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.
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.
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.
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.
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.
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.
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.
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.
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.
20 citations
,
June 1995 in “Tetrahedron Letters” This study reported that newly synthesized phenanthridin-3-one derivatives effectively inhibit human steroid 5-α-reductase.
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.
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.
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.
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.
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.
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.
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.
17 citations
,
November 1997 in “Andrology” Finasteride effectively treats enlarged prostate and male baldness, improves symptoms of hirsutism in women, but doesn't work for acne, and may delay prostate cancer progression with few side effects.
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.
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.
17 citations
,
December 2015 in “BMC Complementary and Alternative Medicine” This study found that Avicennia marina extract significantly inhibited 5α-reductase type 1 activity in human hair dermal papilla cells, suggesting its potential use for treating androgenic alopecia.
1 citations
,
October 2019 in “مجله كليه طب الكندي” In this study, researchers highlight the role of androgens like dihydrotestosterone in the pathophysiology of acne, pointing to the enzyme 5a-reductase type 1 as potentially more active in individuals with acne, which may contribute to hormonal influences in the condition's development.
March 2014 in “The Journal of Urology” In this study, treatment with a 5a-reductase inhibitor increased CD8+ T cell infiltration in benign prostatic hyperplasia tissues, suggesting an impact on inflammatory responses.
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.
10 citations
,
January 2018 in “Functional Foods in Health and Disease” This study found that berry extracts, especially black raspberry extract, may have anti-aging effects due to their high antioxidant activities.
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.
16 citations
,
April 2017 in “Journal of Cosmetic Dermatology” This study found that fig leaf extract significantly downregulated inflammatory and androgenic gene expression in vitro, suggesting potential topical benefits for certain skin disorders.
2 citations
,
January 2004 in “Enshou saisei” This study suggests that beard dermal papilla cells may produce androgen-dependent growth factors that stimulate keratinocyte proliferation, while frontal scalp cells can have an inhibitory effect mediated by TGF-β1.
This review discusses treatments for androgenic alopecia, noting that current options like finasteride and minoxidil are effective for only 10% of patients, thus highlighting the need for new therapies.