Next generation selective estrogen receptor degraders in postmenopausal women with advanced-stage hormone...

Area of Science:

• Oncology
• Endocrinology
• Pharmacology

Background:

• Breast cancer is a heterogeneous malignancy, with hormone receptor-positive (HR+) subtypes being the most prevalent.
• Endocrine therapies targeting estrogen receptor (ER) signaling are crucial for HR+ breast cancer treatment.
• Current therapies include selective estrogen receptor modulators (SERMs), aromatase inhibitors (AIs), and selective estrogen receptor degraders (SERDs).

Purpose of the Study:

• To review the development of novel oral selective estrogen receptor degraders (SERDs) for breast cancer treatment.
• To provide a practical therapeutic perspective on these emerging agents.
• To enhance understanding of the mechanisms of action for oral SERDs.

Main Methods:

• Literature review of ongoing research and clinical development of oral SERDs.
• Analysis of the pharmacological mechanisms of action for novel SERDs.
• Discussion of therapeutic implications and future directions.

Main Results:

• Selective estrogen receptor degraders (SERDs) effectively block and degrade ER signaling in breast cancer cells.
• Novel oral SERDs are under development, offering a more convenient administration route compared to injectable forms.
• Combination therapies involving SERDs with CDK4/6 inhibitors or alpelisib show promise for advanced-stage disease.

Conclusions:

• Oral SERDs represent a significant advancement in endocrine therapy for ER-positive breast cancer.
• These agents offer a potent and practical approach to overcoming endocrine resistance.
• Further research into novel oral SERDs will likely expand treatment options and improve patient outcomes.