# Rintodestrant

> Mediated Wiki article. Canonical URL: https://mediated.wiki/source/Rintodestrant
> Markdown URL: https://mediated.wiki/source/Rintodestrant.md
> Source: https://en.wikipedia.org/wiki/Rintodestrant
> Source revision: 1344916407
> License: Creative Commons Attribution-ShareAlike 4.0 International (https://creativecommons.org/licenses/by-sa/4.0/)

{{Short description|Chemical compound}}
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| CAS_number        = 2088518-51-6
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| PubChem           = 129205616
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| IUPHAR_ligand     = 
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| ChemSpiderID      = 76743881
| UNII              = W3Y784Y0ES
| KEGG              = D11736
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| ChEMBL            = 4059888
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| PDB_ligand        = 
| synonyms          = G1T48

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| IUPAC_name        = <nowiki>(E)-3-[4-[2-(4-fluoro-2,6-dimethyl-benzoyl)-6-hydroxy-benzothiophen-3-yl]oxyphenyl]prop-2-enoic acid</nowiki>
| C= 26
| H= 19
| F= 1
| O= 5
| S= 1
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| SMILES            = CC1=CC(=CC(=C1C(=O)C2=C(C3=C(S2)C=C(C=C3)O)OC4=CC=C(C=C4)/C=C/C(=O)O)C)F
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'''Rintodestrant (G1T48)''' is an orally bioavailable [selective estrogen receptor degrader](/source/selective_estrogen_receptor_degrader) (SERD) discovered in Greg Thatcher's lab at UIC<ref>{{cite journal | vauthors = Xiong R, Zhao J, Gutgesell LM, Wang Y, Lee S, Karumudi B, Zhao H, Lu Y, Tonetti DA, Thatcher GR | title = Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer | journal = Journal of Medicinal Chemistry | volume = 60 | issue = 4 | pages = 1325–1342 | date = February 2017 | pmid = 28117994 | doi = 10.1021/acs.jmedchem.6b01355 | pmc = 5786431 }}</ref> and developed by [G1 Therapeutics](/source/G1_Therapeutics) for the treatment of estrogen receptor-positive (ER+) [breast cancer](/source/breast_cancer).<ref>{{cite journal | vauthors = Andreano KJ, Wardell SE, Baker JG, Desautels TK, Baldi R, Chao CA, Heetderks KA, Bae Y, Xiong R, Tonetti DA, Gutgesell LM, Zhao J, Sorrentino JA, Thompson DA, Bisi JE, Strum JC, Thatcher GR, Norris JD | title = G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer | journal = Breast Cancer Research and Treatment | volume = 180 | issue = 3 | pages = 635–646 | date = April 2020 | pmid = 32130619 | doi = 10.1007/s10549-020-05575-9 | pmc = 7103015 }}</ref> Structurally inspired by the 6-OH-[benzothiophene](/source/benzothiophene) scaffold used in [arzoxifene](/source/arzoxifene) and [raloxifene](/source/raloxifene), rintodestrant selectively binds to the [estrogen receptor](/source/estrogen_receptor) and inhibits ER signaling, demonstrating efficacy in endocrine-resistant tumors.<ref name="Gheysen_2024">{{cite journal | vauthors = Gheysen M, Punie K, Wildiers H, Neven P | title = Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review | journal = Cancer Treatment Reviews | volume = 130 | issue =  | article-number = 102825 | date = November 2024 | pmid = 39293125 | doi = 10.1016/j.ctrv.2024.102825 | doi-access = free }}</ref>

A phase I clinical trial evaluated rintodestrant as monotherapy and in combination with the CDK4/6 inhibitor [palbociclib](/source/palbociclib) in patients with ER+/HER2- advanced breast cancer.<ref>{{ClinicalTrialsGov|NCT03455270|G1T48, an Oral SERD, Alone and in Combination With Palbociclib in ER-Positive, HER2-Negative Advanced Breast Cancer}}</ref>

== References ==
{{Reflist}}

Category:Antineoplastic drugs
Category:Selective estrogen receptor degraders
Category:Diaryl ethers
Category:Benzothiophenes
Category:Enoic acids
Category:Fluorobenzene derivatives
Category:Ketones
Category:Phenols

{{antineoplastic-drug-stub}}

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Adapted from the Wikipedia article [Rintodestrant](https://en.wikipedia.org/wiki/Rintodestrant) by Wikipedia contributors ([contributor history](https://en.wikipedia.org/wiki/Rintodestrant?action=history)). Available under [Creative Commons Attribution-ShareAlike 4.0 International](https://creativecommons.org/licenses/by-sa/4.0/). Changes may have been made.