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Updated: Jun 22, 2025

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Practical implications of androgen receptor inhibitors for prostate cancer treatment
Fabio Campodonico1, Luca Foppiani2, Vittoria Campodonico3
1Department of Abdominal Surgery, Urology Unit, Galliera Hospital, 16128 Genova, Italy.
Abstract:
Antiandrogens have been used for the treatment of prostate cancer as a single agent or in combination with hormone deprivation therapy. New generation antiandrogens act like androgen receptor inhibitors (ARIs). Their binding complex blocks the pathways of cellular proliferation and differentiation of the prostate. Enzalutamide, apalutamide and darolutamide are the new ARIs that demonstrated acceptable tolerability and toxicity, both active in hormone-sensitive and castration-resistant prostate cancer (CRPC). There is no evidence of superiority of one drug over the other, therefore the therapeutic choice depends on the safety profile in relation to the individual patient, their comorbidities and clinical condition. ARIs have also shown promising results in association with new drugs that are active on patients with metastatic CRPC carrying the mutated breast cancer gene (BRCA). Before undergoing new antiandrogenic therapies, patients should be evaluated for cardiological and metabolic risk and possible drug interactions.
Insights
New androgen receptor inhibitors (ARIs) like enzalutamide, apalutamide, and darolutamide effectively treat prostate cancer. Patient-specific safety profiles guide treatment choices for hormone-sensitive and castration-resistant prostate cancer.
Area of Science:
- Oncology
- Pharmacology
- Urology
Background:
- Antiandrogens are established treatments for prostate cancer, used alone or with hormone deprivation.
- Newer antiandrogens function as androgen receptor inhibitors (ARIs), blocking prostate cell proliferation and differentiation pathways.
Purpose of the Study:
- To review the role and application of new-generation androgen receptor inhibitors (ARIs) in prostate cancer management.
- To discuss the efficacy, tolerability, and selection criteria for ARIs in hormone-sensitive and castration-resistant prostate cancer (CRPC).
Main Methods:
- Review of current literature on new ARIs including enzalutamide, apalutamide, and darolutamide.
- Analysis of clinical data regarding efficacy, safety profiles, and patient selection for ARIs.
Main Results:
- Enzalutamide, apalutamide, and darolutamide are effective ARIs for both hormone-sensitive and castration-resistant prostate cancer (CRPC).
- These agents show acceptable tolerability and toxicity.
- No single ARI demonstrates superiority; therapeutic choice hinges on individual patient safety profiles, comorbidities, and clinical status.
- ARIs show promise in combination therapies for metastatic CRPC, particularly in patients with BRCA mutations.
Conclusions:
- New ARIs represent a significant advancement in prostate cancer treatment.
- Treatment selection requires a personalized approach considering patient-specific factors and safety profiles.
- Pre-treatment evaluation for cardiometabolic risks and drug interactions is crucial for patients undergoing ARI therapy.
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