乳腺癌新一代雌激素受体向药物:现状和未来前景
Jian Min1, Xin Liu1, Rouming Peng1
1National & Local Joint Engineering Research Center of High-throughput Drug Screening Technology, State Key Laboratory of Biocatalysis and Enzyme Engineering, Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, School of Life Sciences, Hubei University, Wuhan, 430062, China.
Acta materia medica
|October 7, 2024
概括
新疗法对于雌激素受体 (ER) 阳性瘤的乳腺癌患者至关重要,这些瘤对内分泌疗法产生抵抗力. 本综述涵盖了下一代针对ER的药物,如口服选择性ER降解剂 (SERD) 和PROTAC.
科学领域:
- 在瘤学瘤学.
- 内分泌学 在内分泌学.
- 药理学 药理学是指药理学的学科.
背景情况:
- 向雌激素受体 (ER) 的内分泌疗法是ER阳性乳腺癌的基石治疗.
- 耐药性,特别是ESR1突变,限制了当前针对ER的治疗方法的长期疗效.
- 开发新药来克服耐药性和抑制ERα活性是一个关键的临床需求.
研究的目的:
- 审查最近在开发下一代针对乳腺癌的ER向药物的进展.
- 突出旨在克服内分泌抵抗的新型治疗策略.
- 为新兴ER向化合物提供药物设计,疗效和临床试验数据的概述.
主要方法:
- 对新型ER向药物的最新研究和临床试验的文献综述.
- 对下一代疗法的药物设计原则的分析.
- 针对ERα的化合物的疗效和临床数据的摘要,包括那些对ESR1突变有效的化合物.
主要成果:
- 一些下一代针对ER的药物正在开发中,包括口服选择性ER降解剂 (SERD) 和向蛋白质溶解的嵌合体 (PROTAC) ER降解剂.
- 诸如完全雌激素受体对抗剂 (CERAN) 和选择性雌激素受体共价对抗剂 (SERCA) 等创新分子显示出有前途.
- 这些药物旨在更有效地抑制ERα活性,克服包括ESR1突变在内的抵抗机制.
结论:
- 下一代针对ER的药物代表了克服乳腺癌内分泌耐药性的前沿.
- 口服SERD,PROTAC,CERAN和SERCA提供了各种机制来抑制ER信号和降低受体.
- 进一步的临床评估对于确定这些新药在患者治疗中的作用至关重要.
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