First Approval of Elacestrant as a Selective Estrogen Receptor Degrader for the Treatment of Metastatic Breast Cancer


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Аннотация

Elacestrant was approved by the US FDA on January 27, 2023, for treating postmenopausal women or adult men with estrogen receptor (ER)-positive, HER2- negative, ESR1-mutated advanced or metastatic breast cancer with disease progression prior to using at least one line of endocrine therapy. In this short perspective, physicochemical properties, dosage and administration, mechanism of action, pharmacodynamics, pharmacokinetics, drug interaction, and treatment-related adverse reactions of elacestrant are summarized.

Об авторах

Surya De

Department of Chemistry, Conju-Probe

Автор, ответственный за переписку.
Email: info@benthamscience.net

Список литературы

  1. Bidard, F.C.; Kaklamani, V.G.; Neven, P.; Streich, G.; Montero, A.J.; Forget, F.; Mouret-Reynier, M.A.; Sohn, J.H.; Taylor, D.; Harnden, K.K.; Khong, H.; Kocsis, J.; Dalenc, F.; Dillon, P.M.; Babu, S.; Waters, S.; Deleu, I.; García Sáenz, J.A.; Bria, E.; Cazzaniga, M.; Lu, J.; Aftimos, P.; Cortés, J.; Liu, S.; Tonini, G.; Laurent, D.; Habboubi, N.; Conlan, M.G.; Bardia, A. 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., 2022, 40(28), 3246-3256. doi: 10.1200/JCO.22.00338 PMID: 35584336
  2. Wang, Y.; Tang, S.C. The race to develop oral SERDs and other novel estrogen receptor inhibitors: Recent clinical trial results and impact on treatment options. Cancer Metastasis Rev., 2022, 41(4), 975-990. doi: 10.1007/s10555-022-10066-y PMID: 36229710
  3. Lloyd, M.R.; Wander, S.A.; Hamilton, E.; Razavi, P.; Bardia, A. Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: Current and emerging role. Ther. Adv. Med. Oncol., 2022, 14. doi: 10.1177/17588359221113694 PMID: 35923930
  4. Bardia, A.; Kaklamani, V.; Wilks, S.; Weise, A.; Richards, D.; Harb, W.; Osborne, C.; Wesolowski, R.; Karuturi, M.; Conkling, P.; Bagley, R.G.; Wang, Y.; Conlan, M.G.; Kabos, P.; Phase, I. Phase I study of elacestrant (RAD1901), a novel selective estrogen receptor degrader, in ER-Positive, HER2-negative advanced breast cancer. J. Clin. Oncol., 2021, 39(12), 1360-1370. doi: 10.1200/JCO.20.02272 PMID: 33513026
  5. Bihani, T.; Patel, H.K.; Arlt, H.; Tao, N.; Jiang, H.; Brown, J.L.; Purandare, D.M.; Hattersley, G.; Garner, F. Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), has antitumor activity in multiple ER+ breast cancer patient-derived xenograft models. Clin. Cancer Res., 2017, 23(16), 4793-4804. doi: 10.1158/1078-0432.CCR-16-2561 PMID: 28473534
  6. Bardia, A.; Aftimos, P.; Bihani, T.; Anderson-Villaluz, A.T.; Jung, J.; Conlan, M.G.; Kaklamani, V.G. EMERALD: Phase III trial of elacestrant (RAD1901) vs. endocrine therapy for previously treated ER+ advanced breast cancer. Future Oncol., 2019, 15(28), 3209-3218. doi: 10.2217/fon-2019-0370 PMID: 31426673
  7. Sanchez, K.G.; Nangia, J.R.; Schiff, R.; Rimawi, M.F. Elacestrant and the promise of oral SERDs. J. Clin. Oncol., 2022, 40(28), 3227-3229. doi: 10.1200/JCO.22.00841 PMID: 35737918
