flutamide / Generic mfg. - LARVOL DELTA

Sex- and Lineage-Dependent Transgenerational Effects of Vinclozolin and Flutamide on Rat Development and Behavior. (PubMed, J Endocr Soc) - "More behavioral effects of VIN emerged at the F3 generation's paternal lineage compared to the F1 generation. Overall, this study provides more detailed insight into the transgenerational effects of a high dose of VIN exposure and suggests future inquiry into the mechanisms of action of the EDC, specifically as it pertains to its differences from FLUT and its differing effects on lineage, sex, and generation."

Journal • Preclinical • Mood Disorders • Psychiatry

NRG-GU002: Antiandrogen Therapy and Radiation Therapy With or Without Docetaxel in Treating Patients With Prostate Cancer That Has Been Removed by Surgery (clinicaltrials.gov) - P2/3 | N=612 | Completed | Sponsor: NRG Oncology | Active, not recruiting ➔ Completed | Trial completion date: May 2026 ➔ Oct 2025 | Trial primary completion date: May 2026 ➔ Oct 2025

Trial completion • Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Self-assembled xK1 rosette nanotube as a nanocarrier for chemotherapeutic drug molecules: a molecular dynamics study. (PubMed, RSC Adv) - "Chemotherapy is widely recognized as an effective treatment for various types of cancers, relying on chemotherapeutic drugs such as chlorambucil (CBL), camptothecin (CPT), doxorubicin (DOX), and flutamide (FLU) to inhibit cancer cell metastasis through their cytotoxic effects. Furthermore, MD simulations of the release mechanism revealed structural disassembly, validating the responsiveness of the systems under acidic conditions. The findings here offer insights into the viability of xK1 for targeted drug delivery, which warrants further experimental studies."

Journal • Alopecia • Infertility • Oncology • Pain • Sexual Disorders

Anti-androgenic compound Embelin ameliorates polycystic ovary syndrome by reversing the ovarian dysfunction and associated metabolic irregularities in 5α-DHT-induced PCOS rats. (PubMed, Fitoterapia) - "The anti-androgenic activity of the extracted Embelin was evaluated using the Yeast RIKILT Androgen Assay and compared against (i) 5α-dihydrotestosterone (5α-DHT), (ii) a commercially sourced Embelin standard, and (iii) flutamide, a known androgen receptor antagonist. Embelin treatment effectively reversed several hallmark features of PCOS, including ovarian dysfunction (e.g., hypo-progesteronemia, follicular cysts, and estrous cycle irregularities) as well as metabolic disturbances such as insulin resistance, weight gain, dyslipidaemia, and adipocyte hypertrophy. In conclusion, this is the first study to demonstrate the therapeutic potential of Embelin in ameliorating PCOS-related ovarian and metabolic dysfunctions."

Journal • Preclinical • Dyslipidemia • Metabolic Disorders • Polycystic Ovary Syndrome

Cyproterone acetate for hirsutism. (PubMed, Cochrane Database Syst Rev) - "There were some differences in clinical outcome between CPA and spironolactone, CPA and flutamide, and CPA and finasteride. There were no clinical differences between CPA and the other medical therapies, possibly because of small study size, lack of standardised assessment and objective determinants of improvement in many studies. There are insufficient data presented to compare the adverse effects of all the treatment options. Larger, carefully designed studies are needed to compare efficacy and safety profiles between the therapeutic options available."

Clinical • Journal • Review • Gynecology

Sex differences in microglia morphology and function across the lifespan are mediated by the early hormone environment. (PubMed, Brain Behav Immun) - "Testosterone treatment also resulted in greater transcriptomic changes in the aged hippocampus compared to flutamide treatment, especially in genes related to mitochondrial function and inflammation. These results indicate that (1) early hormone environment is critical for the induction of sex differences in microglial morphology and (2) sex differences in microglial morphology reverse during aging, and this reversal is also recapitulated with early hormone treatment."

Journal • Inflammation

Characteristics, treatment patterns and healthcare resource use of Finnish men with prostate cancer. (PubMed, BJUI Compass) - "In the mPC cohort, ADT (92%), radiotherapy (38%) and first-generation antiandrogens bicalutamide or flutamide (22%) were the most common first-year treatments. As expected, the disease burden seems to be higher among men with metastatic disease. The estimated high proportion of patients with mPC at or soon after diagnosis should be interpreted with caution."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Computational discovery of resiniferatoxin and euphol as potential androgen receptor inhibitors for prostate cancer therapy. (PubMed, Comput Biol Chem) - "This screening identified two leading compounds, Resiniferatoxin and Euphol, both demonstrated favorable binding poses and docking scores of -10 kcal/mol and -8.6 kcal/mol, respectively, surpassing Flutamide, the standard antiandrogen (-7.7 kcal/mol). Furthermore, a 100 ns molecular dynamics simulation showed that these two molecules formed stable complexes with AR, suggesting their potential utility as natural AR inhibitors in prostate cancer therapy. However, additional experimental studies are essential to validate their efficacy, elucidate their mechanisms of action, and assess their safety profiles, potentially paving the way for innovative plant-based treatments targeting AR-driven prostate cancer."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Pulp and paper mill industry effluent yields androgenic and anti-androgenic activity and leads to a reproduction arrest in fathead minnow. (PubMed, Environ Pollut) - "While ER activity was low (<0.01 ng/L EEQ (estrogen-equivalent)), AR and anti-AR activities were measured at ∼1.8 ng/L DHT-Eq (dihydrotestosterone equivalent) and at ∼209 μg/L FLU-Eq (flutamide equivalent), respectively...20 out of 150 chemical compounds were quantified, including bisphenol A and S - known EDCs, which yielded ∼500 and 2,000 μg/L, respectively. Overall, this study validates that the approach used can detect EDC activity in a pulp and paper mill effluent, which could help better understand their impacts in receiving aquatic ecosystems."

