PIPELINE > TRIAL OVERVIEW

Selective ER Degrader
Imlunestrant
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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

  1. Gladden AB, Diehl JA. J Cell Biochem. 2005;96(5):906-913.
  2. Patel HK, Bihani T. Pharmacol Ther. 2018;186:1-24.
  3. Tecalco-Cruz AC, et al. Cell Signal. 2017;34:121-132.
  4. Wardell SE, et al. Clin Cancer Res. 2015;21(22):5121-5130.
  5. Lee HR, et al. Int J Mol Med. 2012;29:883-890.
  6. Bhagwat SV, et al. Cancer Res. 2021;81(13_Suppl):1236.
  7. VandeKopple M, et al. ESMO Breast Cancer Annual Congress; May 11-13, 2023; Berlin, Germany. Abstract 41P.
Clinical Development

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

References

  1. Gladden AB, Diehl JA. J Cell Biochem. 2005;96(5):906-913.
  2. Patel HK, Bihani T. Pharmacol Ther. 2018;186:1-24.
  3. Tecalco-Cruz AC, et al. Cell Signal. 2017;34:121-132.
  4. Wardell SE, et al. Clin Cancer Res. 2015;21(22):5121-5130.
  5. Lee HR, et al. Int J Mol Med. 2012;29:883-890.
  6. Bhagwat SV, et al. Cancer Res. 2021;81(13_Suppl):1236.
  7. VandeKopple M, et al. ESMO Breast Cancer Annual Congress; May 11-13, 2023; Berlin, Germany. Abstract 41P.
For information on trial enrollment, locations, and more, call 1-800-545-5979.

or visit www.clinicaltrials.gov for more information on this trial