Amcenestrant

Amcenestrant
Identifiers
	IUPAC name 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid;
CAS Number	2114339-57-8;
PubChem CID	130232326;
IUPHAR/BPS	10566;
DrugBank	DB17864;
ChemSpider	76117729;
UNII	TBF1NHY02O;
KEGG	D12145;
ChEMBL	ChEMBL4475463;
PDB ligand	L5B (PDBe, RCSB PDB);
Chemical and physical data
Formula	C31H30Cl2FNO3
Molar mass	554.48 g·mol−1
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)O[C@H]5CCN(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.^[1]

Phase III trial for breast cancer in Japan had started, but this trial has been discontinued.^[2]

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. hdl:2434/1128718. 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.