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DRUG CLASS:

Androgen receptor inhibitor

2d
New P1 trial
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Xtandi (enzalutamide) • bicalutamide • apalutamide
4d
Enrollment closed • Real-world evidence
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docetaxel • Nubeqa (darolutamide)
4d
A Trial of SHR3680 in Prostate Cancer Patients Who Are Candidates for Radical Prostatectomy (clinicaltrials.gov)
P3, N=391, Terminated, Jiangsu HengRui Medicine Co., Ltd. | N=1256 --> 391 | Recruiting --> Terminated; Due to the adjustment of the sponsor's development plan, after discussion with leading PI, sponsor has decided to terminate this study.
Enrollment change • Trial termination
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goserelin acetate • AiRuiEn (rezvilutamide)
5d
A Phase II Study of Advanced Salivary Gland Carcinoma Based on Molecular Typing (clinicaltrials.gov)
P2, N=88, Active, not recruiting, Fudan University | Trial primary completion date: Dec 2025 --> Dec 2026
Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • AR (Androgen receptor)
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HER-2 overexpression • AR positive
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trastuzumab rezetecan (SHR-A1811) • leuprolide acetate for depot suspension • AiRuiEn (rezvilutamide) • tizetatug rezetecan (SHR-A1921)
6d
Cytoplasmic versus nuclear localization of androgen receptor splice variant 7 as a predictor of benefit from androgen receptor pathway inhibitors in metastatic castration-resistant prostate cancer (PROPHECY trial). (PubMed, Prostate Cancer Prostatic Dis)
This study clarifies the clinical relevance of cytoplasmic AR-V7 in circulating tumor cells from men with metastatic castration-resistant prostate cancer. While nuclear-localized AR-V7 predicts extremely poor response, PFS, and overall survival with AR pathway inhibitors, cytoplasmic AR-V7 expands the definition of AR-V7-positive status and identifies patients with equally poor PFS and intermediate response and overall survival outcomes. Assessing both nuclear and cytoplasmic AR-V7 fractions may thus improve risk stratification heterogeneity and could better guide poor-risk ARPI treatment decisions by avoiding ineffective ARPI treatment, helping personalize therapy, and improving outcomes in men with mCRPC.
Journal
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AR (Androgen receptor)
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AR splice variant 7
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CELLSEARCH®
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Xtandi (enzalutamide) • abiraterone acetate
6d
Trial completion date • Trial primary completion date • Real-world evidence
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docetaxel • Xtandi (enzalutamide) • abiraterone acetate • Nubeqa (darolutamide) • apalutamide
6d
Enrollment change • Trial initiation date
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Xtandi (enzalutamide) • abiraterone acetate • Pluvicto (lutetium Lu 177 vipivotide tetraxetan)
6d
Biobank of genetically defined murine prostate cancer tumoroids uncovers oncogenic pathways and drug vulnerabilities driven by PTEN-loss. (PubMed, Cell Rep Methods)
Notably, these compounds also inhibited the growth of several human PCa cell lines and displayed synergistic effects when combined with the standard-of-care antiandrogen enzalutamide. Together, our findings provide evidence that murine tumoroids are versatile preclinical models for studying PCa tumorigenesis and drug sensitivities to develop therapeutic options for PCa patients.
Preclinical • Journal
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TP53 (Tumor protein P53) • PTEN (Phosphatase and tensin homolog) • STAT3 (Signal Transducer And Activator Of Transcription 3) • PDPK1 (3-Phosphoinositide dependent protein kinase 1)
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TP53 mutation • PTEN deletion • PTEN mutation
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Xtandi (enzalutamide)
7d
Diminished expression of decorin drives enzalutamide resistance in CRPC by suppressing ACSL4-dependent lipid remodeling and ferroptosis. (PubMed, Int Immunopharmacol)
In conclusion, promoting DCN-mediated ferroptosis might be a potential strategy for enhancing the sensitivity of enzalutamide in PCa cells. This study delineates a novel mechanism by which DCN downregulation suppresses ferroptosis and drives enzalutamide resistance in CRPC.
Journal
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PRKCH (Protein Kinase C Eta) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4) • DCN (Decorin) • PRKCB (Protein Kinase C Beta)
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Xtandi (enzalutamide)
7d
Study of Drug 1 (Enzalutamide) Plus Drug 2 (Relacorilant) for Patients With Prostate Cancer (clinicaltrials.gov)
P1, N=42, Completed, University of Chicago | Active, not recruiting --> Completed
Trial completion
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Xtandi (enzalutamide) • Lifyorli (relacorilant)
10d
Improved Anticancer Properties of Silver Nanoparticles by Albumin Coating in Prostate Cancer Cell Lines: An In Vitro Study. (PubMed, Pharmaceutics)
AgNPs-Alb significantly inhibited PC3 cell migration compared to AgNPs (p < 0.001) and Bicalutamide (p < 0.0001)...Additionally, a significant increase in P53 and E-cadherin, alongside a decrease in VEGF-C expression in LnCAP cells, was observed (p < 0.05). This study suggests that AgNPs-Alb have stronger anticancer and cytotoxic effects compared to AgNPs alone against PCa cell lines and higher effects were observed on PC3 cells compared to LnCAP cells.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • CDH1 (Cadherin 1) • BAX (BCL2-associated X protein) • VEGFC (Vascular Endothelial Growth Factor C) • SNAI1 (Snail Family Transcriptional Repressor 1) • ANXA5 (Annexin A5)
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bicalutamide
11d
Quercetin Inhibits AKT Ser473 Phosphorylation and Disrupts AKT-Androgen Receptor Signaling in Castration-Resistant Prostate Cancer Cells. (PubMed, Antioxidants (Basel))
C4-2B and 22Rv1 CRPC cell lines were treated with increasing QRC concentrations, with or without enzalutamide (Enz)...Enz cotreatment with QRC did not produce additive effects, consistent with a model in which QRC acts upstream of ligand-driven AR activation and thereby limits the incremental benefit of AR antagonism under these conditions. These data support QRC as an AKT-AR axis modulator in CRPC and provide a target engagement framework beyond simple ROS scavenging.
Journal
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AR (Androgen receptor) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
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Xtandi (enzalutamide)