17 citations
,
October 2003 in “Brazilian Journal of Medical and Biological Research” This study found that SDR5A1 gene expression was similar between hirsute women, normal women, and men, suggesting it may not explain differences in hair growth among these groups.
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.
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.
27 citations
,
February 2005 in “Journal of Cellular Biochemistry” This study found that rat male costochondral chondrocytes, unlike female chondrocytes, respond to testosterone through metabolism to dihydrotestosterone, which shows a maturation-state dependent effect in male growth plate cells.
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.
7 citations
,
August 1996 in “The Journal of Clinical Endocrinology and Metabolism”
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.
10 citations
,
August 2014 in “Skin research and technology” This study found that variations in sleep patterns, free testosterone, and 5-alpha-reductase type 1 activity are associated with changes in sebum excretion in women, which may contribute to variability in acne studies.
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
,
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.
March 2010 in “The Journal of Urology” This study demonstrated that methylation of the 5-alpha reductase type 2 (5-AR2) promoter is linked to reduced expression of the 5-AR2 protein, possibly explaining resistance to Finasteride in some BPH patients.
5 citations
,
November 2015 in “Journal of Enzyme Inhibition and Medicinal Chemistry” This study found that aliphatic ester moieties in 16-formyl-17-methoxy dehydroepiandrosterone derivatives increased their potency as 5α-reductase type 2 inhibitors in vitro compared to finasteride.
63 citations
,
November 1999 in “British journal of dermatology/British journal of dermatology, Supplement” This study observes the expression of mRNA for androgen receptor, 5α‐reductase, and 17β‐hydroxysteroid dehydrogenase in human dermal papilla cells.
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.
May 2022 in “bioRxiv (Cold Spring Harbor Laboratory)” This study found that intracrine androgen signaling, mediated by steroid 5α-reductase, is essential for optimal decidualization and vascular development in the endometrium during pregnancy, indicating potential targets for improving age-related fertility issues.
4 citations
,
November 2022 in “Frontiers in endocrinology” This study found that intracrine androgen signaling via 5α-reductase is essential for optimal endometrial decidualization and vascular development during this process in mice.
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.
12 citations
,
February 1997 in “British Journal of Dermatology” This study found that 5α–reductase activity is higher in infrainfundibular keratinocytes compared to interfollicular epidermal keratinocytes, suggesting a potential role in acne-related follicular changes.
22 citations
,
August 2011 in “Journal of Supercritical Fluids” In this study, fraction No. 3 of Oryza sativa bran extract demonstrated high unsaturated fatty acid content and significant 5α-reductase inhibition, suggesting potential for developing anti-androgenic alopecia products.
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.
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.
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.
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.
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.
56 citations
,
December 2002 in “The Journal of Clinical Endocrinology & Metabolism” This study suggests that in human osteoblast-like cells, the 5alpha-reductase type 1 isozyme predominantly catalyzes the conversion of testosterone to DHT, which may play a role in bone homeostasis.