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https://www.readbyqxmd.com/read/28432800/effect-of-n-methyl-deuteration-on-pharmacokinetics-and-pharmacodynamics-of-enzalutamide
#1
Xuehai Pang, Lingling Peng, Yuanwei Chen
Enzalutamide, a 2nd generation antiandrogen, has been developed for the treatment of CRPC. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger anti-tumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.
April 22, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28430389/combination-of-carmustine-and-selenite-inhibits-egfr-mediated-growth-signaling-in-androgen-independent-prostate-cancer-cells
#2
Vijayalakshmi Thamilselvan, Mani Menon, Gary S Stein, Fred Valeriote, Sivagnanam Thamilselvan
Although aberrant androgen receptor (AR) signaling is a central mechanism for castration resistant prostate cancer (CRPC) progression, AR-independent survival and growth signaling is also present in CRPC. The current therapeutic options for patients with CRPC are limited and new drugs are desperately needed to eliminate these crucial growth signaling pathways. Overexpression of EGFR in CRPC primarily mediates the proliferation of androgen-independent prostate cancer (AIPC) cells. We have previously shown that combination of carmustine and selenite effectively induces apoptosis and growth inhibition by targeting AR and AR-variants in castration resistant prostate cancer cells...
April 21, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28429372/long-term-clinical-impact-of-psa-surge-in-castration-resistant-prostate-cancer-patients-treated-with-abiraterone
#3
Vincenza Conteduca, Orazio Caffo, Cristian Lolli, Michele Aieta, Emanuela Scarpi, Emanuela Bianchi, Francesca Maines, Giuseppe Schepisi, Samanta Salvi, Francesco Massari, Francesco Carrozza, Antonello Veccia, Vincenzo E Chiuri, Enrico Campadelli, Gaetano Facchini, Ugo De Giorgi
BACKGROUND: Early changes in PSA have been evaluated in association to treatment outcome. The aim of this study was to assess PSA surge phenomenon in castration-resistant prostate cancer (CRPC) patients treated with abiraterone and to correlate those variations with long-term treatment outcome. PATIENTS AND METHODS: We retrospectively evaluated 330 CRPC patients in 11 Italian hospitals, monitoring PSA levels at baseline and every 4 weeks. Other clinical, biochemical and molecular parameters were determined at baseline...
April 20, 2017: Prostate
https://www.readbyqxmd.com/read/28428880/long-term-complete-remission-with-ipilimumab-in-metastatic-castrate-resistant-prostate-cancer-case-report-of-two-patients
#4
Luc Cabel, Elika Loir, Gwenaelle Gravis, Pernelle Lavaud, Christophe Massard, Laurence Albiges, Giulia Baciarello, Yohann Loriot, Karim Fizazi
BACKGROUND: Prostate cancer is one of the most common cancers in men and the fourth leading cause of cancer mortality worldwide. Although major progress has been achieved in the last years for patients with metastatic castrate-resistant prostate cancer (mCRPC), thanks to next-generation androgen receptor axis targeted drugs, taxanes, and bone-targeted agents, immunotherapy has not been widely approved and used for the treatment of prostate cancer. Two large studies with ipilimumab, an anti-CTLA-4 (cytotoxic T-lymphocyte antigen 4) antibody reported improved progression-free survival, but not statistically improved overall survival at the primary analysis (CA184 043 and CA184 095)...
2017: Journal for Immunotherapy of Cancer
https://www.readbyqxmd.com/read/28428441/selective-glucocorticoid-receptor-modulators-sgrms-delay-castrate-resistant-prostate-cancer-growth
#5
Jacob Kach, Tiha M Long, Phillip Selman, Eva Y Tonsing-Carter, Maria A Bacalao, Ricardo R Lastra, Larischa de Wet, Shane Comiskey, Marc Gillard, Calvin VanOpstall, Diana C West, Wen-Ching Chan, Donald Vander Griend, Suzanne D Conzen, Russell Z Szmulewitz
Increased glucocorticoid receptor (GR) expression and activity following androgen blockade can contribute to castration-resistant prostate cancer (CRPC) progression. Therefore, we hypothesized that GR antagonism will have therapeutic benefit in CRPC. However, the FDA-approved nonselective, steroidal GR antagonist, mifepristone, lacks GR specificity, reducing its therapeutic potential. Here we report that two novel non-steroidal and highly selective GR modulators (SGRMs), CORT118335 and CORT108297, have the ability to block GR activity in prostate cancer (PC) and slow CRPC progression...
April 20, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28427507/is-still-there-a-place-for-orteronel-in-management-of-prostate-cancer-data-from-a-literature-based-meta-analysis-of-randomized-trials
#6
REVIEW
Giandomenico Roviello, Chiara Pacifico, Giorgio Chiriacò, Daniele Generali
Orteronel (TAK-700) is an oral, non-steroidal 17,20-lyase inhibitor with higher specificity for 17,20 lyase over 17 hydroxylase. The first phase III studies showed an advantage with orteronel compared with placebo in terms of progression free survival and response of PSA. Unfortunately orteronel did not significantly prolong the overall survival. In order to assess the efficacy of orteronel in prostate cancer, we evaluated all available data on orteronel in the management of prostate cancer. A total of 2716 patients were evaluated from 3 randomized trials...
