Selective estrogen receptor modulators in clinical practice: a safety overview.

Area of Science:

• Pharmacology
• Endocrinology
• Oncology

Background:

• Selective estrogen receptor modulators (SERMs) are nonsteroidal compounds interacting with estrogen receptors (ERs) with tissue-specific effects.
• SERMs demonstrate efficacy in indications such as osteoporosis, dyspareunia, and breast cancer, but also present safety risks.

Purpose of the Study:

• To review the safety profiles of various SERMs (tamoxifen, raloxifene, toremifene, bazedoxifene, lasofoxifene, ospemifene) and fulvestrant.
• To compare the safety of newer generation SERMs against first-generation tamoxifen.

Main Methods:

• Analysis of Phase III trials, long-term extension studies, and active comparator studies.
• Evaluation of safety data for tamoxifen, toremifene, raloxifene, bazedoxifene, lasofoxifene, ospemifene, and fulvestrant.

Main Results:

• Tamoxifen is associated with significant risks including endometrial cancer, venous thromboembolic events (VTE), and stroke.
• Newer SERMs generally show improved safety profiles compared to tamoxifen, particularly regarding endometrial cancer and stroke.
• VTE risk remains a concern across most SERMs.

Conclusions:

• Each SERM has a unique risk/benefit profile, necessitating careful patient selection and monitoring.
• Future research aims to develop SERMs for endocrine-resistant cancers and menopausal symptoms.