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Updated: May 23, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Role of 5α-reductase inhibitors in prostate cancer prevention and treatment
1Department of Urology, Roswell Park Cancer Institute, Buffalo, New York 14263, USA. faris.azzouni@roswellpark.org
Abstract:
Although testosterone is the most abundant serum androgen, dihydrotestosterone is the main prostatic androgen. Testosterone is converted to dihydrotestosterone by the enzyme 5α-reductase (5α-R). Dihydrotestosterone plays an important role in several human diseases, including benign prostate enlargement and prostate cancer. The observation that males born with 5α-R 2 deficiency have never been reported to develop prostate cancer stimulated interest in development of 5α-R inhibitors. Thus far, 2 5α-R inhibitors are approved for clinical use. Several trials evaluated the use of 5α-R inhibitors in prostate cancer prevention and treatment and will be reviewed in this article.
Insights
Dihydrotestosterone (DHT) is a key prostate androgen. Inhibiting its production via 5α-reductase (5α-R) is a promising strategy for preventing and treating prostate cancer, with two inhibitors currently approved.
Area of Science:
- Andrology
- Urologic Oncology
- Pharmacology
Background:
- Dihydrotestosterone (DHT) is the primary androgen in the prostate gland.
- DHT is synthesized from testosterone by the enzyme 5α-reductase (5α-R).
- DHT is implicated in the pathogenesis of benign prostate enlargement and prostate cancer.
Purpose of the Study:
- To review the role of 5α-reductase inhibitors in prostate cancer.
- To discuss clinical trials evaluating 5α-R inhibitors for prostate cancer prevention and treatment.
Main Methods:
- Literature review of studies on 5α-reductase inhibitors.
- Analysis of clinical trial data regarding efficacy and safety.
Main Results:
- The enzyme 5α-reductase (5α-R) converts testosterone to dihydrotestosterone (DHT).
- Males with 5α-R 2 deficiency show no incidence of prostate cancer, highlighting 5α-R's role.
- Two 5α-R inhibitors are approved for clinical use.
Conclusions:
- 5α-reductase inhibitors represent a significant therapeutic avenue for prostate cancer.
- Further research and clinical application of these inhibitors are warranted.
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