6 citations
,
August 1996 in “The Journal of Clinical Endocrinology and Metabolism” MK-386 and finasteride together effectively reduce DHT levels, potentially treating acne and male pattern baldness.
53 citations
,
June 1993 in “Proceedings of the National Academy of Sciences of the United States of America” This study identified LY191704 as a specific noncompetitive inhibitor of human 5 alpha-reductase type 1, which may be useful in treating endocrine disorders related to DHT overproduction.
7 citations
,
August 1996 in “The Journal of Clinical Endocrinology and Metabolism” 12 citations
,
April 1995 in “Journal of Medicinal Chemistry” In this study, 4-substituted N-(1,1-dimethylethyl)-3-oxo-4-androstene-17.beta.-carboxamides were synthesized and evaluated in vitro as potential 5 alpha-reductase inhibitors and antiandrogens.
August 2025 in “ACS Omega” This study synthesized and evaluated hydroxycinnamate derivatives for their ability to inhibit human SRD5A1, finding that three compounds showed significant inhibitory activity and low cytotoxicity. Compound 10a notably reduced SRD5A1 protein expression in cells, suggesting potential for nonsteroidal treatment of androgen-related conditions.
49 citations
,
January 2004 in “Journal of steroid biochemistry and molecular biology/The Journal of steroid biochemistry and molecular biology” This review discusses the development and selectivity of 5 alpha-reductase inhibitors, particularly non-steroidal ones, and reports no new clinical trial results.
August 2025 in “OPAL (Open@LaTrobe) (La Trobe University)” This study found that hydroxycinnamate derivatives, especially a compound named 10a, effectively inhibited SRD5A1 activity and protein expression in cell assays, suggesting potential for treating androgen-related conditions.
1 citations
,
December 2021 in “Natural Product Research” In this study, in silico screening and molecular simulations identified β-sitosterol and brassicasterol as stable potential inhibitors of 5α-reductase1, suggesting they could be explored for androgenic alopecia treatment.
11 citations
,
May 1996 in “The Journal of clinical endocrinology and metabolism/Journal of clinical endocrinology & metabolism” This study reported that 5 alpha-reductase type 2 is the predominant enzyme in pubic skin fibroblasts across normal men, women, and hirsute patients, suggesting potential treatment options for idiopathic hirsutism.
8 citations
,
June 2017 in “Steroids” This study evaluated novel steroid compounds for their ability to inhibit 5α-reductase, showing that compound 16a significantly reduced rat prostate weight more than epristeride and exhibited excellent in vitro inhibitory potency, indicating its potential as a lead candidate for further benign prostatic hyperplasia drug research.
1 citations
,
March 1997 in “Journal of Chromatography B: Biomedical Sciences and Applications” This study discovered that the disposition of LY191704 enantiomers in rats and dogs is both stereoselective and species specific.
47 citations
,
January 2003 in “Current opinion in urology” This review discusses recent advancements in understanding the use of 5 alpha-reductase inhibitors for benign prostatic hyperplasia, indicating that dual isoenzyme inhibitors like dutasteride may enhance treatment outcomes, but no new clinical results are presented.
This study identified distinct and significant adverse event patterns across different drug classes used to treat benign prostatic hyperplasia, confirming known risks and suggesting novel safety signals for further investigation.
This study analyzed the FDA Adverse Event Reporting System and found distinct safety signals and adverse event patterns among α1-blockers, 5α-reductase inhibitors, and tadalafil used in treating benign prostatic hyperplasia, emphasizing known risks and identifying potential new ones that require further study.
March 2026 in “The Aging Male” This retrospective pharmacovigilance study reviewed adverse event reports from 2004 to 2025 for drugs treating benign prostatic hyperplasia, identifying distinct safety signals for α1-blockers, 5ARIs, and PDE5I, including some potential new adverse events that require further investigation.
9 citations
,
November 2004 in “Bioorganic & Medicinal Chemistry Letters” This study identified potent dual inhibitors of 5α-reductases 1 and 2 that may aid in designing new drugs for related diseases.
28 citations
,
May 2018 in “Scientific reports” This study found that exercise decreases the expression of 5αR1, thereby enhancing the PI3K/AKT signaling pathway in PCOS rats.
3 citations
,
June 2018 in “Bioorganic & medicinal chemistry” This study identified that derivatives 4, 4b, and 4c strongly inhibited the enzyme type 1 5α-reductase and decreased reproductive organ weights in hamsters, suggesting potential as prodrugs for prostate tumor growth inhibition.
12 citations
,
June 2001 in “Bioorganic & Medicinal Chemistry” This study found that octahydrobenzo[c]quinolizin-3-one derivatives, particularly compound 3, were potent and selective inhibitors of the enzyme 5α-reductase type 1.
124 citations
,
January 1996 in “Dermatology” This article reviews the biochemical properties of 5 alpha-reductase isoforms and highlights the limited dermatological use of inhibitors like finasteride, especially for type 1 isozyme-targeting agents, while suggesting further clinical exploration.
20 citations
,
June 1995 in “Tetrahedron Letters” This study reported that newly synthesized phenanthridin-3-one derivatives effectively inhibit human steroid 5-α-reductase.
28 citations
,
September 2000 in “Journal of Medicinal Chemistry” This study identified novel compounds as selective inhibitors of the type 1 isoenzyme of 5α-reductase, displaying promising potential for treating DHT-dependent disorders such as acne and androgenic alopecia.
8 citations
,
March 2002 in “Archiv Der Pharmazie” In this study, 4-(4-(phenylaminocarbonyl)benzoyl) benzoic acid exhibited the strongest inhibitory activity against the human type 2 steroid 5α-reductase isozyme among the compounds tested.
45 citations
,
September 2000 in “Archives of dermatology” This study found that 5alpha-reductase type 1 localizes specifically to sebaceous glands in both normal and acne follicles, suggesting its role in sebum regulation.
July 2023 in “Dermatology and Therapy” This review analyzed the use of 5-alpha reductase inhibitors (5ARIs) for treating various dermatological conditions such as androgenetic alopecia, acne, and hirsutism, emphasizing their efficacy and safety profile.
15 citations
,
July 2016 in “Urologic Clinics of North America” This study found that combining 5-alpha reductase inhibitors with alpha-blockers provided the best symptomatic relief and reduced the risk of clinical progression for BPH, while PDE5 inhibitors could offset sexual side effects.
13 citations
,
August 2007 in “Bioorganic & medicinal chemistry letters” This study developed a new competitive 5alpha-reductase inhibitor with an IC(50) of 0.84 microM using a novel chemical structure.
237 citations
,
December 2001 in “Urology” This review discusses the role of 5α-reductase in prostate development and BPH, and reports no new clinical results; ongoing trials are exploring dual isozyme inhibitors for improved treatment efficacy.
January 2014 in “프로그램북(구 초록집)” This article reviews updates on 5 alpha-reductase inhibitors for treating male pattern hair loss and presents no new clinical findings; the author aims to enhance understanding of these therapies.
184 citations
,
January 2000 in “European Urology” This abstract reviews the role of finasteride and potential dual 5alpha-reductase inhibitors in treating benign prostatic hyperplasia, suggesting that dual inhibitors may offer greater DHT suppression and therapeutic advantages, while emphasizing the need for clinical evaluation.