# Palazestrant

> Mediated Wiki article. Canonical URL: https://mediated.wiki/source/Palazestrant
> Markdown URL: https://mediated.wiki/source/Palazestrant.md
> Source: https://en.wikipedia.org/wiki/Palazestrant
> Source revision: 1347514976
> License: Creative Commons Attribution-ShareAlike 4.0 International (https://creativecommons.org/licenses/by-sa/4.0/)

{{Short description|Chemical compound}}
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| image             = Palazestrant.svg
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<!-- Identifiers -->
| CAS_number        = 2092925-89-6
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| PubChem           = 135351887
| PubChemSubstance  = 
| IUPHAR_ligand     = 
| DrugBank          = DB18971
| ChemSpiderID      = 128922074
| UNII              = VU35KM56Q4
| KEGG              = D12827
| ChEBI             = 
| ChEMBL            = 5314475
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| PDB_ligand        = 
| synonyms          = OP-1250

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| IUPAC_name        = <nowiki>(1R,3R)-2-(2-fluoro-2-methyl-propyl)-3-methyl-1-[4-(1-propylazetidin-3-yl)oxyphenyl]-1,3,4,9-tetrahydropyrido[3,4-b]indole</nowiki>
| C= 28
| H= 36
| F= 1
| N= 3
| O= 1
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| SMILES            = CCCN1CC(C1)OC2=CC=C(C=C2)[C@@H]3C4=C(C[C@H](N3CC(C)(C)F)C)C5=CC=CC=C5N4
| Jmol              = 
| StdInChI          = 1S/C28H36FN3O/c1-5-14-31-16-22(17-31)33-21-12-10-20(11-13-21)27-26-24(23-8-6-7-9-25(23)30-26)15-19(2)32(27)18-28(3,4)29/h6-13,19,22,27,30H,5,14-18H2,1-4H3/t19-,27-/m1/s1
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'''Palazestrant''' is an [investigational new drug](/source/investigational_new_drug) which is being evaluated for the treatment of estrogen receptor-positive (ER+) [breast cancer](/source/breast_cancer), with a dual mechanism of action as both a complete [estrogen receptor antagonist](/source/estrogen_receptor_antagonist) (CERAN) and a [selective estrogen receptor degrader](/source/selective_estrogen_receptor_degrader) (SERD). This orally bioavailable small molecule has demonstrated potent activity against both wild-type and mutant forms of the estrogen receptor.<ref name="Parisian_2024">{{cite journal | vauthors = Parisian AD, Barratt SA, Hodges-Gallagher L, Ortega FE, Peña G, Sapugay J, Robello B, Sun R, Kulp D, Palanisamy GS, Myles DC, Kushner PJ, Harmon CL | title = Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination | journal = Molecular Cancer Therapeutics | volume = 23 | issue = 3 | pages = 285–300 | date = March 2024 | pmid = 38102750 | pmc = 10911704 | doi = 10.1158/1535-7163.MCT-23-0351 }}</ref>

==See also==
* [Substituted β-carboline](/source/Substituted_%CE%B2-carboline)

== References ==
{{Reflist}}

{{Estrogen receptor modulators}}
{{Tryptamines}}

Category:Antineoplastic drugs
Category:Azetidines
Category:Organofluorides
Category:Phenol ethers
Category:Propyl compounds
Category:Selective estrogen receptor degraders
Category:Tryptolines

{{Antineoplastic-drug-stub}}

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