原发性和获得性内分泌抵抗仍然是激素受体阳性乳腺癌治疗中的一个主要问题。获得性耐药通常是由雌激素受体 1 (ESR1) 突变导致的，导致雌激素独立的雌激素受体激活。选择性雌激素受体降解剂（SERD）诱导该受体降解，从而克服这种耐药性。第一种 SERD 氟维司群的肌肉注射和适度疗效引发了口服、更有效的 SERD 的开发。这篇叙述性综述概述了有关这一新药类别的当前证据。使用系统搜索策略对 Medline/PubMed 和 Embase 数据库进行了筛选。我们通过应用以下术语评估了圣安东尼奥乳腺癌研讨会摘要报告、欧洲肿瘤内科学会 (ESMO) 和美国临床肿瘤学会 (ASCO) 会议资源：“SERD”、“giredestrant”、“elacestrant”、“ imlunestrant'、'amcenestrant'、'camizestrant' 和 'rintodestrant'.gov 被咨询以包括正在进行的试验。搜索检索到 1191 篇文章。经筛选，保留108篇文章。在 3 期 EMERALD 试验中，elacestrant 证明对绝经后女性或男性二线转移性疾病的无进展生存期 (PFS) 有益，导致美国食品和药物管理局 (FDA) 和欧洲药品管理局 (EMA) 批准用于 ESR1 突变人群。这种 PFS 优势在之前接受过至少 12 个月的细胞周期蛋白依赖性激酶 4/6 抑制剂 (CDK4/6i) 治疗的患者中更为明显。在 2 期 SERENA-2 试验中，卡米司群作为二线治疗可改善 PFS。然而，giredestrant 和 amcenestrant 的试验未能显示二线转移性病例中 PFS 的益处。在术前，一些口服 SERD 导致肿瘤增殖显着减少。此外，许多试验仍在进行中。口服 SERD 是一类令人兴奋的新药。正在进行和未来的研究将进一步完善这些药物在标准内分泌治疗和靶向治疗之外的作用。版权所有 © 2024 作者。由爱思唯尔有限公司出版。保留所有权利。

Primary and acquired endocrine resistance remains a major issue in the treatment of hormone receptor positive breast cancer. Acquired resistance often results from estrogen receptor 1 (ESR1) mutations leading to estrogen independent estrogen receptor activation. Selective estrogen receptor degraders (SERDs) induce degradation of this receptor, thereby overcoming this resistance. The intramuscular administration and modest efficacy of fulvestrant, the first SERD, triggered development of oral, more potent SERDs. This narrative review gives an overview of the current evidence regarding this new drug class.Medline/PubMed and Embase database were screened using a systematic search strategy. We assessed the San Antonio Breast Cancer Symposium abstract reports, the European Society of Medical Oncology (ESMO) and American Society of Clinical Oncology (ASCO) meeting resources by applying the following terms: 'SERD', 'giredestrant', 'elacestrant', 'imlunestrant', 'amcenestrant', 'camizestrant' and 'rintodestrant'.gov was consulted to include ongoing trials.The search retrieved 1191 articles. After screening, 108 articles were retained. In the phase 3 EMERALD trial, elacestrant demonstrated benefit in progression free survival (PFS) in second line metastatic disease in postmenopausal women or men, leading to Food and Drug Administration (FDA) and European Medicines Agency (EMA) approval for the ESR1 mutated population. This PFS advantage was more pronounced among patients who had priorly received at least 12 months of a cyclin-dependent kinases 4/6 inhibitor (CDK4/6i). In the phase 2 SERENA-2 trial, camizestrant improved PFS as second line treatment. However, trials of giredestrant and amcenestrant failed to show PFS benefit in second line metastatic setting. In the preoperative setting, several oral SERDs resulted in a significant reduction of tumoral proliferation. Furthermore, many trials are still in progress.Oral SERDs constitute an exciting new drug class. Ongoing and future research will further refine the role of these drugs next to standard endocrine treatments and targeted therapies.Copyright © 2024 The Author(s). Published by Elsevier Ltd.. All rights reserved.