{{Short description|Chemical compound}} {{cs1 config|name-list-style=vanc|display-authors=6}} {{Infobox drug | drug_name = | INN = | type = <!-- empty --> | image = Palazestrant.svg | image_class = skin-invert-image | width = 250px | alt = | caption = | image2 = | width2 = | alt2 = | caption2 = | imageL = | widthL = | altL = | imageR = | widthR = | altR = | captionLR =
<!-- Clinical data --> | pronounce = | tradename = | Drugs.com = | MedlinePlus = | licence_CA = <!-- Health Canada may use generic or brand name (generic name preferred) --> | licence_EU = <!-- EMA uses INN (or special INN_EMA) --> | DailyMedID = <!-- DailyMed may use generic or brand name (generic name preferred) --> | licence_US = <!-- FDA may use generic or brand name (generic name preferred) --> | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_AU_comment = | pregnancy_category= | dependency_liability = | addiction_liability = | routes_of_administration = | class = | ATCvet = | ATC_prefix = <!-- 'none' if uncategorised --> | ATC_suffix = | ATC_supplemental =
<!-- Legal status --> | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled --> | legal_AU_comment = | legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C5, D1, D2, E, F1, F2, F3, F4 --> | legal_BR_comment = | legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII --> | legal_CA_comment = | legal_DE = <!-- Anlage I, II, III or Unscheduled --> | legal_DE_comment = | legal_NZ = <!-- Class A, B, C --> | legal_NZ_comment = | legal_UK = <!-- GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD (Benz) POM, CD (Anab) POM or CD Inv POM / Class A, B, C --> | legal_UK_comment = | legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> | legal_US_comment = | legal_EU = | legal_EU_comment = | legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> | legal_UN_comment = | legal_status = <!-- For countries not listed above -->
<!-- Pharmacokinetic data --> | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action= | excretion =
<!-- Identifiers --> | CAS_number = 2092925-89-6 | CAS_supplemental = | PubChem = 135351887 | PubChemSubstance = | IUPHAR_ligand = | DrugBank = DB18971 | ChemSpiderID = 128922074 | UNII = VU35KM56Q4 | KEGG = D12827 | ChEBI = | ChEMBL = 5314475 | NIAID_ChemDB = | PDB_ligand = | synonyms = OP-1250
<!-- Chemical and physical data --> | 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 | molecular_weight = | 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 | StdInChI_comment = | StdInChIKey = LBSFUBLFDCAEKV-XHCCPWGMSA-N | density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }}
'''Palazestrant''' is an investigational new drug which is being evaluated for the treatment of estrogen receptor-positive (ER+) breast cancer, with a dual mechanism of action as both a complete estrogen receptor antagonist (CERAN) and a 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
== 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
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