23 citations
,
October 2008 in “Journal of medicinal chemistry” This study suggests that PF-0998425 is an effective androgen receptor antagonist for sebum control and androgenetic alopecia with rapid metabolism reducing the risk of systemic side effects.
2 citations
,
November 2017 in “Elsevier eBooks” This article discusses the role of the androgen receptor in regulating development and homeostasis, and reviews treatment approaches for conditions related to hormone imbalances, without reporting new clinical findings.
204 citations
,
February 2000 in “Current Medicinal Chemistry” This review discusses the use of antiandrogens like flutamide and its derivatives in prostate cancer treatment and highlights the need for next-generation antiandrogens for improved efficacy; it reports no new clinical results.
11 citations
,
May 2010 in “Journal of Medicinal Chemistry” This study introduced a novel nonsteroidal androgen receptor antagonist that effectively controls sebum production in the golden Syrian hamster ear model through targeted follicular delivery.
17 citations
,
January 2015 in “MedChemComm” New treatments for prostate cancer are less toxic and show promise, but more research is needed to enhance their effectiveness and reduce side effects.
11 citations
,
February 2016 in “Current Medicinal Chemistry” This review discusses various targets for treating prostate cancer and benign prostatic hyperplasia and reports on recent studies of new compounds and 5α-reductase inhibitors, but provides no new experimental results.
September 2024 in “Journal of Cutaneous and Aesthetic Surgery” This review focuses on the pharmacological properties, indications, contraindications, and safety profile of bicalutamide, a non-steroidal androgen receptor antagonist, in dermatological research, particularly its off-label use for improving female pattern hair loss as measured by Sinclair grading.
14 citations
,
November 2006 in “Current Medicinal Chemistry” This review discusses recent developments in α1-adrenoceptor antagonists and 5α-reductase inhibitors for treating benign prostatic hyperplasia, reporting no new clinical results while identifying potential areas for future drug development.
36 citations
,
October 2009 in “Journal of biological chemistry/The Journal of biological chemistry” This study reports that TFM-4AS-1, a selective androgen receptor modulator, promoted bone and muscle growth with reduced effects on reproductive organs in ovariectomized rats.
72 citations
,
January 2003 in “American Journal of Pathology” This study found that the co-activator CBP enhances the agonistic action of hydroxyflutamide on androgen receptors, suggesting a mechanism for therapy resistance in prostate cancer.
20 citations
,
May 2011 in “Cancer Biology & Therapy” This study found that finasteride decreased DHT-stimulated AR activity and cell growth in prostate cancer cells with mutant AR, but not in those with wild type AR.
7 citations
,
January 1994 in “Annual Reports in Medicinal Chemistry” This review discusses hormonal manipulation for conditions like prostatic disorders and skin issues and highlights promising treatments like casodex and finasteride, but it reports no new clinical results.
June 2026 in “HAL (Le Centre pour la Communication Scientifique Directe)” This article presents the SH-1 molecule as a novel AR antagonist for androgenetic alopecia treatment, highlighting its tissue-specific action and potential for commercialization, but provides no new clinical results.
June 2026 in “Zenodo (CERN European Organization for Nuclear Research)” This source describes SH‑1 as a next-generation androgen receptor antagonist designed for localized treatment of androgenetic alopecia, aiming to reverse follicular miniaturization while maintaining endocrine balance. Unlike traditional therapies, SH‑1 offers tissue-specific action, avoiding systemic effects.
25 citations
,
June 2019 in “Endocrine Related Cancer” This review discusses the structure and function of steroid nuclear receptors, particularly focusing on androgen receptor dysregulation in prostate cancer and androgen insensitivity syndromes, without reporting new experimental results.
5 citations
,
January 2005 in “Journal of Enzyme Inhibition and Medicinal Chemistry” This study found that certain steroidal compounds, especially 10a–10c, demonstrated strong antiandrogenic activity by binding to the androgen receptor and reducing prostate weight in a hamster model.
The document explains how certain drugs block hormones to treat cancers like breast and prostate cancer.
20 citations
,
September 2005 in “Endocrinology” This study identified novel selective androgen receptor modulators with enhanced in vivo pharmacological activity through structure-activity relationship analysis in castrated rats.
1 citations
,
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.
September 2012 in “The Egyptian Journal of Histology” In this study, flutamide at therapeutic doses caused significant histological changes in the testes and epididymis of adult albino rats, reducing androgen receptor immunoreactivity and increasing estrogen receptor immunoreactivity.
27 citations
,
January 1984 in “Pharmacology & Therapeutics” This review discusses androgen manipulation strategies for conditions like benign prostatic hyperplasia and prostatic carcinoma but reports no new clinical results.
August 2024 in “Steroids” This review summarizes structural insights into androgen receptor dynamics, highlighting its flexibility in binding numerous partners, which may explain adaptive resistance mutations in cancer and loss of function in androgen insensitivity syndrome.
14 citations
,
September 2015 in “Expert Opinion on Therapeutic Targets” This review discusses potential treatments for androgen excess in polycystic ovary syndrome and reports no new findings, emphasizing the importance of individualized antiandrogenic management to minimize side effects.
3 citations
,
January 2016 in “Elsevier eBooks” This article discusses the various roles of steroids in vertebrate organ systems and notes several glucocorticoids that were among the Top 200 Drugs by sales in the 2010s, but it reports no new clinical findings.
1 citations
,
January 2001 in “Endocrine Practice” This study suggests that topical finasteride may benefit women with facial hirsutism, based on observations from a small sample.
August 2025 in “Fabad Journal of Pharmaceutical Sciences” This review highlights that bicalutamide, a non-steroidal antiandrogen used in prostate cancer treatment, is mainly effective through its (R)-enantiomer and emphasizes the need to monitor its adverse effects despite its targeted antiandrogenic action.
11 citations
,
August 1997 in “Expert Opinion on Therapeutic Patents” This review discusses nearly 70 patent applications for the treatment of androgenetic alopecia and other hair conditions, highlighting the mechanisms of action explored but reports no clinical results.
40 citations
,
September 2019 in “Molecular and Cellular Endocrinology” This paper discusses mechanisms by which various chemicals disrupt male sexual differentiation, concluding that mixture risk assessments should include a broader set of compounds beyond phthalates to address cumulative reproductive health risks.
23 citations
,
May 2019 in “Expert Opinion on Therapeutic Patents” This review discusses AR-modulating agents developed between 2012 and 2018, highlighting challenges with ligand-binding domain antagonists and proposing nonconventional approaches targeting other domains as promising strategies.
December 2022 in “CRC Press eBooks” This research outlines that antiandrogens have mechanisms involving competitive inhibition of androgen binding and enzyme inhibition, with contraindications during pregnancy due to potential fetal risks.