依维莫司：首次获批。
Elacestrant: First Approval.
机构信息
Springer Nature, Mairangi Bay, Private Bag 65901, Auckland, 0754, New Zealand.
出版信息
Drugs. 2023 Apr;83(6):555-561. doi: 10.1007/s40265-023-01861-0.
Abstract
Elacestrant (ORSERDU™) is an orally available selective estrogen receptor degrader (SERD) being developed by Stemline Therapeutics, a subsidiary of Menarini Group, for the treatment of estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer. In January 2023, elacestrant received its first approval for the treatment of postmenopausal women or adult men with ER-positive, HER2-negative, estrogen receptor 1 (ESR1)-mutated (as determined by a US FDA-approved test) advanced or metastatic breast cancer with disease progression following ≥ 1 line of endocrine therapy in the USA. A regulatory assessment of elacestrant for the treatment of ER-positive, HER2-negative advanced or metastatic breast cancer is currently underway in the EU. Development of elacestrant for the treatment of vasomotor symptoms has been discontinued. This article summarizes the milestones in the development of elacestrant leading to this first approval for this indication.
摘要
Elacestrant（ORSERDU™）是一种口服的选择性雌激素受体降解剂（SERD），由 Menarini Group 的子公司 Stemline Therapeutics 开发，用于治疗雌激素受体（ER）阳性、人表皮生长因子受体 2（HER2）阴性乳腺癌。2023 年 1 月，elacestrant 在美国获得批准，用于治疗绝经后妇女或成年男性的 ER 阳性、HER2 阴性、雌激素受体 1（ESR1）突变（通过美国 FDA 批准的检测方法确定）的晚期或转移性乳腺癌，这些患者在接受≥1 线内分泌治疗后疾病进展。elacestrant 治疗 ER 阳性、HER2 阴性晚期或转移性乳腺癌的监管评估正在欧盟进行。elacestrant 治疗血管舒缩症状的开发已被停止。本文总结了导致这一适应证首次批准的 elacestrant 开发的里程碑事件。
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本文引用的文献
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2
Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: current and emerging role.新一代选择性雌激素受体降解剂及其他用于治疗转移性激素受体阳性乳腺癌的新型内分泌疗法：当前及新出现的作用
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3
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J Clin Oncol. 2022 Oct 1;40(28):3246-3256. doi: 10.1200/JCO.22.00338. Epub 2022 May 18.
4
Phase I Study of Elacestrant (RAD1901), a Novel Selective Estrogen Receptor Degrader, in ER-Positive, HER2-Negative Advanced Breast Cancer.Elacestrant（RAD1901），一种新型选择性雌激素受体降解剂，在 ER 阳性、HER2 阴性晚期乳腺癌中的 I 期研究。
J Clin Oncol. 2021 Apr 20;39(12):1360-1370. doi: 10.1200/JCO.20.02272. Epub 2021 Jan 29.
5
A phase 1b study evaluating the effect of elacestrant treatment on estrogen receptor availability and estradiol binding to the estrogen receptor in metastatic breast cancer lesions using F-FES PET/CT imaging.一项 1b 期研究，使用 F-FES PET/CT 成像评估 Elacestrant 治疗对转移性乳腺癌病灶中雌激素受体可用性和雌二醇与雌激素受体结合的影响。
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6
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Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader.选择性雌激素受体降解剂RAD1901的药理活性评估
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