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DRUG CLASS:

CYP17A1 inhibitor

2d
Randomized Phase II Study of ADT + Abiraterone vs ADT + Docetaxel + Abiraterone (clinicaltrials.gov)
P2, N=150, Active, not recruiting, Northwestern University | Recruiting --> Active, not recruiting | Trial primary completion date: Dec 2028 --> May 2024
Enrollment closed • Trial primary completion date • Metastases
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docetaxel • abiraterone acetate • dexamethasone injection
4d
Prognostic and Predictive Role of SPOP Mutations in Prostate Cancer: A Systematic Review and Meta-analysis. (PubMed, Eur Urol Oncol)
Patients with SPOPmut PC seem to exhibit superior oncological outcomes compared with patients with SPOPwt. Tailored risk stratification and treatment approaches should be explored in such patients.
Retrospective data • Review • Journal
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SPOP (Speckle Type BTB/POZ Protein)
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SPOP mutation
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docetaxel • abiraterone acetate
14d
ACTIon: Abiraterone Acetate in Combination With Tildrakizumab (clinicaltrials.gov)
P1/2, N=13, Terminated, Institute of Cancer Research, United Kingdom | Trial completion date: Oct 2024 --> Nov 2023 | Active, not recruiting --> Terminated; Funder decided that response outcomes to date did not support continuation of the study.
Trial completion date • Trial termination • Combination therapy • Metastases
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IL23A (Interleukin 23 Subunit Alpha)
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Ilumya (tildrakizumab-asmn) • Yonsa (abiraterone acetate)
15d
Enrollment open
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abiraterone acetate • Yonsa (abiraterone acetate)
22d
Predicting abiraterone efficacy in advanced prostate cancer: Insights from marker of proliferation Ki67. (PubMed, Prostate)
This study highlights KI67 positivity in prostate biopsy as a strong predictor of abiraterone efficacy in advanced PCa. These insights will assist clinicians in anticipating clinical outcomes and refining treatment decisions for PCa patients.
Journal • Metastases
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MKI67 (Marker of proliferation Ki-67)
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abiraterone acetate
22d
New P2 trial
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abiraterone acetate • Yonsa (abiraterone acetate)
23d
PET/CT Characterization of Treatment Resistance (clinicaltrials.gov)
P=N/A, N=20, Recruiting, University of Wisconsin, Madison | Trial completion date: Sep 2024 --> Mar 2027 | Trial primary completion date: Sep 2024 --> Mar 2025
Trial completion date • Trial primary completion date
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abiraterone acetate
27d
Stereotactic Ablative Radiation Therapy for Abiraterone-Resistant, Oligoprogressive Metastatic Prostate Cancer (clinicaltrials.gov)
P=N/A, N=30, Recruiting, Sunnybrook Health Sciences Centre | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2023 --> Dec 2025
Trial completion date • Trial primary completion date • Metastases
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abiraterone acetate
30d
Current Systemic Therapy in Men with Metastatic Castration-Sensitive Prostate Cancer. (PubMed, Curr Oncol Rep)
In less than a decade, evidence was chronologically provided that (1) systemic treatment intensification with docetaxel improves outcomes, including survival, in men with mCSPC, (2) then that these outcomes are also improved when a second-generation androgen receptor pathway inhibitor (ARPI) is combined with androgen deprivation therapy (ADT), and (3) using a "triplet systemic therapy," which consists in the combination of ADT, an ARPI and docetaxel, further improves outcomes, including survival...Combining prostate radiotherapy and intensified systemic treatment including abiraterone may be synergistic as suggested in the PEACE-1 trial...Importantly, most evidence currently available was obtained in men with de novo metastases, while for those with metastatic relapse after definitive local treatment, the role of treatment intensification is less well established. Treatment intensification is nowadays the standard of care for patients with de novo mCSPC as it leads to outcomes improvement, including survival, and the standard of care is evolving almost on a yearly basis.
Review • Journal • BRCA Biomarker • Metastases
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BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • FOLH1 (Folate hydrolase 1)
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FOLH1 expression
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docetaxel • abiraterone acetate
1m
Cytoreductive Prostatectomy Combined With Triple or Dual Systemic Therapy in mHSPC Patients (clinicaltrials.gov)
P3, N=200, Recruiting, The First Affiliated Hospital with Nanjing Medical University
New P3 trial • Metastases
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docetaxel • abiraterone acetate
1m
Real-World Overall Survival and Treatment Patterns by PTEN Status in Metastatic Castration-Resistant Prostate Cancer. (PubMed, JCO Precis Oncol)
PTEN LOF, identified with genomic testing, was associated with decreased survival and negative prognoses in patients with mCRPC.