Journal • ER

Innovative Se-Flutamide Derivatives: Enhanced Activity Toward Androgen Receptor (AR)-Dependent and -Independent Prostate Cancer Cells. (PubMed, Arch Pharm (Weinheim)) - "Besides, it induced the G0/G1 cell cycle arrest. Altogether, it could be concluded that this Se-flutamide analog could be a feasible and promising candidate for further development for the treatment of both AR-dependent and -independent prostate cancers."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AR

Assessing Induction of Double Strand Breaks With Androgen Receptor Partial Agonist in Patients on Androgen Suppression (clinicaltrials.gov) - P1 | N=25 | Completed | Sponsor: Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Active, not recruiting ➔ Completed

Trial completion • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

RTOG 0815: Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer (clinicaltrials.gov) - P3 | N=1538 | Completed | Sponsor: Radiation Therapy Oncology Group | Active, not recruiting ➔ Completed

Trial completion • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Hormone Therapy, Radiation Therapy, and Steroid 17alpha-monooxygenase TAK-700 in Treating Patients With High-Risk Prostate Cancer (clinicaltrials.gov) - P3 | N=239 | Completed | Sponsor: Radiation Therapy Oncology Group | Active, not recruiting ➔ Completed | Trial completion date: Jun 2029 ➔ Sep 2025

Trial completion • Trial completion date • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

ARCH: Contributions to Hypertension With Androgen Deprivation Therapy (clinicaltrials.gov) - P4 | N=10 | Completed | Sponsor: University of Colorado, Denver | Recruiting ➔ Completed | N=228 ➔ 10 | Trial completion date: Mar 2028 ➔ Jul 2025 | Trial primary completion date: Mar 2028 ➔ Jul 2025

Enrollment change • Trial completion • Trial completion date • Trial primary completion date • Cardiovascular • Genito-urinary Cancer • Hypertension • Nephrology • Oncology • Prostate Cancer • Renal Disease • Solid Tumor

Investigating the role of androgen signaling in the PDAC tumor microenvironment Free (AACRPanCa 2025) - "Previous reports describe the treatment of male PDAC patients with the anti-androgen drug flutamide, which resulted in enhanced survival and suggests a pro-tumor role for androgen signaling in PDAC...These data reveal the role of AR signaling in modulating the PDAC TME, ultimately leading to a pro-tumor environment that does not support effective anti-tumor T cell responses. These results are important in understanding the male bias in PDAC incidence and mortality and serve as the groundwork for a novel potential therapeutic target."

Biomarker • IO biomarker • Tumor microenvironment • Fibrosis • Metabolic Disorders • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • CD8 • GZMB • PD-1 • TNFA

Testosterone-mediated regulation of renal GSTA1/2 expression in male mice. (PubMed, J Vet Sci) - "These suggest that testosterone suppresses renal GSTA isoform expression in male mice, with GSTA1/2 being more sensitive to testosterone-mediated inhibition than GSTA3 or GSTA4."

Journal • Preclinical • GSTP1

Androgen receptor antagonist flutamide modulates estrogen receptor alpha expression in distinct regions of the hypospadiac rat penis. (PubMed, Front Endocrinol (Lausanne)) - "Notably, beyond this established androgen-estrogen relationship in hormone-sensitive tissues, anti-androgenic exposure also induced spatial changes in Esr1 expression in specific regions of the GT. Future toxicological testing using new approach methodologies (NAMs) should consider androgen-estrogen balance and crosstalk in reproductive tissues as a mechanism of action."

Journal • Preclinical • ER

A Canadian Consensus on Androgenetic Alopecia: Approach and Management. (PubMed, J Cutan Med Surg) - "Seven interventions are recommended, including oral dutasteride; oral finasteride; topical finasteride; topical minoxidil; platelet-rich plasma; microneedling; and oral minoxidil. Five interventions are recommended with near consensus: intralesional dutasteride; ketoconazole shampoo; low level laser therapy; aminexil; as part of a regimen and 17 are not recommended (adenosine; cetirizine; carboxytherapy; amla syrup; microfilament thread; Nourkrin; injectable minoxidil; caffeine; ceramide; topical herbal formulations; piroctone olamine shampoo or leave-on; rosemary oil; shampoo and lotion hair care products containing fermented papaya, fermented mangosteen, and caffeine; basic Fibroblast Growth Factor (bFGF); flutamide)."

