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Discovery of Natural Steroid 5 Alpha-Reductase Inhibitors

Assay and Drug Development Technologies, 2019
Human steroid 5 alpha-reductases (S5αRs) and NADPH irreversibly reduce testosterone to the more potent dihydrotestosterone (DHT). S5αR inhibitors are useful treatments for DHT-dependent diseases, including benign prostatic hyperplasia, androgenic alopecia and hair growth, and acne.
C Norman Scholfield   +2 more
exaly   +3 more sources

5-Alpha reductase inhibitors in active surveillance

Current Opinion in Urology, 2014
Active surveillance is now one of the recommended treatment options for low-risk prostate cancer (PCa). However, about 10-30% of men on active surveillance will progress and require definitive therapy. In this review, we examine the role of 5-alpha reductase inhibitors (5-ARIs) in secondary prevention among men with low-risk PCa who opted to be managed
Patrick O, Richard, Antonio, Finelli
openaire   +2 more sources

5 Alpha-reductase inhibitors: whatʼs new?

Current Opinion in Urology, 2003
Medical therapy is now the first-line treatment for most men with symptomatic benign prostatic hyperplasia. This review aims to highlight the recent contributions to our understanding of 5 alpha-reductase inhibitor usage.For the last decade, finasteride has been the only available 5 alpha-reductase inhibitor, acting upon the type 2 isoenzyme of 5-alpha
Charlotte L, Foley, Roger S, Kirby
openaire   +2 more sources

5-Alpha-reductase inhibitors in diseases of the prostate

Current Opinion in Endocrinology, Diabetes & Obesity, 2014
To summarize the history of the use of 5-alpha-reductase inhibitors in the treatment of urologic diseases and discuss the current practices and indications for therapy.5-Alpha-reductase inhibitors (5-ARIs) are indicated in the treatment of benign prostatic hyperplasia (BPH) with obstructive urinary symptoms to reduce symptoms, reduce the risk of acute ...
Robert J, Carrasquillo   +2 more
openaire   +2 more sources

Finasteride: A slow-binding 5.alpha.-reductase inhibitor

Biochemistry, 1993
A microsomal preparation of human prostatic tissue was used to study the kinetics of interaction of steroid 5 alpha-reductase with finasteride, a known 5 alpha-reductase inhibitor. This molecule has been reported to reversibly bind 5 alpha-reductase in a competitive manner to testosterone with a Ki value in the 10 nM range.
B, Faller, D, Farley, H, Nick
openaire   +2 more sources

The role of 5-alpha-reductase inhibitors in active surveillance

Current Opinion in Urology, 2012
Active surveillance is now considered one of the preferred treatments for men with favorable risk prostate cancer (PCa). Unfortunately, 30-50% of men choosing active surveillance will progress and require therapy. In this context, we will present recent data on the efficacy of 5-alpha-reductase inhibitors (5-ARIs) in secondary prevention among men with
David, Margel, Neil, Fleshner
openaire   +2 more sources

Azasteroids as inhibitors of rat prostatic 5.alpha.-reductase

Journal of Medicinal Chemistry, 1984
A series of A-ring heterocyclic steroids has been prepared and tested for inhibition of rat prostatic steroid 5 alpha-reductase in vitro. Strikingly high inhibitory activity was found with a group of 17 beta-substituted 4-methyl-4-aza-5 alpha-androstan-3-ones. These compounds were prepared from 3-keto-delta 4-precursors by oxidative (O3 or NaIO4-KMnO4)
G H, Rasmusson   +6 more
openaire   +2 more sources

Pharmacotherapy of benign prostatic hyperplasia: Inhibitor of 5 alpha-reductase

International Urology and Nephrology, 1997
We studied the effects of 5 alpha-reductase inhibitor (finasteride) in the treatment of benign prostatic hyperplasia (BPH). This study is a randomized controlled trial. Sixty-two patients were treated with 5 alpha-reductase (finasteride 5 mg/day) and 61 patients (control group) with placebo for one year.
BAYRAKTAR, YILMAZ   +4 more
openaire   +3 more sources

[5-alpha-reductase inhibitors].

Acta urologica Belgica, 1995
A reflection is made, on the one hand, on the lack of correlation between the intensity of micturition problems and the volume of the prostate and, on the other hand, on the different therapeutic approaches of irritative or obstructive voiding problems, and finally on the insufficiently convincing activity of Finasteride.
K, De Jaegher, P, Kozyreff, H, Claes
openaire   +1 more source

Finasteride: the first 5 alpha-reductase inhibitor.

Pharmacotherapy, 1993
Finasteride is a synthetic 4-azasteroid that is a specific competitive inhibitor of 5 alpha-reductase, an intracellular enzyme that converts testosterone to dihydrotestosterone (DHT). It has no binding affinity for androgen receptor sites and itself possesses no androgenic, antiandrogenic, or other steroid hormone-related properties.
S L, Sudduth, M J, Koronkowski
openaire   +2 more sources

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