Journal • Real-world evidence • Real-world • Metastases
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PTEN (Phosphatase and tensin homolog)
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Xtandi (enzalutamide capsule) • abiraterone acetate
2ms
Ductal, intraductal, and cribriform carcinoma of the prostate: Molecular characteristics and clinical management. (PubMed, Urol Oncol)
Evidence suggests abiraterone may be superior to docetaxel as a first-line treatment for patients with IDC-P. To address these and other critical pathological attributes, this review examines the molecular pathology, genetics, treatments, and oncologic outcomes associated with CC-P, PDA, and IDC-P with the objective of creating a comprehensive resource with a centralized repository of information on PDA, IDC-P, and CC-P.
Review • Journal • BRCA Biomarker
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TP53 (Tumor protein P53) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • HRD (Homologous Recombination Deficiency) • RB1 (RB Transcriptional Corepressor 1) • PALB2 (Partner and localizer of BRCA2) • CHEK2 (Checkpoint kinase 2) • CHD1 (Chromodomain Helicase DNA Binding Protein 1) • MAP3K7 (Mitogen-Activated Protein Kinase Kinase Kinase 7) • NKX3-1 (NK3 homeobox 1)
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TP53 mutation • PTEN mutation • PALB2 mutation • CHEK2 mutation
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docetaxel • abiraterone acetate
2ms
DHODH inhibition represents a therapeutic strategy and improves abiraterone treatment in castration-resistant prostate cancer. (PubMed, Oncogene)
However, the combination treatment with BAY2402234 and abiraterone decreased intratumoral testosterone levels and induced apoptosis, which inhibited the growth of CWR22Rv1 xenograft tumors and patient-derived xenograft organoids. Taken together, these results establish DHODH as a key player in CRPC and as a potential therapeutic target for advanced prostate cancer.
Journal
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DHODH (Dihydroorotate Dehydrogenase (Quinone))
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abiraterone acetate • orludodstat (BAY2402234)
2ms
Androgen Reduction in Congenital Adrenal Hyperplasia, Phase 1 (clinicaltrials.gov)
P1, N=36, Suspended, University of Texas Southwestern Medical Center | Recruiting --> Suspended
Trial suspension
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abiraterone acetate
2ms
Enrollment closed • Metastases
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Xtandi (enzalutamide capsule) • abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
2ms
Study of Abiraterone Acetate Without Exogenous Glucocorticoids in Men With Castration-resistant Prostate Cancer (clinicaltrials.gov)
P2, N=60, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Jan 2024 --> Apr 2024
Trial completion date
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abiraterone acetate
2ms
NCI-2018-01054: Apalutamide, Abiraterone Acetate, and Prednisone in Treating Participants With Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
P2, N=7, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Apr 2024 --> Apr 2025 | Trial primary completion date: Apr 2024 --> Apr 2025
Trial completion date • Trial primary completion date • Metastases
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PTEN (Phosphatase and tensin homolog)
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AR overexpression • AR expression • AR-V7 expression
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abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
2ms
CASCARA: Castration Sensitive Carboplatin, Cabazitaxel and Abiraterone (clinicaltrials.gov)
P2, N=22, Active, not recruiting, Masonic Cancer Center, University of Minnesota | Recruiting --> Active, not recruiting | N=61 --> 22 | Trial primary completion date: May 2025 --> Jun 2023
Enrollment closed • Enrollment change • Trial primary completion date • Metastases
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carboplatin • abiraterone acetate • cabazitaxel
2ms
Advanced ChemoHormonal Therapy for Treatment Naive Metastatic Prostate Cancer (clinicaltrials.gov)
P2, N=7, Active, not recruiting, OHSU Knight Cancer Institute | Trial completion date: Jan 2026 --> Jan 2030 | Trial primary completion date: Jan 2024 --> Jan 2028
Trial completion date • Trial primary completion date • Metastases
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docetaxel • abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
3ms
A Study on the Safety and Efficacy of LAE001 in the Treatment of Metastatic Prostate Cancer (clinicaltrials.gov)
P1/2, N=33, Suspended, Laekna Limited | N=80 --> 33 | Trial completion date: Aug 2022 --> Jun 2025 | Unknown status --> Suspended | Trial primary completion date: Feb 2022 --> Oct 2023
Enrollment change • Trial completion date • Trial suspension • Trial primary completion date
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LAE001
3ms
Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer. (PubMed, Eur J Med Chem)
Co-treatment with scalar dilutions of either compound 6 or 6e and the clinically used drug abiraterone led to a significant reduction in cell proliferation, and thus confirmed that treatment with both CYP171A1-and AKR1C3-targeting compounds possess the potential to intervene in key steps in the steroidogenic pathway. Taken together, the novel compounds display desirable biochemical potency and cellular target inhibition as well as good in-vitro ADME properties, which highlight their potential for further preclinical studies.
