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Does imlunestrant cross the blood brain barrier?
Imlunestrant is an oral brain-penetrant selective estrogen receptor degrader (SERD) that has demonstrated activity in a preclinical brain metastasis model.
Imlunestrant Brain Penetration and Activity in Brain Metastasis: Preclinical Data
LY3484356 (imlunestrant) is a novel, orally bioavailable selective estrogen receptor degrader (SERD) with pure antagonistic properties resulting in sustained inhibition of estrogen receptor (ER)-dependent gene transcription and cell growth.1,2
Imlunestrant showed sustained exposure in the brains of mice, demonstrating its ability to effectively cross the blood-brain barrier (see ). In an ER+ brain orthotopic mouse model, imlunestrant treatment prolonged overall survival compared to control, fulvestrant, and alternative SERD therapies (see ).3
The published references below are available by contacting 1-800-LillyRx (1-800-545-5979).
1Vandekopple M, Mur C, Shen W, et al. Preclinical characterization of imlunestrant, an oral brain-penetrant selective estrogen receptor degrader with activity in a brain metastasis (BM) model. ESMO Open. 2023;8(1 suppl 4):101265. European Society for Medical Oncology abstract 41P. https://doi.org/10.1016/j.esmoop.2023.101265
2Bhagwat SV, Zhao B, Shen W, et al. Preclinical characterization of LY3484356, a novel, potent and orally bioavailable selective estrogen receptor degrader (SERD). Cancer Res. 2021;18(13 suppl):1236. American Association of Cancer Research abstract 1236. https://doi.org/10.1158/1538-7445.AM2021-1236
3Vandekopple M, Mur C, Shen W, et al. Preclinical characterization of imlunestrant, an oral brain-penetrant selective estrogen receptor degrader with activity in a brain metastasis (BM) model. Poster presented at: 5th European Society for Medical Oncology Breast Cancer (ESMO-BC) Congress; May 11-13, 2023; Berlin, Germany. Accessed October 11, 2023. https://cslide.ctimeetingtech.com/breast23hybrid/public/download_uploaded_media/pdf/125
Date of Last Review: September 29, 2023