文章：

口服选择性雌激素受体降解剂：雌激素受体阳性乳腺癌的新型内分泌疗法

Oral SERD, a Novel Endocrine Therapy for Estrogen Receptor-Positive Breast Cancer

原文发布日期：31 January 2024

DOI: 10.3390/cancers16030619

类型: Article

开放获取: 是

英文摘要：

Breast cancer is the most common cancer among women worldwide, and estrogen receptor-positive (ER+) breast cancer accounts for a significant proportion of cases. While various treatments are available, endocrine therapies are often the first-line treatment for this type of breast cancer. However, the development of drug resistance poses a significant challenge in managing this disease.ESR1mutations have been identified as a common mechanism of endocrine therapy resistance in ER+ breast cancer. The first-generation selective estrogen receptor degrader (SERD) fulvestrant has shown some activity againstESR1mutant tumors. However, due to its poor bioavailability and need for intramuscular injection, it may not be the optimal therapy for patients. Second-generation SERDs were developed to overcome these limitations. These newer drugs have improved oral bioavailability and pharmacokinetics, making them more convenient and effective for patients. Several oral SERDs are now in phase III trials for early and advanced ER+ breast cancer. This review summarizes the background of oral SERD development, the current status, and future perspectives.

摘要翻译： 

乳腺癌是全球女性最常见的恶性肿瘤，其中雌激素受体阳性（ER+）亚型占据重要比例。尽管存在多种治疗手段，内分泌疗法通常作为此类乳腺癌的一线治疗方案。然而，耐药性的产生成为疾病管理中的重大挑战。 研究表明，ESR1基因突变是ER+乳腺癌内分泌治疗耐药的常见机制。第一代选择性雌激素受体降解剂（SERD）氟维司群对ESR1突变肿瘤展现出一定活性，但由于其生物利用度低且需肌肉注射给药，可能并非患者的最佳治疗选择。为克服这些局限性，第二代SERD应运而生。这类新型药物具有更优的口服生物利用度和药代动力学特性，为患者提供了更便捷有效的治疗选择。目前已有数种口服SERD药物针对早期及晚期ER+乳腺癌开展III期临床试验。本文综述了口服SERD的研发背景、现状及未来展望。

原文链接：

Oral SERD, a Novel Endocrine Therapy for Estrogen Receptor-Positive Breast Cancer