potential therapeutic for tamoxifen-resistant breast cancers.Шаблон:Cite journal
- ↑ Шаблон:Cite web
- ↑ 6,0 6,1 Шаблон:Cite web
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 9,0 9,1 9,2 Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 11,0 11,1 Шаблон:Cite journal
- ↑ 12,0 12,1 Шаблон:Cite web
- ↑ Шаблон:Cite journal
- Английская Википедия
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- Drugs developed by GSK plc
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