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Selective oestrogen receptor modulators in desmoid tumours
Lucia Picariello1, Francesco Tonelli, Maria Luisa Brandi
1Department of Clinical Physiopathology, University of Florence, Italy.
Abstract:
Selective oestrogen receptor modulators (SERMs) are compounds with a mixed agonist/antagonist activity on oestrogen receptors. An ideal SERM is a compound with an oestrogen antagonist effect on the breast and uterus but oestrogen agonist effect on bone. Beside tamoxifen, a group of well-investigated SERMs is represented by raloxifene, LY-353381 (SERM3), EM-800 and CP-336156. On an empirical basis, tamoxifen has been used to pharmacologically treat desmoid tumours. Recently, raloxifene, a second-generation SERM, has been used in the treatment of familial adenomatous polyposis patients affected by desmoid tumour. The mechanisms through which these molecules affect desmoid tumour growth appear to be due, in part, to the fact that SERMs may act independently of oestrogen receptors. The knowledge of the molecular basis of SERM action will make the development of novel synthetic compounds with engineered tissue selectivity possible.
Insights
Selective oestrogen receptor modulators (SERMs) show promise in treating desmoid tumors. These compounds may act independently of oestrogen receptors, paving the way for new targeted therapies.
Area of Science:
- Pharmacology
- Oncology
- Endocrinology
Background:
- Selective oestrogen receptor modulators (SERMs) exhibit mixed agonist/antagonist activity at oestrogen receptors.
- An ideal SERM offers oestrogen antagonism in breast/uterus and agonism in bone.
- Tamoxifen and raloxifene are examples of SERMs with clinical applications.
Purpose of the Study:
- To explore the potential of SERMs in treating desmoid tumors.
- To investigate the mechanisms underlying SERM action in desmoid tumor growth.
- To highlight the possibility of developing novel SERMs with engineered tissue selectivity.
Main Methods:
- Review of existing literature on SERMs and their applications.
- Analysis of clinical observations regarding SERM use in desmoid tumors.
- Exploration of potential molecular mechanisms of SERM action.
Main Results:
- Tamoxifen has been empirically used for desmoid tumor treatment.
- Raloxifene has shown utility in familial adenomatous polyposis patients with desmoid tumors.
- SERMs may influence desmoid tumor growth independently of oestrogen receptors.
Conclusions:
- SERMs represent a potential therapeutic avenue for desmoid tumors.
- Understanding SERM molecular mechanisms is crucial for developing targeted therapies.
- Future research can focus on creating novel SERMs with enhanced tissue selectivity.
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