  8. Jacobson, A. Elacestrant improves progression-free survival after endocrine therapy for estrogen receptor-positive metastatic breast cancer. Oncologist, 2022, 27(Suppl. 1), S7-S8. doi: 10.1093/oncolo/oyac015 PMID: 35348779
  9. Conlan, M.G.; de Vries, E.F.J.; Glaudemans, A.W.J.M.; Wang, Y.; Troy, S. Pharmacokinetic and pharmacodynamic studies of elacestrant, a novel oral selective estrogen receptor degrader, in healthy post-menopausal women. Eur. J. Drug Metab. Pharmacokinet., 2020, 45(5), 675-689. doi: 10.1007/s13318-020-00635-3 PMID: 32661909
  10. Wardell, S.E.; Nelson, E.R.; Chao, C.A.; Alley, H.M.; McDonnell, D.P. Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. Endocr. Relat. Cancer, 2015, 22(5), 713-724. doi: 10.1530/ERC-15-0287 PMID: 26162914
  11. Shah, N.; Mohammad, A.S.; Saralkar, P.; Sprowls, S.A.; Vickers, S.D.; John, D.; Tallman, R.M.; Lucke-Wold, B.P.; Jarrell, K.E.; Pinti, M.; Nolan, R.L.; Lockman, P.R. Investigational chemotherapy and novel pharmacokinetic mechanisms for the treatment of breast cancer brain metastases. Pharmacol. Res., 2018, 132, 47-68. doi: 10.1016/j.phrs.2018.03.021 PMID: 29604436
  12. Chinnasamy, K.; Saravanan, M.; Poomani, K. Investigation of binding mechanism and downregulation of elacestrant for wild and L536S mutant estrogen receptor‐α through molecular dynamics simulation and binding free energy analysis. J. Comput. Chem., 2020, 41(2), 97-109. doi: 10.1002/jcc.26076 PMID: 31602686
  13. Patel, H.K.; Tao, N.; Lee, K.M.; Huerta, M.; Arlt, H.; Mullarkey, T.; Troy, S.; Arteaga, C.L.; Bihani, T. Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors. Breast Cancer Res., 2019, 21(1), 146. doi: 10.1186/s13058-019-1230-0 PMID: 31852484
  14. Lüftner, D. New treatment options for hormone receptor positive breast cancer in 2023. Curr. Opin. Obstet. Gynecol., 2023, 35(1), 62-66. doi: 10.1097/GCO.0000000000000834 PMID: 36341983
  15. Garcia-Fructuoso, I.; Gomez-Bravo, R.; Schettini, F. Integrating new oral selective oestrogen receptor degraders in the breast cancer treatment. Curr. Opin. Oncol., 2022, 34(6), 635-642. doi: 10.1097/CCO.0000000000000892 PMID: 36000362
  16. Liang, J.; Zbieg, J.R.; Blake, R.A.; Chang, J.H.; Daly, S.; DiPasquale, A.G.; Friedman, L.S.; Gelzleichter, T.; Gill, M.; Giltnane, J.M.; Goodacre, S.; Guan, J.; Hartman, S.J.; Ingalla, E.R.; Kategaya, L.; Kiefer, J.R.; Kleinheinz, T.; Labadie, S.S.; Lai, T.; Li, J.; Liao, J.; Liu, Z.; Mody, V.; McLean, N.; Metcalfe, C.; Nannini, M.A.; Oeh, J.; O’Rourke, M.G.; Ortwine, D.F.; Ran, Y.; Ray, N.C.; Roussel, F.; Sambrone, A.; Sampath, D.; Schutt, L.K.; Vinogradova, M.; Wai, J.; Wang, T.; Wertz, I.E.; White, J.R.; Yeap, S.K.; Young, A.; Zhang, B.; Zheng, X.; Zhou, W.; Zhong, Y.; Wang, X. GDC-9545 (Giredestrant): A potent and orally bioavailable selective estrogen receptor antagonist and degrader with an exceptional preclinical profile for er+ breast cancer. J. Med. Chem., 2021, 64(16), 11841-11856. doi: 10.1021/acs.jmedchem.1c00847 PMID: 34251202
  17. Hancock, G.R.; Young, K.S.; Hosfield, D.J.; Joiner, C.; Sullivan, E.A.; Yildiz, Y.; Lainé, M.; Greene, G.L.; Fanning, S.W. Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells. NPJ Breast Cancer, 2022, 8(1), 130. doi: 10.1038/s41523-022-00497-9 PMID: 36517522

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