Jump to content

Palazestrant

Palazestrant
Clinical data
Other namesOP-1250
Identifiers
  • (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
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC28H36FN3O
Molar mass449.614 g·mol−1
3D model (JSmol)
  • 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=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

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

  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.
Stub icon

This pharmacology-related article is a stub. You can help Wik.ipedia.Pro by expanding it.

Retrieved from "https://en.Wik.ipedia.Pro.org/w/index.php?title=Palazestrant&oldid=1255310466"

See what we do next...

OR

By submitting your email or phone number, you're giving mschf permission to send you email and/or recurring marketing texts. Data rates may apply. Text stop to cancel, help for help.

Success: You're subscribed now !