PIPELINE > TRIAL OVERVIEW

Selective Estrogen Receptor Degrader
Imlunestrant
Selective ER Degrader

Bhagwat SV1; VandeKopple M2; Patel HK and Bihani T3; Jeselsohn R4; Tecalco-Cruz AC5

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.6 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.1,2

Clinical Development

Imlunestrant is being investigated in clinical trials in patients with ER+ breast cancer or endometrial cancer.

References

  1. Bhagwat SV, et al. Cancer Res. 2021;81(13_Suppl):1236.
  2. VandeKopple M, et al. ESMO Open. 2023;8(1_Suppl):19.
  3. Patel HK, Bihani T. Pharmacol Ther. 2018;186:1-24.
  4. Jeselsohn R, et al. Clin Cancer Res. 2014;20(7):1757-1767.
  5. Tecalco-Cruz AC, et al. Cell Signal. 2017;34:121-132.
  6. Lee HR, et al. Int J Mol Med. 2012;29:883-890.
For information on trial enrollment, locations, and more, call 1-800-545-5979.