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治疗乳腺癌新药vepdegestrantOA

Vepdegestrant:A new drug for the treatment of breast cancer

中文摘要英文摘要

Vepdegestrant是一种口服异双功能蛋白质降解剂.它是一种小分子化合物,由雌激素受体(ER)结合结构域通过连接子与E3泛素连接酶结合结构域组成.vepdegestrant用于经美国食品药品监督管理局(FDA)批准的检测方法确认为ER阳性、人表皮生长因子受体2(HER2)阴性、雌激素受体1(ESR1)突变的晚期或转移性乳腺癌,且既往接受至少一线内分泌治疗后出现疾病进展的成人患者.临床研究表明,在目标患者人群中,vepdegestrant较氟维司群可延长无进展生存期(PFS)(5.0 vs.2.1个月).本文对vepdegestrant的作用机制、药动学特征、有效性、安全性及临床定位等进行介绍.

Vepdegestrant is an oral heterobifunctional protein degrader.It is a small molecule comprised of an estrogen receptor binding domain joined by a linker to an E3 ubiquitin ligase binding domain.Vepdegestrant is indicated for the treatment of adults with estrogen receptor(ER)-positive,human epidermal growth factor receptor 2(HER2)-negative,estrogen receptor 1(ESR1)-mutated advanced or metastatic breast cancer,as detected by a U.S.Food and Drug Administration(FDA)-authorized test,with disease progression following at least one line of endocrine therapy.Clinical trials have shown that vepdegestrant prolonged progression-free survival(PFS)versus fulvestrant in patients with ESR1-mutated ER-positive/HER2-negative advanced breast cancer(5.0 vs 2.1 months).This paper presents an overview of the mechanism of action,pharmacokinetic characteristics,clinical efficacy,safety profile and clinical positioning of vepdegestrant.

孙韬华;张芳;陈安进

青岛市市立医院,药物临床试验研究科,山东青岛 266011青岛市市立医院,药学部,山东青岛 266011青岛市市立医院,药物临床试验研究科,山东青岛 266011

医药卫生

vepdegestrant靶向蛋白降解剂药动学乳腺癌雌激素受体ESR1突变

vepdegestranttargeted protein degradation agentspharmacokineticsbreast cancerestrogen receptorESR1 mutation

《中国临床药理学杂志》 2026 (14)

2068-2073,6

10.13699/j.cnki.1001-6821.2026.14.018

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