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DRUG:

flutamide

i
Other names: Sch-13521, NK-601
Company:
Generic mfg.
Drug class:
Androgen receptor inhibitor
2ms
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
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AR (Androgen receptor)
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flutamide
2ms
Assessing Induction of Double Strand Breaks With Androgen Receptor Partial Agonist in Patients on Androgen Suppression (clinicaltrials.gov)
P1, N=25, Completed, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Active, not recruiting --> Completed
Trial completion
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flutamide
2ms
RTOG 0815: Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer (clinicaltrials.gov)
P3, N=1538, Completed, Radiation Therapy Oncology Group | Active, not recruiting --> Completed
Trial completion
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bicalutamide • triptorelin • goserelin acetate • flutamide • Firmagon (degarelix) • leuprolide acetate for depot suspension • Suprefact (buserelin acetate)
2ms
Hormone Therapy, Radiation Therapy, and Steroid 17alpha-monooxygenase TAK-700 in Treating Patients With High-Risk Prostate Cancer (clinicaltrials.gov)
P3, N=239, Completed, Radiation Therapy Oncology Group | Active, not recruiting --> Completed | Trial completion date: Jun 2029 --> Sep 2025
Trial completion • Trial completion date
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bicalutamide • triptorelin • goserelin acetate • flutamide • leuprolide acetate for depot suspension • orteronel (TAK 700) • Suprefact (buserelin acetate)
2ms
ARCH: Contributions to Hypertension With Androgen Deprivation Therapy (clinicaltrials.gov)
P4, N=10, Completed, University of Colorado, Denver | Recruiting --> Completed | N=228 --> 10 | Trial completion date: Mar 2028 --> Jul 2025 | Trial primary completion date: Mar 2028 --> Jul 2025
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
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Xtandi (enzalutamide) • bicalutamide • goserelin acetate • flutamide • leuprolide acetate for depot suspension
3ms
Enrollment closed
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CD4 (CD4 Molecule)
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bicalutamide • apalutamide • triptorelin • goserelin acetate • flutamide • Firmagon (degarelix) • Orgovyx (relugolix) • leuprolide acetate for depot suspension • Suprefact (buserelin acetate)
3ms
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
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AKR1C1 (Aldo-Keto Reductase Family 1 Member C1) • AKR1C2 (Aldo-Keto Reductase Family 1 Member C2)
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flutamide • nilutamide
4ms
VA STARPORT: Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-directed Local Therapy for Oligometastatic pRosTate Cancer (clinicaltrials.gov)
P2/3, N=464, Recruiting, VA Office of Research and Development | Trial completion date: Dec 2025 --> Mar 2029 | Trial primary completion date: Jul 2025 --> Mar 2026
Trial completion date • Trial primary completion date
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docetaxel • Xtandi (enzalutamide) • abiraterone acetate • prednisone • bicalutamide • apalutamide • triptorelin • goserelin acetate • flutamide • nilutamide • Firmagon (degarelix) • Orgovyx (relugolix) • leuprolide acetate for depot suspension
5ms
WTAP-mediated m6A modification promotes drug sensitivity by regulating NR3C1 in prostate cancer. (PubMed, Sci China Life Sci)
Our study uncovered a novel molecular mechanism by which the m6A-induced WTAP/YTHDF2/NR3C1 axis promotes CRPC flutamide drug sensitivity. This finding suggests the potential of WTAP as a promising prognostic marker and therapeutic target against flutamide drug sensitivity in CRPC.
Journal
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WT1 (WT1 Transcription Factor) • PKM (Pyruvate Kinase M1/2) • WTAP (WT1 Associated Protein) • YTHDF2 (YTH N6-Methyladenosine RNA Binding Protein 2)
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flutamide
6ms
Three Drug Combination Therapy Versus Conventional Treatment of Children With Congenital Adrenal Hyperplasia (clinicaltrials.gov)
P3, N=66, Completed, Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) | Phase classification: P4 --> P3
Phase classification
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letrozole • flutamide
7ms
Therapeutic Efficacy of Melatonin and Flutamide Combination in Safety for Prostate Cancer: An In Vitro Study. (PubMed, DNA Cell Biol)
The combination of melatonin and flutamide significantly upregulated the expression of BAX/BCL2 ratio in all three cell lines (p < 0.0001) and downregulated the expression of KLK3 (p < 0.01), HIF1α (p < 0.01), VEGFC (p < 0.001), and epithelial-mesenchymal transition pathway genes in PC3 and LNCaP (p < 0.01). Melatonin in combination with flutamide reduced its dose and increased the sensitivity of prostate cancer cells to treatment.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • CDH1 (Cadherin 1) • BAX (BCL2-associated X protein) • VEGFC (Vascular Endothelial Growth Factor C) • SNAI2 (Snail Family Transcriptional Repressor 2) • KLK3 (Kallikrein-related peptidase 3)
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flutamide
7ms
Reducing the effective dosage of flutamide on prostate cancer cell lines through combination with selenium nanoparticles: An in-vitro study. (PubMed, PLoS One)
It is suggested that simultaneous administration of SeNPs and flutamide could potentially reduce the effective dosage of flutamide and decrease its adverse effects.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • CDH1 (Cadherin 1) • BAX (BCL2-associated X protein) • VEGFC (Vascular Endothelial Growth Factor C) • SNAI1 (Snail Family Transcriptional Repressor 1) • ANXA5 (Annexin A5) • KLK3 (Kallikrein-related peptidase 3)
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flutamide