Synonyms: ER-306323 | ER306323 | Orserdu® | RAD-1901 | RAD1901
elacestrant is an approved drug (FDA & EMA (2023))
Compound class:
Synthetic organic
Comment: Elacestrant is an orally bioactive, selective, non-steroidal dual estrogen receptor degrader (SERD)/selective estrogen receptor modulator (SERM; with antagonist action) [6]. It was developed primarily for antineoplastic potential (via its SERD action at high concentrations) [3]. It has also demonstrated potential to treat the vasomotor symptoms of the menopause with estrogen-like effects detected at low concentrations (SERM activity), but the pharmacology in this setting is very complex [4]. Elacestrant crosses the blood-brain barrier, so is predicted to provide efficacy against breast cancer metastases in the brain.
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References |
1. Bardia A, Aftimos P, Bihani T, Anderson-Villaluz AT, Jung J, Conlan MG, Kaklamani VG. (2019)
EMERALD: Phase III trial of elacestrant (RAD1901) vs endocrine therapy for previously treated ER+ advanced breast cancer. Future Oncol, 15 (28): 3209-3218. [PMID:31426673] |
2. Bidard FC, Kaklamani VG, Neven P, Streich G, Montero AJ, Forget F, Mouret-Reynier MA, Sohn JH, Taylor D, Harnden KK et al.. (2022)
Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial. J Clin Oncol, 40 (28): 3246-3256. [PMID:35584336] |
3. Garner F, Shomali M, Paquin D, Lyttle CR, Hattersley G. (2015)
RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs, 26 (9): 948-56. [PMID:26164151] |
4. Hattersley G, Harris AG, Simon JA, Constantine GD. (2017)
Clinical investigation of RAD1901, a novel estrogen receptor ligand, for the treatment of postmenopausal vasomotor symptoms: a phase 2 randomized, placebo-controlled, double-blind, dose-ranging, proof-of-concept trial. Menopause, 24 (1): 92-99. [PMID:27575546] |
5. Hoy SM. (2023)
Elacestrant: First Approval. Drugs, 83 (6): 555-561. [PMID:37060385] |
6. Wardell SE, Nelson ER, Chao CA, Alley HM, McDonnell DP. (2015)
Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. Endocr Relat Cancer, 22 (5): 713-24. [PMID:26162914] |