In this study, the researchers reported that the optimized compound 39 demonstrated potent AR antagonism and favorable pharmacokinetics in a hair-growth mouse model, achieving similar efficacy to pyrilutamide with faster onset and preserved safety, offering promise for next-generation topical AR antagonist development.
April 2026 in “Frontiers in Medicine” This study analyzed data from the FDA Adverse Event Reporting System and found that enfortumab vedotin, used for urothelial carcinoma, is linked to various cutaneous adverse events, including severe reactions like Stevens–Johnson syndrome, typically occurring early in treatment and predominantly affecting elderly male patients.
441 citations
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May 2008 in “British Journal of Pharmacology” This article reviews the potential clinical use of anabolic steroids in treating muscle loss from chronic diseases and aging and highlights both the benefits and risks of these substances in sports.
January 2016 in “The Korean Journal of Internal Medicine” This case report presents the first instance in Korea of unilateral gynecomastia and breast pain associated with doxazosin use.
1 citations
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November 2008 in “Acta crystallographica” This study reports the crystallization of the human androgen receptor's ligand-binding domain with nonsteroidal ligands, which may aid in understanding the differences in binding compared to steroidal ligands.
The document explains how certain drugs block hormones to treat cancers like breast and prostate cancer.
July 2026 in “Journal of Enzyme Inhibition and Medicinal Chemistry” This review discusses the evolution of Cereblon ligands in PROTAC technology, highlighting chemical innovations that may enhance drug-likeness and applicability in protein degradation, while noting challenges and future research directions.
This study found that the optimized topical AR antagonist 39, derived from 14-P1, demonstrated potent AR antagonism and comparable efficacy to pyrilutamide in a hair-growth mouse model, with a faster onset and favorable safety profile.
5 citations
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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.
14 citations
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December 1998 in “The Journal of Clinical Endocrinology and Metabolism” This study found that MENT is 10 times more potent than testosterone in suppressing gonadotropins and contributing to anabolism in monkeys, with a potentially wider therapeutic index for human androgen replacement and male contraception.
34 citations
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December 2012 in “Current Opinion in Clinical Nutrition and Metabolic Care” This review discusses the potential of DHEAS and testosterone treatments to increase muscle mass in older men with sarcopenia, while effects on muscle function and physical performance remain unclear, and calls for further research on optimized approaches.
6 citations
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August 2024 in “Steroids”
This study reports that the newly optimized AR antagonist 39 demonstrated effective hair growth and safety in a mouse model of androgenetic alopecia, showing comparable efficacy to pyrilutamide with faster response and favorable pharmacokinetics, due to innovative structural design and dual metabolic inactivation strategy.
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.
6 citations
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January 2018 in “Pharmacoepidemiology and Drug Safety” In this study, 5-α reductase inhibitors were not significantly linked to increased rhabdomyolysis risk, but they may raise the risk of myopathy and myositis in men aged 66 and older.
42 citations
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May 2003 in “Mini-reviews in Medicinal Chemistry” This study found that newly synthesized steroidal trienones demonstrated stronger 5α-reductase inhibitory activity compared to dienones in various biological models, suggesting potential for developing enhanced antiandrogenic drugs.
12 citations
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December 2012 in “Current Drug Targets” The Androgen Receptor could be a target for treating diseases like cancer, but more research is needed to confirm the effectiveness of potential treatments.
September 2003 in “Reactions Weekly” 8 citations
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June 2023 in “European Journal of Endocrinology” This study identified serum androsterone as a robust biomarker for monitoring response to AKR1C3 inhibitor treatment in women and found that a 4-week administration of aldo-keto reductase 1C3 inhibitors did not impact ovarian function.
June 2023 in “Sri Lanka Journal of Menopause”
20 citations
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June 2007 in “Recent Patents on Endocrine, Metabolic & Immune Drug Discovery” This review summarizes recent research and patents on 17β-HSD3, 17β-HSD5, and 3α-HSD3 inhibitors, suggesting their potential in treating androgen-dependent diseases, but reports no new clinical results.
January 2026 in “Zenodo (CERN European Organization for Nuclear Research)” This study reports the discovery of LX-38, a novel non-steroidal drug candidate that may offer safer treatment for conditions like Benign Prostatic Hyperplasia by avoiding hormonal side effects associated with current therapies.
33 citations
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May 2017 in “Journal of Clinical Oncology” This phase I study reported that ETC-159, targeting Wnt signalling, showed tolerable safety profiles at doses that inhibit its pathway, though bone turnover markers increased, warranting early and regular monitoring. No tumor responses were observed, but two patients achieved stable disease for several cycles.
July 2025 in “Medical Science” This review discusses recent studies on the hepatotoxic effects of anabolic androgenic steroids and selective androgen receptor modulators, including liver damage, tumors, and related conditions, and reports no new primary research results.
67 citations
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October 2005 in “Annals of Oncology” This review found that fulvestrant is well tolerated in postmenopausal women with hormone receptor-positive advanced breast cancer, showing lower incidence of joint disorders than non-steroidal aromatase inhibitors.
68 citations
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April 2002 in “Journal of Alternative and Complementary Medicine” This study suggests that botanical 5AR inhibitors like Serenoa repens and β-sitosterol may improve symptoms of androgenetic alopecia, with 60% of treated subjects showing improvement compared to placebo.
June 2020 in “bioRxiv (Cold Spring Harbor Laboratory)” In male mice and rats, this study found that 17α-estradiol improves metabolic health by acting through estrogen receptor α, suggesting a potential target for treating chronic diseases in male mammals.
186 citations
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December 2011 in “Molecules” This study reported that while no synthesized compounds surpassed finasteride in 5α-reductase inhibitory activity, certain 4-azasteroid-2-oximes exhibited notable inhibition.
In this study, a dual soft drug design strategy improved the AR antagonist candidate 39, showing potent AR antagonism and good safety in a mouse hair-growth model, with similar efficacy to pyrilutamide but faster response.
In this study, bicalutamide at low doses was not linked to significant liver enzyme changes compared to other androgen-blocking treatments in transfeminine adolescents and young adults, suggesting its safety with careful monitoring for this population over one year.