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DRUG CLASS:

Androgen receptor inhibitor

1d
Pembrolizumab in Treating Patients With Metastatic Castration Resistant Prostate Cancer Previously Treated With Enzalutamide (clinicaltrials.gov)
P2, N=58, Active, not recruiting, OHSU Knight Cancer Institute | Trial completion date: Jun 2025 --> Jun 2026
Trial completion date • IO biomarker
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PD-L1 (Programmed death ligand 1) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
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Keytruda (pembrolizumab) • Xtandi (enzalutamide)
1d
Androgen receptor blockade and its effect on PSMA-localization in prostate cancer: Implications for radioligand therapy. (PubMed, Biomed Pharmacother)
LNCaP and VCaP cells were treated with enzalutamide (0.1-10 µM) for 1-7 days...Crucially, ER stress markers correlated with PSMA trafficking, suggesting serum-based profiling could enable individualized ARB adjustments. Future studies should validate these biomarkers to establish personalized ARB-RLT strategies for improved clinical outcomes.
Journal
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AR (Androgen receptor)
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Xtandi (enzalutamide)
6d
Proteome-Based Plasma Biomarkers for Cognitive Dysfunction in an Androgen Deprivation Model. (PubMed, Mol Neurobiol)
Sixteen-week-old BALB/c mice received enzalutamide, a nonsteroidal antiandrogen, at 50 mg/kg/day via oral gavage 5 days a week for 8 weeks to simulate the ADT protocol...These results suggest that blood could be a valuable source of biomarkers for ADT-induced cognitive dysfunction. Further studies are needed to assess their clinical applicability in monitoring cognitive decline in prostate cancer patients on ADT and in neurotypical aging.
Journal
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ARL6IP1 (ADP Ribosylation Factor Like GTPase 6 Interacting Protein 1)
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Xtandi (enzalutamide)
8d
A novel disulfidptosis-related lncRNA signature to predict prognosis and immune response of cervical cancer. (PubMed, Medicine (Baltimore))
The low-risk group exhibited improved survival outcomes and increased sensitivity to immunotherapy, whereas the high-risk group showed heightened sensitivity to to bexarotene, bicalutamide, embelin, FH535, and pazopanib. Quantitative PCR results indicated that ILF3-DT and PPP1R14B-AS1 were downregulated in CC tissues, whereas RUSC1-AS1 was upregulated. In conclusion, we developed a novel prognostic risk signature based on 9 disulfidptosis-related lncRNAs, which may serve as an independent predictor of immunotherapy response and chemotherapy sensitivity in CC.
Journal • IO biomarker
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RUSC1-AS1 (RUSC1 Antisense RNA 1)
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pazopanib • bicalutamide • Targretin oral (bexarotene oral)
8d
NSD2 targeting reverses plasticity and drug resistance in prostate cancer. (PubMed, Nature)
Pharmacological inhibition of NSD2 with a first-in-class small molecule reverses plasticity and synergizes with enzalutamide to suppress growth and promote cell death in human patient-derived organoids of multiple CRPC subtypes in culture and in xenografts. Co-targeting of NSD2 and AR may represent a new therapeutic strategy for lethal forms of CRPC that are currently recalcitrant to treatment.
Journal
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NSD2 (Nuclear Receptor Binding SET Domain Protein 2)
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Xtandi (enzalutamide)
9d
Enrollment open
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Xtandi (enzalutamide) • abiraterone acetate • Pluvicto (lutetium Lu 177 vipivotide tetraxetan)
9d
A Phase II Study of Advanced Salivary Gland Carcinoma Based on Molecular Typing (clinicaltrials.gov)
P2, N=88, Active, not recruiting, Fudan University | Recruiting --> Active, not recruiting
Enrollment closed
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HER-2 (Human epidermal growth factor receptor 2) • AR (Androgen receptor)
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HER-2 positive • HER-2 amplification • HER-2 mutation • AR positive
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trastuzumab rezetecan (SHR-A1811) • leuprolide acetate for depot suspension • AiRuiEn (rezvilutamide) • tizetatug rezetecan (SHR-A1921)
10d
Population Pharmacokinetics Analysis of Talazoparib and Enzalutamide Combination Therapy for Patients With Metastatic Castration-Resistant Prostate Cancer. (PubMed, J Clin Pharmacol)
The single covariate effect of baseline creatinine clearance on CLt0/Ft showed that relative to the reference value for normal renal function, CLt0/Ft decreased by 8% for mild, 27% for moderate, and 46.7% for severe renal impairment. Simulations showed that a dose reduction of enzalutamide does not require talazoparib dose modification since the magnitude of exposure reduction for talazoparib was not considered clinically significant.
PK/PD data • Journal • PARP Biomarker
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HRD (Homologous Recombination Deficiency)
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Talzenna (talazoparib) • Xtandi (enzalutamide)
10d
Enrollment open • HEOR
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Xtandi (enzalutamide) • abiraterone acetate • Nubeqa (darolutamide) • apalutamide
11d
A memory-driven reinforcement learning model of phenotypic adaptation for anticipating therapeutic resistance in prostate cancer. (PubMed, bioRxiv)
When applied to prostate cancer, this memory-driven adaptive model successfully captures the experimentally-observed dynamics of drugsensitive and drug-resistant LNCaP cells under varying dosing schedules of androgen receptor blockade with enzalutamide (enza), significantly outperforming traditional transition models that lack history dependence...Our model accurately predicts the PSA dynamics under repeated treatment cycles and effectively distinguishing between patients who respond and those who do not respond to treatment, thereby providing quantitative insight into prostate cancer progression. We anticipate that such adaptive modeling frameworks will be broadly useful for predicting cancer treatment outcomes and developing optimized adaptive therapeutic strategies tailored to patient-specific disease dynamics in additional cancer contexts.
Journal
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AR (Androgen receptor)
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Xtandi (enzalutamide)
13d
New P3 trial
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AiRuiEn (rezvilutamide)
14d
Study of TVB-2640 in Men With Metastatic Castration-Resistant Prostate Cancer (clinicaltrials.gov)
P1, N=30, Recruiting, Weill Medical College of Cornell University | Trial completion date: Nov 2026 --> Jan 2029 | Trial primary completion date: Nov 2025 --> Jan 2027
Trial completion date • Trial primary completion date
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Xtandi (enzalutamide) • denifanstat (TVB-2640)