Imlunestrant

Imlunestrant
Clinical data
Other names	LY3484356
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (5R)-5-[4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-8-(trifluoromethyl)-5H-chromeno[4,3-c]quinolin-2-ol;
CAS Number	2408840-26-4;
PubChem CID	146603228;
ChemSpider	115010421;
UNII	9CXQ3PF69U;
KEGG	D12216;
ChEMBL	ChEMBL5095183;
Chemical and physical data
Formula	C29H24F4N2O3
Molar mass	524.516 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1C(CN1CCOC2=CC=C(C=C2)[C@@H]3C4=C5C=CC(=CC5=NC=C4C6=C(O3)C=C(C=C6)C(F)(F)F)O)CF;
	InChI InChI=1S/C29H24F4N2O3/c30-13-17-15-35(16-17)9-10-37-21-5-1-18(2-6-21)28-27-23-8-4-20(36)12-25(23)34-14-24(27)22-7-3-19(29(31,32)33)11-26(22)38-28/h1-8,11-12,14,17,28,36H,9-10,13,15-16H2/t28-/m1/s1; Key:UVBQMXOKKDCBJN-MUUNZHRXSA-N;

Imlunestrant is an experimental selective estrogen receptor degrader developed by Eli Lilly and Company for the treatment of some types of breast cancer.^[1]^[2]^[3]

References

^ Neven, P.; Stahl, N.; Losada, M.J. Vidal; Jimenez, M. Martin; Kaufman, P.A.; Harbeck, N.; Hunt, K.; Carter, S.A.; Bidard, F.C.; Fasching, P.; Aftimos, P.G.; Wheatley, D.; Hamilton, E.P.; Aft, R.; Kulkarni, S.; Ismail-Khan, R.; Karacsonyi, C.; Estrem, S.T.; Ozbek, U.; Ciruelos, E.M. (October 2023). "273P A preoperative window-of-opportunity (WOO) study of imlunestrant in ER+, HER2- early breast cancer (EBC): Final analysis from EMBER-2". Annals of Oncology. 34: S292–S293. doi:10.1016/j.annonc.2023.09.470. S2CID 264385454.
^ Jhaveri, Komal; O’Shaughnessy, Joyce; Andre, Fabrice; Goetz, Matthew P.; Harbeck, Nadia; Martín, Miguel; Bidard, Francois-Clement; Thomas, Zachary M.; Young, Suzanne; Ismail-Khan, Roohi; Smyth, Lillian M.; Gnant, Michael (1 March 2023). "Abstract OT1-01-02: EMBER-4: A phase 3 adjuvant trial of imlunestrant vs standard endocrine therapy (ET) in patients with ER+, HER2- early breast cancer (EBC) with an increased risk of recurrence who have previously received 2 to 5 years of adjuvant ET". Cancer Research. 83 (5_Supplement): OT1–01–02-OT1-01–02. doi:10.1158/1538-7445.SABCS22-OT1-01-02.
^ Jhaveri, Komal L.; Jeselsohn, Rinath; Lim, Elgene; Hamilton, Erika P.; Yonemori, Kan; Beck, J. Thaddeus; Kaufman, Peter A.; Sammons, Sarah; Bhave, Manali A.; Saura, Cristina; Calvo, Emiliano; Meniawy, Tarek; Larson, Timothy; Ma, Cynthia X.; García-Corbacho, Javier; Cao, Shanshan; Estrem, Shawn T.; Milata, Jennifer L.; Nguyen, Bastien; Beeram, Muralidhar (1 June 2022). "A phase 1a/b trial of imlunestrant (LY3484356), an oral selective estrogen receptor degrader (SERD) in ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC): Monotherapy results from EMBER". Journal of Clinical Oncology. 40 (16_suppl): 1021. doi:10.1200/JCO.2022.40.16_suppl.1021. S2CID 249445691.

[1] Neven, P.; Stahl, N.; Losada, M.J. Vidal; Jimenez, M. Martin; Kaufman, P.A.; Harbeck, N.; Hunt, K.; Carter, S.A.; Bidard, F.C.; Fasching, P.; Aftimos, P.G.; Wheatley, D.; Hamilton, E.P.; Aft, R.; Kulkarni, S.; Ismail-Khan, R.; Karacsonyi, C.; Estrem, S.T.; Ozbek, U.; Ciruelos, E.M. (October 2023). "273P A preoperative window-of-opportunity (WOO) study of imlunestrant in ER+, HER2- early breast cancer (EBC): Final analysis from EMBER-2". Annals of Oncology. 34: S292–S293. doi:10.1016/j.annonc.2023.09.470. S2CID 264385454.

[2] Jhaveri, Komal; O’Shaughnessy, Joyce; Andre, Fabrice; Goetz, Matthew P.; Harbeck, Nadia; Martín, Miguel; Bidard, Francois-Clement; Thomas, Zachary M.; Young, Suzanne; Ismail-Khan, Roohi; Smyth, Lillian M.; Gnant, Michael (1 March 2023). "Abstract OT1-01-02: EMBER-4: A phase 3 adjuvant trial of imlunestrant vs standard endocrine therapy (ET) in patients with ER+, HER2- early breast cancer (EBC) with an increased risk of recurrence who have previously received 2 to 5 years of adjuvant ET". Cancer Research. 83 (5_Supplement): OT1–01–02-OT1-01–02. doi:10.1158/1538-7445.SABCS22-OT1-01-02.

[3] Jhaveri, Komal L.; Jeselsohn, Rinath; Lim, Elgene; Hamilton, Erika P.; Yonemori, Kan; Beck, J. Thaddeus; Kaufman, Peter A.; Sammons, Sarah; Bhave, Manali A.; Saura, Cristina; Calvo, Emiliano; Meniawy, Tarek; Larson, Timothy; Ma, Cynthia X.; García-Corbacho, Javier; Cao, Shanshan; Estrem, Shawn T.; Milata, Jennifer L.; Nguyen, Bastien; Beeram, Muralidhar (1 June 2022). "A phase 1a/b trial of imlunestrant (LY3484356), an oral selective estrogen receptor degrader (SERD) in ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC): Monotherapy results from EMBER". Journal of Clinical Oncology. 40 (16_suppl): 1021. doi:10.1200/JCO.2022.40.16_suppl.1021. S2CID 249445691.

[1]

[2]

[3]