Selective ER Degrader

Imlunestrant

Selective ER Degrader

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 key component of tumor growth.5 Disruption of estrogen signaling by selective estrogen receptor degraders (SERDs) is one of the treatment options for patients with estrogen-receptor-positive (ER+) cancers.
Molecule
Imlunestrant is an orally available SERD that has demonstrated the inhibition of estrogen signaling and subsequent inhibition of cell proliferation in ER-expressing tumor models.
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.
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.

The safety and efficacy of the agents under investigation have not been established. There is no guarantee that the agents will receive regulatory approval and become commercially available for the uses being investigated.

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