Palazestrant

Palazestrant
Clinical data
Other names	OP-1250
Identifiers
	IUPAC name (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;
CAS Number	2092925-89-6 ;
PubChem CID	135351887 ;
DrugBank	DB18971 ;
ChemSpider	128922074 ;
UNII	VU35KM56Q4 ;
KEGG	D12827 ;
ChEMBL	ChEMBL5314475 ;
Chemical and physical data
Formula	C28H36FN3O
Molar mass	449.614 g·mol−1
3D model (JSmol)	Interactive image ;
	SMILES CCCN1CC(C1)OC2=CC=C(C=C2)[C@@H]3C4=C(C[C@H](N3CC(C)(C)F)C)C5=CC=CC=C5N4;
	InChI InChI=InChI=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; Key:LBSFUBLFDCAEKV-XHCCPWGMSA-N;

Last updated June 29, 2025

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.^[1]

References

↑ Parisian AD, Barratt SA, Hodges-Gallagher L, Ortega FE, Peña G, Sapugay J, et al. (March 2024). "Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination". Molecular Cancer Therapeutics. 23 (3): 285–300. doi:10.1158/1535-7163.MCT-23-0351. PMC 10911704 . PMID 38102750.

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[Parisian_2024-1] Parisian AD, Barratt SA, Hodges-Gallagher L, Ortega FE, Peña G, Sapugay J, et al. (March 2024). "Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination". Molecular Cancer Therapeutics. 23 (3): 285–300. doi:10.1158/1535-7163.MCT-23-0351. PMC 10911704 . PMID 38102750.

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