6 citations
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July 2026 in “Zenodo (CERN European Organization for Nuclear Research)” This review evaluates the use of 5α-reductase inhibitors in feminising hormone therapy, finding their additive feminising benefits unclear due to their specific action on testosterone conversion, with concerns highlighted regarding limited supporting evidence and safety signals, particularly for psychiatric and sexual effects.
This review concluded that 5α-reductase inhibitors like finasteride and dutasteride offer limited additional feminising effects in hormone therapy for transfeminine individuals, with the clearest use being androgenetic alopecia treatment; more research is needed for other potential benefits.
14 citations
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April 2024 in “The Journal of Steroid Biochemistry and Molecular Biology” This study found that epitestosterone, a stereoisomer of testosterone, is metabolized to 5α-dihydroepitestosterone by human 5α-reductase enzymes, which enhances its androgenic activity and reduces its antagonistic effect on testosterone-driven androgen receptor signaling.
30 citations
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June 2010 in “Endocrine Related Cancer” In this study, dutasteride more effectively reduced prostate cancer cell viability than finasteride in vitro, but did not significantly alter the angiogenic response.
June 2026 in “Oriental Journal Of Chemistry” This research found that a novel dehydroepiandrosterone derivative (12) significantly reduces cell viability and increases apoptosis in testosterone-stimulated normal and tumor prostate cells, unlike finasteride and dutasteride, which also showed activity under dihydrotestosterone stimulation.
22 citations
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January 2001 in “Chemical & Pharmaceutical Bulletin” This study found that two new progesterone derivatives showed higher antiandrogenic effects and 5α-reductase inhibition than finasteride in hamsters, particularly reducing seminal vesicle weight and flank organ size.
1 citations
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November 2001 in “Acc Current Journal Review” This review found that 5α‐reductase inhibitors were associated with slightly increased rates of decreased libido, erectile and ejaculatory dysfunction, gynecomastia, and mood disorders compared to placebo, though their long-term effects remain unclear.
34 citations
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June 2015 in “Journal of cardiovascular pharmacology and therapeutics” This article discusses the use of direct vasodilators and sympatholytic agents in hypertension management, highlighting their utility in specific cases like refractory hypertension and heart failure, but reports no new clinical results.
8 citations
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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.
January 2019 in “Oncogen” This report suggests that for prostate cancer patients with cardiovascular disease, prescribing the GnRH antagonist degarelix may reduce cardiac events compared to using GnRH agonists, although prescribing should consider potential cardiac risks, particularly in patients with pre-existing conditions or older age.
13 citations
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January 2005 in “Chemical and Pharmaceutical Bulletin” This study reported that newly synthesized progesterone derivatives significantly reduced prostate weight in testosterone-treated hamsters, with 5alpha-reductase inhibitory activity dependent on the size of the substituent at C-17.
January 2024 in “Life sciences” This study observed that in spontaneously hypertensive rats, testosterone's effects on endothelium-dependent vasodilation involved reduced nitric oxide levels, increased oxidative stress, and greater reliance on endothelium-dependent hyperpolarization, with variations in these responses noted when testosterone was combined with either anastrozole or finasteride.
April 2026 in “The Journal of Steroid Biochemistry and Molecular Biology” January 2008 in “Lishizhen Medicine and Materia Medica Research” This study found that the n-butanol extract from Untica mairei Levl's roots significantly inhibited 5α-reductase activity in an in vitro model using rat prostate enzyme.
In a laboratory setting, this study reported that the n-butanol fraction of Urtica laetevirens Maxim. water extracts significantly inhibited 5α-reductase activity.
13 citations
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October 2017 in “Bioorganic & Medicinal Chemistry” This study found that compound 3, a tetrahydropyridoindole carboxymethylated at position 5, significantly inhibited sorbitol accumulation in both rat eye lenses and tissues affected by diabetes, indicating its potential as a lead compound for ALR2 inhibition.
3 citations
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November 1998 in “PubMed” This study found that finasteride significantly inhibits the metabolism of tirilazad to its active metabolites without greatly affecting tirilazad's overall clearance.
52 citations
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January 2005 in “PubMed” This study concluded that alpha(1)-adrenoceptor antagonists are more effective than finasteride in the short term for reducing symptoms of lower urinary tract symptoms associated with benign prostatic hyperplasia.
June 2025 in “Experimental and Сlinical Urology” This research found that the new combination drug Predstanormix Duo, with dutasteride and tamsulosin, is bioequivalent to established treatments for benign prostatic hyperplasia, showing similar pharmacokinetics and safety, potentially improving treatment availability and adherence in high-risk patients.
22 citations
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June 2002 in “Journal of Medicinal Chemistry” This study found that several synthesized compounds were potent inhibitors of human steroid 5alpha-reductase type 2 and reduced prostate weights in treated rats, with compound 15 showing promise for potency in humans.
6 citations
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October 2021 in “Brain Sciences” This study reported that dutasteride, identified through a drug repurposing strategy, showed the potential to reduce neuroinflammation and cognitive impairment in LPS-stimulated models.
15 citations
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June 2019 in “Journal of Neuroendocrinology” This study found that isoallopregnanolone reduced stress-induced tic-like behaviors and sensorimotor gating deficits in a mouse model of Tourette syndrome, suggesting potential therapeutic properties comparable to existing treatments like haloperidol and finasteride.
38 citations
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January 2005 in “PubMed” This study found that dutasteride effectively improves symptoms of benign prostatic hyperplasia, showing benefits in urinary flow and quality of life, with only modestly elevated sexual side effects compared to placebo.
1 citations
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October 2020 in “Current Drug Discovery Technologies” This study investigated various synthesized 5-reductase inhibitors and found that compound 6 had the highest anti-androgenic activity and receptor affinity compared to finasteride, showing potential due to its improved efficacy and bioavailability for further research in treating lower urinary tract symptoms.
36 citations
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July 2005 in “Journal of Neuroendocrinology” This study suggests that both the central biosynthesis and metabolism of progesterone to 3α,5α‐THP in the ventral tegmental area are crucial for facilitating lordosis in female rats.
6 citations
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November 2004 in “Bioorganic & Medicinal Chemistry Letters” This study found that arylhydantoin and arylthiohydantoin derivatives with hydroxybutyl or methyl side-chains showed superior androgen receptor binding affinity and may serve as promising radioiodinated AR ligands.
June 2008 in “Drugs & therapy perspectives” Dutasteride effectively treats benign prostatic hyperplasia, improving symptoms and quality of life.
3 citations
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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.
October 2019 in “European heart journal” This study found that androgen deprivation therapy is associated with an increased risk of acquired long-QT syndrome and Torsades de Pointes, particularly highlighting enzalutamide's greater association with sudden death compared to other therapies.
1 citations
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March 2009 in “The Journal of Urology” This review discusses trials on therapies for benign prostatic hyperplasia and reports that combination treatment is more effective than monotherapy for symptom relief and slowing disease progression in men with moderate to severe symptoms and enlarged prostate glands.