New insights in the paradigm of upregulation of tumoral PSMA expression by androgen receptor blockade: Enzalutamide induces PSMA upregulation in castration-resistant prostate cancer even in patients having previously progressed on enzalutamide

ConclusionsOur results suggest that enzalutamide could be considered as a PSMA radioligand treatment enhancing primer medication, which may increase PSMA expression by a dimension of 50% in mCRPC. The effect was shown even in patients having previously failed enzalutamide treatment for arrest of progression in the mCRPC setting. Our observation deserves evaluation in a prospective setting.
Source: European Journal of Nuclear Medicine and Molecular Imaging - Category: Nuclear Medicine Source Type: research

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Enzalutamide (Enz) has shown limited bioavailability via oral administration. Castration-resistant prostate cancer (CRPC) is frequent among patients receiving 18 –24 months of androgen deprivation therapy. The ...
Source: Journal of Nanobiotechnology - Category: Nanotechnology Authors: Tags: Research Source Type: research
This study aimed to evaluate the drug-like properties of ailanthone, a novel Chinese medicine monomer that was shown to have activity against castration-resistant prostate cancer tumour growth and metastasis in our previous study. The drug-like properties detected in the present study included effects on permeability, liver microsome stability, plasma protein binding rate, plasma stability, and human ether-à-go-go-related gene inhibition. Additionally, the following results were obtained: the efflux ratio of ailanthone was> 32 during permeability detection; the half-life and intrinsic clearance (Clint) in ...
Source: Planta Medica - Category: Drugs & Pharmacology Authors: Tags: Original Papers Source Type: research
ConclusionBased on the vesicular cargo, the molecular constituents, the exosomes have the potential to change the fate of macrophage phenotypes, either M1, classically activated macrophages, or M2, alternatively activated macrophages. In this review, we discuss and describe the ability of tumor-derived exosomes in the mechanism of macrophage activation and polarization.
Source: Inflammation Research - Category: Research Source Type: research
Authors: Shabataev V, Saadat SH, Elterman DS Abstract The two major long-term concerns associated with different options for the management of prostate cancer, (including surgery, radiotherapy, brachytherapy, cryotherapy, HIFU, etc.) include difficulties with lower urinary tract symptoms (LUTS) and/or erectile dysfunction. LUTS can be in the form of stress urinary incontinence (SUI), urge urinary incontinence (UUI), frequency/urgency, and/or voiding difficulties. While surgery is mostly associated with SUI and radiation mostly results in UUI, there can be an overlap. Incontinence rates after cryotherapy and high in...
Source: Canadian Journal of Urology - Category: Urology & Nephrology Tags: Can J Urol Source Type: research
AbstractApalutamide (ERLEADA®), a next-generation androgen receptor (AR) inhibitor, is approved in several countries, including those of the EU and in the USA, for the treatment of non-metastatic castration-resistant prostate cancer (nmCRPC). In the pivotal SPARTAN study in men with nmCRPC who were at high risk of developing metastases despite androgen-deprivation therapy (+  ADT), oral apalutamide (+ ADT) significantly prolonged metastasis-free survival (MFS) compared with placebo (+ ADT) at a median follow-up of 20.3 months, with consistent benefits demonstrated across prespecified subgroups...
Source: Drugs and Therapy Perspectives - Category: Drugs & Pharmacology Source Type: research
RARITAN, N.J., February 3, 2020 – The Janssen Pharmaceutical Companies of Johnson &Johnson announced today multiple data presentations from a robust solid tumor portfolio that will be featured at the American Society of Clinical Oncology Genitourinary (ASCO GU) Cancers Symposium, taking place February 13-15 in San Francisco. Company-sponsored data presentations will include clinical results for ERLEADA® (apalutamide) and niraparib in prostate cancer; and BALVERSA™ (erdafitinib) in bladder cancer. “We are committed to improving outcomes in patients with prostate and bladder cancer where high unmet ...
Source: Johnson and Johnson - Category: Pharmaceuticals Tags: Innovation Source Type: news
This study showed that both drugs significantly improved lumbar spine and total hip bone mineral density in Asian men with prostate cancer who received ADT.IntroductionTo evaluate whether monthly oral minodronate or semiannual subcutaneous injection of denosumab improves bone mineral density (BMD) in Asian men with prostate cancer (PCa) receiving ADT.MethodsA multicenter, open-label, randomized, controlled study including patients with hormone-sensitive PCa without bone metastasis receiving ADT was performed. Patients were randomized (1:1:1) to minodronate, denosumab, or no agent control groups. The primary end point was t...
Source: Osteoporosis International - Category: Orthopaedics Source Type: research
Guanylate-binding protein 1 (GBP1) is a large GTPase of the dynamin superfamily involved in the regulation of membrane, cytoskeleton, and cell cycle progression dynamics. In many cell types, such as endothelial cells and monocytes, GBP1 expression is strongly provoked by interferon γ (IFNγ) and acts to restrain cellular proliferation in inflammatory contexts. In immunity, GBP1 activity is crucial for the maturation of autophagosomes infected by intracellular pathogens and the cellular response to pathogen-associated molecular patterns. In chronic inflammation, GBP1 activity inhibits endothelial cell proliferati...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Hayley B. Schultz, Tahlia R. Meola, Nicky Thomas, Clive A. PrestidgeAbstractAbiraterone acetate, marketed as Zytiga®, is an antiandrogen medication used in the treatment of prostate cancer. Abiraterone acetate is a BCS Class IV compound associated with several oral delivery challenges. Its low solubility and high lipophilicity lead to poor oral bioavailability (
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research
Selenium deficiency is associated with many physiological disorders including the high risk of cancer. The rehabilitation of selenium with different selenium supplements, however, fails due to their low therapeutic index. Therefore, it is advantageous to have a less toxic form of selenium for supplementation with potentially high anticancer activity. Here we show Bacillus licheniformis derived biogenic selenium nanoparticles at a minimal concentration of 2 μg Se/ml induce necroptosis in LNCaP-FGC cells, without affecting the RBC integrity. Real-time gene expression analysis indicated the overexpression of tumor necrotic...
Source: Frontiers in Oncology - Category: Cancer & Oncology Source Type: research
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