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Updated: Apr 23, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Safety of antiandrogen therapy for treating prostate cancer
Francesco Ricci1, Giulia Buzzatti, Alessandra Rubagotti
1University of Genoa, School of Medicine, Department of Internal Medicine , Genoa , Italy.
Introduction:
Antiandrogens are a treatment option in patients with prostate cancer, given either in combination with androgen deprivation or, in selected cases, as monotherapy. New-generation antiandrogens have been recently introduced in clinical practice (enzalutamide) or are under evaluation in clinical trials (ARN-509).
Areas Covered:
This review elucidates the safety profile of antiandrogens, in particular focusing on the tolerability profile of each drug either when employed in combination with castration or as monotherapy, in hormone-naive or in castration-resistant patients.
Expert Opinion:
Non-steroidal antiandrogens are widely used in the management of hormone-sensitive disease in combination with luteinizing hormone-releasing hormone agonists or in patients failing front-line treatment with androgen-deprivative maneuvers. In selected patients, non-steroidal antiandrogen monotherapy appears to yield comparable results as castration. Novel non-steroidal antiandrogens have been investigated with promising results in castration-resistant prostate cancer. Beyond the safety profile specific to any individual compound, increased testosterone and 17β-estradiol levels are commonly observed during antiandrogen monotherapy, leading to gynecomastia and breast pain. The safety profile of old and novel antiandrogens should be taken into account by clinicians in decision making and in selecting the most suitable patients. Beyond patient selection, full clinical evaluation of patient co-morbidities that might affect the drug tolerability and clinical monitoring are anyway required.
Insights
This review examines antiandrogen safety in prostate cancer treatment. Novel antiandrogens show promise, but clinicians must consider side effects like gynecomastia and patient comorbidities for optimal treatment selection.
Area of Science:
- Oncology
- Pharmacology
Background:
- Antiandrogens are a key treatment for prostate cancer, used alone or with androgen deprivation.
- Newer agents like enzalutamide and ARN-509 are expanding treatment options.
Purpose of the Study:
- To review the safety and tolerability of antiandrogens in prostate cancer management.
- To compare safety profiles of different antiandrogens in various treatment settings.
Main Methods:
- Literature review focusing on safety and tolerability data of antiandrogens.
- Analysis of drug profiles in hormone-naive and castration-resistant prostate cancer patients.
Main Results:
- Non-steroidal antiandrogens are effective in hormone-sensitive and resistant prostate cancer.
- Monotherapy with non-steroidal antiandrogens can be comparable to castration in select cases.
- Novel agents demonstrate promising outcomes in castration-resistant prostate cancer.
Conclusions:
- Clinicians must weigh individual antiandrogen safety profiles and potential side effects, such as gynecomastia.
- Patient selection, considering comorbidities and monitoring, is crucial for safe and effective antiandrogen therapy.
- Both established and novel antiandrogens require careful consideration of their safety profiles in clinical decision-making.
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