Abstract：
UNASSIGNED: Estrogen receptor positive (ER+) breast cancer is the most common breast cancer subtype, and therapeutic management relies primarily on inhibiting ER signaling. In the metastatic setting, ER signaling is typically targeted by selective estrogen receptor degraders (SERDs) or aromatase inhibitors (AIs), the latter of which prevent estrogen production. Activating ESR1 mutations are among the most common emergent breast cancer mutations and confer resistance to AIs.
UNASSIGNED: Until 2023, fulvestrant was the only approved SERD; fulvestrant is administered intramuscularly, and in some cases may also have limited efficacy in the setting of certain ESR1 mutations. In 2023, the first oral SERD, elacestrant, was approved for use in ESR1-mutated, ER+/HER2- advanced breast cancer and represents a new class of therapeutic options. While the initial approval was as monotherapy, ongoing studies are evaluating elacestrant (as well as other oral SERDs) in combination with other therapies including CDK4/6 inhibitors and PI3K inhibitors, which parallels the current combination uses of fulvestrant.
UNASSIGNED: Elacestrant\'s recent approval sheds light on the use of biomarkers such as ESR1 to gauge a tumor\'s endocrine sensitivity. Ongoing therapeutic and correlative biomarker studies will offer new insight and expanding treatment options for patients with advanced breast cancer.
UNASSIGNED: Until 2023, fulvestrant was the only approved SERD; fulvestrant is administered intramuscularly, and in some cases may also have limited efficacy in the setting of certain ESR1 mutations. In 2023, the first oral SERD, elacestrant, was approved for use in ESR1-mutated, ER+/HER2- advanced breast cancer and represents a new class of therapeutic options. While the initial approval was as monotherapy, ongoing studies are evaluating elacestrant (as well as other oral SERDs) in combination with other therapies including CDK4/6 inhibitors and PI3K inhibitors, which parallels the current combination uses of fulvestrant.
UNASSIGNED: Elacestrant\'s recent approval sheds light on the use of biomarkers such as ESR1 to gauge a tumor\'s endocrine sensitivity. Ongoing therapeutic and correlative biomarker studies will offer new insight and expanding treatment options for patients with advanced breast cancer.
摘要：
■雌激素受体阳性（ER+）乳腺癌是最常见的乳腺癌亚型，治疗管理主要依赖于抑制ER信号。在转移性环境中，ER信号通常由选择性雌激素受体降解剂（SERD）或芳香化酶抑制剂（AIs）靶向，后者阻止雌激素的产生。激活ESR1突变是最常见的新兴乳腺癌突变之一，并赋予对AI的抗性。
■直到2023年，氟维司群是唯一批准的SERD；氟维司群是肌肉内给药，并且在某些情况下，在某些ESR1突变的情况下也可能具有有限的功效。2023年，第一个口头SERD，eelacstrant,被批准用于ESR1突变，ER+/HER2-晚期乳腺癌代表了一类新的治疗选择。虽然最初的批准是作为单一疗法，正在进行的研究正在评估elacestrant（以及其他口服SERD）与其他疗法的组合，包括CDK4/6抑制剂和PI3K抑制剂，这与目前氟维司群的组合使用相似。
■Elacestrant的最新批准揭示了使用生物标志物如ESR1来衡量肿瘤的内分泌敏感性。正在进行的治疗和相关生物标志物研究将为晚期乳腺癌患者提供新的见解和扩展的治疗选择。
■直到2023年，氟维司群是唯一批准的SERD；氟维司群是肌肉内给药，并且在某些情况下，在某些ESR1突变的情况下也可能具有有限的功效。2023年，第一个口头SERD，eelacstrant,被批准用于ESR1突变，ER+/HER2-晚期乳腺癌代表了一类新的治疗选择。虽然最初的批准是作为单一疗法，正在进行的研究正在评估elacestrant（以及其他口服SERD）与其他疗法的组合，包括CDK4/6抑制剂和PI3K抑制剂，这与目前氟维司群的组合使用相似。
■Elacestrant的最新批准揭示了使用生物标志物如ESR1来衡量肿瘤的内分泌敏感性。正在进行的治疗和相关生物标志物研究将为晚期乳腺癌患者提供新的见解和扩展的治疗选择。