Journal • Alopecia • Immunology • FGF

Analysis of miRNA expression profiles during spermatogenesis of plateau zokor (Eospalax baileyi) under androgen antagonism treatment. (PubMed, Comp Biochem Physiol Part D Genomics Proteomics) - "To explore the mechanism of androgen in spermatogenesis in seasonal breeding animals, this study used the plateau zokor (Eospalax baileyi) as a model and, during the breeding season, treated it with the androgen receptor antagonist, flutamide, to analyze its effect on the microRNA (miRNA) expression profile in testicular tissue...Androgens regulate spermatogenesis in plateau zokors by inhibiting specific miRNAs (such as miR-486-y). This study provides molecular evidence and new perspectives on the regulatory network of seasonal reproduction in animals."

Journal • Inflammation • Metabolic Disorders • ACSL4 • MIR486-1

Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial (clinicaltrials.gov) - P3 | N=2753 | Active, not recruiting | Sponsor: NRG Oncology | Recruiting ➔ Active, not recruiting

Enrollment closed • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor • CD4

C(sp3)H/N(sp2) Cross-Coupling Reaction for the Synthesis of Tertiary Arylamines via Fluxional SOX·Pd(II) Catalysis. (PubMed, J Am Chem Soc) - "The generality of this reaction enables facile synthesis of six pharmaceuticals and derivatives (e.g., zafirlukast) and five late-stage drug fragment couplings (e.g., flutamide-duloxetine). Phosphoric acids promote the reaction by affording a significant increase in the functionalization rate, rendering a lower energy allylic C-H cleavage as the rate-determining step. We anticipate that this reaction will find broad use in the discovery of complex and medicinally relevant N-alkyl arylamines and that the mechanistic insights will be leveraged to improve efficiencies of other metal-catalyzed aminations."

Journal

Metabolic activation of nitro-containing drugs by AKR1C enzymes: A focus on flunitrazepam (ACS-Fall 2025) - "While the reduction of NO2 moieties in drugs is known to be catalyzed by NADPH-dependent flavoenzymes (NADPH:P450 oxidoreductase, NAD(P)H-quinone oxidoreductase [NQO1]), P450 enzymes, and oxidases (aldehyde oxidase, xanthine oxidase), information regarding the involvement of aldo-keto reductases in the reduction of nitro-containing drugs is limited.In this study, we screened six nitro-containing drugs (flunitrazepam, clonazepam, nimesulide, nilutamide, flutamide, and chloramphenicol) as substrates against recombinant human AKR1C1, 1C2, 1C3, and 1C4. In addition, flunitrazepam was also identified as an inhibitor of AKR1C2.In conclusion, AKR1C3 can reduce flunitrazepam to reactive nitroso-intemediates that could enhance drug toxicity. Our findings also suggested that AKRs can modulate GABAA receptor activity either by metabolizing benzodiazepines via AKR1C3 or by synthesizing the neuroactive steroid allopregnanolone via AKR1C2."

Addiction (Opioid and Alcohol) • AKR1C1 • AKR1C2 • NQO1

Short-term Androgen Deprivation Therapy and High-dose Radiotherapy in Intermediate- and High-risk Localized Prostate Cancer: Results from the GETUG 14 Randomized Phase 3 Trial. (PubMed, Eur Urol) - "STADT is a well-tolerated and effective strategy that can enhance oncological outcomes when combined with high-dose RT, particularly for patients with intermediate- or high-risk prostate cancer."

Journal • P3 data • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Metabolic activation of flunitrazepam via nitroreduction mediated by aldo-keto reductase 1C3. (PubMed, Drug Metab Dispos) - "We screened 6 nitro-containing drugs (flunitrazepam, clonazepam, nimesulide, nilutamide, flutamide, and chloramphenicol) as substrates against recombinant human AKR1C1, AKR1C2, AKR1C3, and AKR1C4, using discontinuous enzymatic assays. We conclude that both AKR1C3 and AKR1C2 may have an important role in flunitrazepam drug response. SIGNIFICANCE STATEMENT: Aldo-keto reductase (AKR)1C3 reduces flunitrazepam to 7-amino-flunitrazepam through the formation of reactive nitroso and hydroxylamino intermediates, and by inhibiting AKR1C2, flunitrazepam may reduce the formation of the neuroactive steroid allopregnanolone."

Journal • Addiction (Opioid and Alcohol) • Hepatocellular Cancer • Liver Cancer • Solid Tumor • AKR1C1 • AKR1C2

Ultra-sensitive electrochemical sensor based on MOF-derived Ni@carbon nanoframework and MWCNTs for the detection of flutamide in environmental water samples. (PubMed, Mikrochim Acta) - "Furthermore, the detection results were validated using ultraviolet-visible spectroscopy (UV-Vis), indicating its applicability for detecting FLT in real environmental water samples. This work presents a novel approach to developing a sensitive, eco-friendly, and cost-effective FLT detection technique, demonstrating the effectiveness of electrochemical sensors."

Journal