1 citations
,
April 2023 in “Heliyon” In this study, a 68-year-old man with muscle-invasive bladder cancer and renal insufficiency achieved a partial radiological response to neoadjuvant therapy with gemcitabine and Disitamab Vedotin, without significant adverse events, highlighting a potential alternative for cisplatin-ineligible patients.
72 citations
,
June 1979 in “Biochemical Society Transactions” This research paper reviews the anti-androgenic properties of the drug flutamide and its metabolite Sch 16423 but presents no new experimental results.
This study found that the optimized AR antagonist candidate 39, in a hair-growth mouse model, achieved similar efficacy to pyrilutamide with faster onset and favorable safety, suggesting a promising approach for developing topical treatments with low systemic toxicity for androgenetic alopecia.
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.
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.
1 citations
,
July 2020 in “Reviews in separation sciences” This study developed a simple method to determine finasteride, indapamide, and tiemonium methylsulfate in pharmaceuticals by using their ability to form silver nanoparticles measurable via spectrophotometry.
In this study, researchers optimized the soft drug AR antagonist 14-P1 to create candidate 39, which demonstrated effective AR antagonism and safety in a hair-growth mouse model, showing similar efficacy to pyrilutamide but with quicker onset and a lower risk of systemic toxicity.
15 citations
,
April 2011 in “The journal of investigative dermatology/Journal of investigative dermatology” This study found that A(3)B(5) downregulates melanin production and suppresses melanoma cell growth by promoting proteasomal degradation of TRP-2.
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.
6 citations
,
September 2015 in “Journal of Medicinal Chemistry” This study synthesized and verified the structures of Setipiprant's major and minor metabolites, confirming their regio- and enantioselectivity from earlier proposals in a clinical study.
March 2014 in “Oxford University Press eBooks” This narrative review explores the failure of fludalanine as an orally active antibiotic and highlights valuable insights into problem-solving strategies in drug discovery, without reporting new clinical results.
7 citations
,
July 2018 in “Biological & Pharmaceutical Bulletin” This study found that Phyllanthus urinaria extract displayed significant anti-alopecia properties in a mouse model, showing potential as an anti-5α-reductase agent for androgenic hair loss.
January 2023 in “IntechOpen eBooks” This chapter reviews various synthetic methods for creating pharmacologically active diazines, particularly focusing on pyrimidines, and discusses their potential in clinical applications. It also examines novel synthetic strategies that improve the drug-like qualities and safety profiles of these compounds.
26 citations
,
January 2005 in “PubMed” This study reports that RU 58841-myristate, a new antiandrogen prodrug formulated with solid lipid nanoparticles, shows potential for targeting hair follicles in preclinical laboratory settings.
9 citations
,
November 2017 in “International Journal of Nanomedicine” This animal study found that intravenous administration of anionic squarticles, a lipid nanoemulsion, increased survival rates in rats with amitriptyline overdose by mitigating adverse effects and restoring normal blood pressure, highlighting its potential as a detoxifying antidote.
8 citations
,
April 2020 in “Journal of The American Academy of Dermatology” This article discusses the potential of oral bicalutamide as a promising treatment for female pattern hair loss and reports no new clinical results.
42 citations
,
February 1998 in “The Journal of Steroid Biochemistry and Molecular Biology” This study found that PNU 157706 is a highly potent inhibitor of human 5α-reductase enzymes, showing a stronger and longer-lasting antiprostatic effect in rats compared to finasteride.
21 citations
,
January 2021 in “Frontiers in Pharmacology” This review examines the role of thiopurines in managing inflammatory bowel diseases like ulcerative colitis and Crohn's disease, and reports no new clinical results, emphasizing the need for more studies on thiopurine withdrawal scenarios.
This study found that four synthesized thiazolidinone derivatives showed potential anticancer activity against MCF7 and HeLa cell lines, suggesting their further investigation for anticancer drug development.
16 citations
,
October 1994 in “The Journal of Steroid Biochemistry and Molecular Biology” Two non-steroidal antiandrogens, RU 58841 and RU 56187, form a common metabolite at different rates, which may influence their effects; RU 56187 could be used for prostate cancer treatment and RU 58841 for acne treatment.
January 2019 in “Nihon Yakuri Gakkai nenkai yoshishu” This article reviews guidelines and medications for treating benign prostatic hyperplasia but presents no new clinical results.
January 2020 in “International Journal of Research in Pharmacy and Chemistry” This study developed a validated HPLC method for accurately estimating dutasteride and its related compounds in capsules, suitable for routine and stability sample analysis.
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.
December 2005 in “Endocrine-related cancer” This case report describes a 57-year-old woman's virilizing adrenal tumor effectively treated with the antiandrogen cyproterone acetate, which led to symptom reversal and tumor resolution.
November 2025 in “Drug Testing and Analysis” This study investigated the metabolic pathways of epristeride, a new Type II 5α‐reductase inhibitor, using in vitro models and found that its metabolites show significant interactions with key proteins, suggesting implications for its role in doping control.
This invention reports piperazine derivatives as potent inhibitors of type 3 17β-hydroxysteroid dehydrogenase, suggesting potential therapeutic applications in treating prostate cancer, acne, and androgenic alopecia.
20 citations
,
June 1995 in “Tetrahedron Letters” This study reported that newly synthesized phenanthridin-3-one derivatives effectively inhibit human steroid 5-α-reductase.
May 2024 in “Journal of molecular structure” This study found that a novel thiohydantoin derivative, 3a, effectively inhibited androgen receptor activity in LNCaP cells and showed promising in vivo results by reducing testosterone-induced prostate changes, outperforming finasteride in mitigating prostate index and histopathological alterations.
3 citations
,
January 2021 in “Minia Journal of Medical Research” This study observed that a single intraperitoneal injection of cyclophosphamide caused significant destruction of the intestinal mucosa in albino rats.
13 citations
,
May 2011 in “Bioorganic & Medicinal Chemistry” This study identified certain benzopyran derivatives with a bulky tert-butyloxycarbonylamino group as effective KATP channel openers that inhibit insulin secretion in rat pancreatic islets.