Journal
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CYP17A1 (Cytochrome P450 Family 17 Subfamily A Member 1) • AKR1C2 (Aldo-Keto Reductase Family 1 Member C2)
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abiraterone acetate
3ms
Androgen deprivation induces double-null prostate cancer via aberrant nuclear export and ribosomal biogenesis through HGF and Wnt activation. (PubMed, Nat Commun)
Specifically, the AR- and neuroendocrine-null PCa, DNPC, occurs in abiraterone and enzalutamide-treated patients. Elevated expression of XPO1 and ribosomal proteins is also identified in clinical DNPC specimens. Inhibition of XPO1 and ribosomal pathways represses DNPC growth in both in vivo and ex vivo conditions, evidencing future therapeutic targets.
Journal • IO biomarker
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XPO1 (Exportin 1)
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Xtandi (enzalutamide capsule) • abiraterone acetate
3ms
Enrollment open
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Xtandi (enzalutamide capsule) • abiraterone acetate • Yonsa (abiraterone acetate)
3ms
Copy Number Gain in Androgen Receptors Predicts the Poor Prognosis in Japanese Castration-resistant Prostate Cancer. (PubMed, Anticancer Res)
AR-amp was associated with high nadir PSA and low iPSA/PSA ratio. AR-amp was significantly associated with poor prognosis in Japanese patients with CRPC.
Journal
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AR (Androgen receptor)
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AR amplification
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docetaxel • Xtandi (enzalutamide capsule) • abiraterone acetate
3ms
Trial completion
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abiraterone acetate
3ms
Dual inhibition of CYP17A1 and HDAC6 by abiraterone-installed hydroxamic acid overcomes temozolomide resistance in glioblastoma through inducing DNA damage and oxidative stress. (PubMed, Cancer Lett)
In vivo studies revealed that compound 12 effectively suppressed tumor growth in xenograft and orthotopic mouse models without inducing significant adverse effects. These findings highlight the potential of dual CYP17A1 and HDAC6 inhibition as a promising strategy for overcoming treatment resistance in GBM and offer new hope for improved therapeutic outcomes.
Journal
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HDAC6 (Histone Deacetylase 6)
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CYP17A1 expression • HDAC6 expression
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temozolomide • abiraterone acetate
3ms
Co-expression of Twist and Snai1: predictor of poor prognosis and biomarker of treatment resistance in untreated prostate cancer. (PubMed, Mol Biol Rep)
These results suggest that Snai1 and Twist are overexpressed during the onset and progression of PCa malignancies and may be theranostic markers of resistance to ADT, abiraterone, or enzalutamide therapy.
Journal
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SNAI1 (Snail Family Transcriptional Repressor 1)
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SNAI1 expression
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Xtandi (enzalutamide capsule) • abiraterone acetate
3ms
Decreasing Dosing Regimens of Abiraterone 500 mg in Men With Prostate Cancer to Find Lowest Recommended Dose. (clinicaltrials.gov)
P1, N=50, Active, not recruiting, University of Chicago | Recruiting --> Active, not recruiting
Enrollment closed
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abiraterone acetate • Yonsa (abiraterone acetate)
4ms
Adaptive Abiraterone Therapy for Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
P1, N=19, Active, not recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial completion date: Dec 2023 --> Dec 2024
Trial completion date • Metastases
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abiraterone acetate
4ms
The impact of circulating tumor cell HOXB13 RNA detection in men with metastatic castration-resistant prostate cancer treated with abiraterone or enzalutamide. (PubMed)
P=N/A; Higher CTC HOXB13 expression is associated with AR-dependent biomarkers in CTCs and is adversely prognostic in the context of potent AR inhibition in men with mCRPC.
