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Steroidal and nonsteroidal oestrogen antagonists in breast cancer: basic and clinical appraisal
1Department of Preclinical Oncology, Istituto Nazionale per la Ricerca sul Cancro, Genova, Italy.
Abstract:
Endogenous sex hormones, such as oestrogens, control the development and growth of breast carcinoma. Blocking the binding between the steroid hormone and its receptor using anti-oestrogenic compounds is one of the possible ways of impeding the action of oestrogens at the level of their target tissues. The nonsteroidal, triphenylethylenic, anti-oestrogen tamoxifen has so far been the standard compound for endocrine treatment of breast cancer. Nevertheless, it forms a complex with the oestrogen receptor which gives rise to a range of biopharmacological events, ranging from full oestrogen antagonism to partial agonism. Moreover, its use is limited by the possible onset of drug resistance in many patients. In spite of these restrictions, tamoxifen has proved to be very helpful as a starting point for the development of new, more efficacious compounds. In this article, Roberto Favoni and Alessandra de Cupis review and discuss tamoxifen, several of its derivatives and the steroidal-like anti-oestrogens in terms of laboratory development, pharmacology and clinical evaluation.
Insights
Tamoxifen, a standard breast cancer drug, acts as an anti-oestrogen but has limitations like drug resistance. Researchers are developing improved derivatives and steroidal-like anti-oestrogens for better breast cancer treatment.
Area of Science:
- Endocrinology
- Oncology
- Pharmacology
Background:
- Endogenous sex hormones, like oestrogens, drive breast carcinoma development.
- Anti-oestrogenic compounds can block oestrogen-receptor interactions in target tissues.
- Tamoxifen, a nonsteroidal anti-oestrogen, is the established endocrine therapy for breast cancer.
Purpose of the Study:
- To review and discuss tamoxifen, its derivatives, and steroidal-like anti-oestrogens.
- To evaluate these compounds in terms of laboratory development, pharmacology, and clinical efficacy.
- To highlight the potential for developing more effective breast cancer treatments.
Main Methods:
- Review of existing literature on tamoxifen and related anti-oestrogens.
- Analysis of pharmacological properties and clinical evaluation data.
- Discussion of laboratory development pathways for novel compounds.
Main Results:
- Tamoxifen exhibits variable oestrogen antagonism/agonism due to its receptor complex formation.
- Drug resistance is a significant limitation for tamoxifen therapy in many patients.
- Tamoxifen serves as a crucial foundation for developing next-generation anti-oestrogenic drugs.
Conclusions:
- Despite limitations, tamoxifen remains a valuable starting point for anti-cancer drug discovery.
- Further research into tamoxifen derivatives and steroidal-like anti-oestrogens is essential.
- Optimizing anti-oestrogen therapy holds promise for improved breast cancer patient outcomes.