20 citations
,
June 1995 in “Tetrahedron Letters” This study reported that newly synthesized phenanthridin-3-one derivatives effectively inhibit human steroid 5-α-reductase.
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.
3 citations
,
October 1994 in “Journal of Labelled Compounds and Radiopharmaceuticals” This synthesis report details the successful development of a C-14 labeled isotopomer of LY300502, a 5α-reductase inhibitor, through a multi-step radiochemical process.
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.
10 citations
,
May 2019 in “BMC Complementary and Alternative Medicine” This study found that Bacillus/Trapa japonica fruit ferment filtrate extracts enhanced human hair follicle dermal papilla cell proliferation through the Akt/ERK/GSK-3β signaling pathway, suggesting potential benefits for alopecia treatment.
31 citations
,
August 2001 in “PubMed” This review discusses the role of androgen metabolism in hair follicles and its potential impact on future treatments for androgenetic alopecia, but reports no clinical results.
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.
31 citations
,
January 2017 in “Advances in Experimental Medicine and Biology” This review discusses the negative health impacts of testosterone deficiency and the potential adverse effects of 5α-reductase inhibitors, emphasizing the need for patient-physician discussions regarding these treatments.
45 citations
,
August 2010 in “Hormone Molecular Biology and Clinical Investigation” This study found that SRD5a-3 is a highly efficient enzyme for converting hormones into androgens, with dutasteride being a much more potent inhibitor of SRD5a-3 than SRD5a-2.
13 citations
,
August 1995 in “The Journal of Steroid Biochemistry and Molecular Biology” This study found that the pH dependency of rat steroid 5α-reductase type II isozyme significantly affects its kinetic properties, including Vmax and Km, suggesting past discrepancies in literature may arise from these pH variances during assays.
June 2023 in “Oriental Journal of Chemistry/Oriental journal of chemistry” This study demonstrated that derivatives of dehydroepiandrosterone (2a-b, 3a-f, and 4a-f) significantly reduced viable LNCaP prostate cancer cells, suggesting potential therapeutic use for metastatic prostate cancer, while finasteride did not alter cell viability.
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.
89 citations
,
February 1993 in “Journal of Medicinal Chemistry” This research article focuses on nonsteroidal inhibitors of human type I steroid 5-alpha-reductase but reports no new results.
46 citations
,
October 1999 in “Journal of The American Academy of Dermatology” This study found that finasteride at 1 mg/day was the most effective dose for treating male pattern hair loss, with similar efficacy to 5 mg/day and better results than lower doses.
22 citations
,
February 2002 in “Planta Medica” In this study, osthenol was identified as a highly potent inhibitor of 5alpha-reductase type I in LNCaP cells, significantly outperforming finasteride.
1 citations
,
October 2013 in “Our Dermatology Online” This study found that individuals in this Egyptian cohort carrying the leucine (L) allele of the 5-α reductase type II enzyme had a higher risk of developing androgenetic alopecia, which may be associated with oxidative stress.
5 citations
,
February 1997 in “Bioorganic & Medicinal Chemistry” This study found that among 17 beta-(N-ureylene-N,N'-disubstituted)-4-azasteroids, those with an N'-phenyl moiety were the most effective inhibitors of human type I 5 alpha-reductase.
22 citations
,
October 2001 in “Biochemical Pharmacology” This study found that GI198745 acts as a time-dependent inhibitor of rat 5α-reductase type 2 but a rapid-equilibrium inhibitor of type 1, potentially making it more effective than finasteride in preventing rat prostate growth.
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.
39 citations
,
April 2018 in “Hormones” This review suggests that most mutations in the SRD5A2 gene show no clear genotype-phenotype correlation in 5-α-Reductase deficiency, although mutation location affects severity.
October 2022 in “Endocrine journal” In this study of male patients with 46,XY 5α-reductase type 2 deficiency, DHT therapy was effective in achieving penile enlargement during infancy, while testosterone replacement therapy proved more beneficial during puberty, possibly due to increased conversion to DHT.
March 2016 in “European Urology Supplements” This study identified that methylation of the 5-AR2 gene promoter is linked to reduced expression of 5-AR2 protein, which may explain why some BPH patients are resistant to finasteride treatment.
19 citations
,
May 2014 in “Molecules” This study found that the methanolic heartwood extract of Avicennia marina significantly inhibits 5α-reductase type 1, reducing 5α-DHT production by 52% in a cell-based assay with human hair dermal papilla cells.
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.
29 citations
,
January 1996 in “Journal of Pharmaceutical Sciences” This study developed a theoretical model that suggests finasteride may completely inhibit 5AR type 2, but not sufficiently suppress type 1, leading to only partial reduction of dihydrotestosterone at clinical doses.
January 2026 in “Frontiers in Natural Products” This study found that combining shikimic acid with Prunus mume fruit extract significantly reduces type I 5α-reductase levels in testosterone-stressed skin sebocytes, surpassing the effects of shikimic acid or standard acne treatments alone, and shows promise for stable, non-irritating acne remedies in cosmetic formulations.
45 citations
,
January 2012 in “The Journal of Steroid Biochemistry and Molecular Biology” This study found that overexpression of AKR1C3 in prostate cancer cells redirected androgen metabolism towards testosterone production, which facilitated cell proliferation, potentially reducing the effectiveness of finasteride treatment.
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.
218 citations
,
December 2011 in “Advances in Urology” This review discusses the biochemical properties and clinical significance of 5 alpha-reductase isozymes and reports no new clinical results.
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.