Journal • Circulating tumor cells • Tumor cell • Metastases
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CELLSEARCH®
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Xtandi (enzalutamide capsule) • abiraterone acetate
4ms
New trial • Metastases
|
abiraterone acetate
4ms
New P1 trial • Metastases
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abiraterone acetate
4ms
Talazoparib With Androgen Deprivation Therapy and Abiraterone for the Treatment of Castration Sensitive Prostate Cancer (clinicaltrials.gov)
P2, N=70, Recruiting, City of Hope Medical Center | Trial completion date: Dec 2023 --> Aug 2027 | Trial primary completion date: Dec 2023 --> Aug 2027
Trial completion date • Trial primary completion date
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Talzenna (talazoparib) • abiraterone acetate • Eligard (leuprolide acetate) • bicalutamide • goserelin acetate • Firmagon (degarelix) • Viadur (leuprorelin implant) • Yonsa (abiraterone acetate)
4ms
PET/CT Characterization of Treatment Resistance (clinicaltrials.gov)
P=N/A, N=20, Recruiting, University of Wisconsin, Madison
Trial completion date • Trial primary completion date
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abiraterone acetate
4ms
Bench to Bedside Development of [F]Fluoromethyl-(1,2-H)choline ([F]D4-FCH). (PubMed, Molecules)
Treatment with abiraterone or enzalutamide in metastatic castrate-resistant prostate cancer patients elicited mixed responses on PET at 12-16 weeks despite predominantly stable radiological appearances. The sum of the weighted tumour-to-background ratios (TBRs-wsum) was associated with the duration of survival.
Review • Journal
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CHKA (Choline Kinase Alpha)
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Xtandi (enzalutamide capsule) • abiraterone acetate
4ms
Poly (ADP-ribose) Polymerase Inhibitors in Patients with Metastatic Castration-Resistant Prostate Cancer: A Meta-Analysis of Randomized Controlled Trials. (PubMed, Medicina (Kaunas))
Context: Several recent randomized controlled trials (RCTs) have reported on the survival benefits of poly (ADP-ribose) polymerase inhibitors (PARPi) compared to standard-of-care (SOC) treatment (enzalutamide, abiraterone, or docetaxel) in patients with metastatic castration-resistant prostate cancer (mCRPC). PARP inhibitors demonstrate greater effectiveness than SOC treatments in HRR/BRCA-positive patients with mCRPC. Further research is required to explore ways to reduce adverse event rates and investigate the efficacy of HRR/BRCA-negative patients.
Retrospective data • Review • Journal • BRCA Biomarker • PARP Biomarker • Metastases
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BRCA (Breast cancer early onset)
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BRCA mutation
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docetaxel • Xtandi (enzalutamide capsule) • abiraterone acetate
5ms
Enrollment open
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Xtandi (enzalutamide capsule) • abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
5ms
Prostate cancer androgen biosynthesis relies solely on CYP17A1 downstream metabolites. (PubMed, J Steroid Biochem Mol Biol)
Precursor steroids upstream of DHEA were converted down the first steps of the alternative DHT biosynthesis pathway, but did not proceed through to active androgen generation. Comprehensive steroid flux analysis of (CR)PC cells provides strong evidence against intratumoral de novo androgen biosynthesis and demonstrates that androgen precursor steroids downstream of CYP17A1 activities constitute the major source of intracrine androgen generation.
Journal
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AR (Androgen receptor) • CYP17A1 (Cytochrome P450 Family 17 Subfamily A Member 1)
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CYP17A1 expression
5ms
S1014 Abiraterone Acetate in Treating Patients With Prostate Cancer Who Have Undergone Initial Hormone Therapy (clinicaltrials.gov)
P2, N=41, Active, not recruiting, SWOG Cancer Research Network | Trial completion date: Oct 2023 --> Oct 2024
Trial completion date
|
abiraterone acetate
5ms
Enrollment closed
|
Xtandi (enzalutamide capsule) • abiraterone acetate • Yonsa (abiraterone acetate)
5ms
Enrollment closed
|
Xtandi (enzalutamide capsule) • abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
5ms
Identifying patient profiles and mapping treatment journeys of ARPI-treated, taxane-naive patients with metastatic prostate cancer across three countries in a digital patient survey. (ASCO-GU 2024)
We identified responses from patients with mPCa who were taxane-naive and received at least one androgen receptor pathway inhibitor (ARPI), such as abiraterone or enzalutamide. In different countries, taxane-naive patients who received one ARPI have different characteristics at diagnosis and distinct patterns of care. It is important to understand how these differences may affect diagnostic and therapeutic trends to maximally improve patient care in this treatment setting.
Clinical • Metastases
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Xtandi (enzalutamide capsule) • abiraterone acetate