Amcenestrant - Misplaced Pages

Chemical compound

Pharmaceutical compound

Amcenestrant
Identifiers

IUPAC name 6-(2,4-dichlorophenyl)-5-oxyphenyl]-8,9-dihydro-7H-benzoannulene-2-carboxylic acid
CAS Number	2114339-57-8
PubChem CID	130232326
DrugBank	DB17864
ChemSpider	76117729
UNII	TBF1NHY02O
KEGG	D12145
ChEMBL	ChEMBL4475463
Chemical and physical data
Formula	C₃₁H₃₀Cl₂FNO₃
Molar mass	554.48 g·mol
3D model (JSmol)	Interactive image
SMILES C1CC2=C(C=CC(=C2)C(=O)O)C(=C(C1)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)O5CCN(C5)CCCF
InChI InChI=InChI=1S/C31H30Cl2FNO3/c32-23-8-12-27(29(33)18-23)28-4-1-3-21-17-22(31(36)37)7-11-26(21)30(28)20-5-9-24(10-6-20)38-25-13-16-35(19-25)15-2-14-34/h5-12,17-18,25H,1-4,13-16,19H2,(H,36,37)/t25-/m0/s1 Key:KISZAGQTIXIVAR-VWLOTQADSA-N

Amcenestrant is a novel oral selective estrogen receptor degrader (SERD) that is being evaluated for the treatment of estrogen receptor-positive (ER+) breast cancer.

Phase III trial for breast cancer in Japan had started, but this trial has been discontinued.

References

Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, et al. (August 2021). "GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer". Journal of Medicinal Chemistry. 64 (16): 11841–11856. doi:10.1021/acs.jmedchem.1c00847. PMID 34251202.
"Amcenestrant - Sanofi". AdisInsight. Springer Nature Switzerland AG.

Gheysen M, Punie K, Wildiers H, Neven P (November 2024). "Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review". Cancer Treatment Reviews. 130: 102825. doi:10.1016/j.ctrv.2024.102825. PMID 39293125.
Guglielmi G, Del Re M, Gol LS, Bengala C, Danesi R, Fogli S (April 2024). "Pharmacological insights on novel oral selective estrogen receptor degraders in breast cancer". European Journal of Pharmacology. 969: 176424. doi:10.1016/j.ejphar.2024.176424. PMID 38402929.
Garcia-Fructuoso I, Gomez-Bravo R, Schettini F (November 2022). "Integrating new oral selective oestrogen receptor degraders in the breast cancer treatment". Current Opinion in Oncology. 34 (6): 635–642. doi:10.1097/CCO.0000000000000892. PMID 36000362.
Chen YC, Yu J, Metcalfe C, De Bruyn T, Gelzleichter T, Malhi V, et al. (June 2022). "Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer". Expert Opinion on Investigational Drugs. 31 (6): 515–529. doi:10.1080/13543784.2021.1983542. PMID 34694932.

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