Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status

被引：37
作者：
Downton, Teesha [1 ,2 ]
Zhou, Fiona [1 ,2 ]
Segara, Davendra [1 ]
Jeselsohn, Rinath [3 ]
Lim, Elgene [1 ,2 ]
机构：
[1] Garvan Inst Med Res, Sydney, NSW, Australia
[2] Univ New South Wales, Fac Med & Hlth, Sch Clin Med, St Vincents Healthcare Clin Campus, Sydney, NSW, Australia
[3] Dana Farber Canc Inst, Boston, MA USA
来源：
DRUG DESIGN DEVELOPMENT AND THERAPY | 2022年 / 16卷
关键词：
selective estrogen receptor degraders; breast cancer; estrogen receptor; FULVESTRANT; 500; MG; NEOADJUVANT ENDOCRINE THERAPY; ANASTROZOLE; POSTMENOPAUSAL WOMEN; PLUS FULVESTRANT; DOUBLE-BLIND; POTENT; MUTATIONS; TAMOXIFEN; TRIAL;
D O I：
10.2147/DDDT.S380925
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Several endocrine therapies are currently available for the treatment of estrogen receptor (ER) positive breast cancer, but the clinical benefit of these agents is limited by endocrine therapy drug resistance. A common mechanism of endocrine therapy resistance is ESR1 mutations. The first-generation selective estrogen receptor degrader (SERD) fulvestrant has activity against ESR1 mutant tumors but requires intramuscular injection and has poor bioavailability that precludes optimal drug dosing. This led to the development of second-generation SERDs which are potent and have improved oral bioavailability and pharmacokinetics. Several of these oral SERDs are now in phase III trials in both the early and advanced ER positive breast cancer settings. This review summarizes the background of oral SERD development, the current status and future perspectives.
引用
收藏
页码：2933 / 2948
页数：16
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