Selective ER Degrader
Imlunestrant
Gladden AB and Diehl JA1; Patel HK and Bihani T2; Tecalco-Cruz AC, et al3; Wardell SE, et al4
Target
Estrogen signaling plays an important role in organ development and growth. In certain cancers, abnormal estrogen signaling via the estrogen receptor is a component of tumor growth.5 Disruption of estrogen signaling by selective estrogen receptor degraders (SERDs) is being investigated in patients with estrogen-receptor-positive (ER+) cancers.
Molecule
Imlunestrant is an orally available SERD that suppresses estrogen signaling and subsequently inhibits cell proliferation in ER-expressing tumor models.6,7
Clinical Development
Imlunestrant is being investigated in clinical trials in patients with ER+ breast cancer or endometrial cancer.
References
- Gladden AB, Diehl JA. J Cell Biochem. 2005;96(5):906-913.
- Patel HK, Bihani T. Pharmacol Ther. 2018;186:1-24.
- Tecalco-Cruz AC, et al. Cell Signal. 2017;34:121-132.
- Wardell SE, et al. Clin Cancer Res. 2015;21(22):5121-5130.
- Lee HR, et al. Int J Mol Med. 2012;29:883-890.
- Bhagwat SV, et al. Cancer Res. 2021;81(13_Suppl):1236.
- VandeKopple M, et al. ESMO Breast Cancer Annual Congress; May 11-13, 2023; Berlin, Germany. Abstract 41P.
or visit www.clinicaltrials.gov for more information on this trial