May 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/28422308/androgen-receptor-regulated-mirna-193a-3p-targets-ajuba-to-promote-prostate-cancer-cell-migration
#7
Li Jia, Bin Gui, Dali Zheng, Keith F Decker, Ilker Tinay, Mingyue Tan, Xiaowei Wang, Adam S Kibel
Background Dysregulation of microRNA (miRNA) expression is implicated in cancer development and progression by modulating oncogenes or tumor suppressors at the post-transcriptional level. Methods To investigate the role of miRNAs in prostate cancer (PCa) progression, we performed small RNA-sequencing (RNA-seq) analysis in androgen-dependent LNCaP cells and LNCaP-derived castration-resistant prostate cancer (CRPC) C4-2B cells. For functional validation, we specifically investigated miR-193a-3p, which is highly upregulated in C4-2B cells and modulated by the androgen receptor (AR)...
April 19, 2017: Prostate
https://www.readbyqxmd.com/read/28421240/a-randomised-phase-ii-study-of-repeated-rhenium-188-hedp-combined-with-docetaxel-and-prednisone-versus-docetaxel-and-prednisone-alone-in-castration-resistant-prostate-cancer-crpc-metastatic-to-bone-the-taxium-ii-trial
#8
Joyce M van Dodewaard-de Jong, John M H de Klerk, Haiko J Bloemendal, Daniela E Oprea-Lager, Otto S Hoekstra, H Pieter van den Berg, Maartje Los, Aart Beeker, Marianne A Jonker, Joe M O'Sullivan, Henk M W Verheul, Alfons J M van den Eertwegh
BACKGROUND: Rhenium-188-HEDP is a beta-emitting radiopharmaceutical used for palliation of metastatic bone pain. We investigated whether the addition of rhenium-188-HEDP to docetaxel/prednisone improved efficacy of chemotherapy in patients with CRPC. METHODS: Patients with progressive CRPC and osteoblastic bone metastases were randomised for first-line docetaxel 75 mg/m(2) 3-weekly plus prednisone with or without 2 injections of rhenium-188-HEDP after the third (40 MBq/kg) and after the sixth (20 MBq/kg) cycle of docetaxel...
April 18, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28413979/drug-resistance-of-enzalutamide-in-crpc
#9
Xuedong Chen, Jieyang Lu, Liqun Xia, Gonghui Li
Enzalutamide (MDV3100, XTANDI ) is a second generation androgen receptor inhibitor that is designed for the treatment of castration-resistant prostate cancer (CRPC) and has prolonged survival time. Although Enzalutamide was also associated with such significant benefits, The majority of treated patients, innate or acquired resistance invariably arises, but the mechanisms of mdv3100 resistance have not yet been clearly clarified. Nevertheless, because the better knowledge of the genetic landscape of MDV3100 is under way, resistance to MDV3100 could be basically divided in two distinct pathways, either dependent or independent of the androgen receptor activity...
April 17, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28411207/transdifferentiation-as-a-mechanism-of-treatment-resistance-in-a-mouse-model-of-castration-resistant-prostate-cancer
#10
Min Zou, Roxanne Toivanen, Antonina Mitrofanova, Nicolas Floc'h, Sheida Hayati, Yanping Sun, Clementine Le Magnen, Daniel Chester, Elahe A Mostaghel, Andrea Califano, Mark A Rubin, Michael M Shen, Cory Abate-Shen
Current treatments for castration-resistant prostate cancer (CPRC) that target androgen receptor (AR) signaling improve patient survival, yet ultimately fail. Here we provide novel insights into treatment response for the anti-androgen abiraterone by analyses of a genetically-engineered mouse model (GEMM) with combined inactivation of Trp53 and Pten, which are frequently co-mutated in human CRPC. These NPp53 mice fail to respond to abiraterone, and display accelerated progression to tumors resembling treatment-related CRPC with neuroendocrine differentiation (CRPC-NE) in humans...
April 14, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28410987/alkaline-phosphatase-velocity-predicts-overall-survival-and-bone-metastasis-in-patients-with-castration-resistant-prostate-cancer
#11
Kai H Hammerich, Timothy F Donahue, Inger L Rosner, Jennifer Cullen, Huai-Ching Kuo, Lauren Hurwitz, Yongmei Chen, Melanie Bernstein, Jonathan Coleman, Daniel C Danila, Adam R Metwalli
INTRODUCTION AND OBJECTIVES: Identifying patients with prostate cancer (CaP) who will ultimately develop bone metastasis (BM) or die of disease is essential. Alkaline phosphatase velocity (APV) has been shown to predict overall survival (OS) and bone metastasis-free survival (BMFS) in an earlier study of an equal access military patient cohort of patients with castrate-resistant prostate cancer (CRPC). To confirm these findings, we examined a cohort of patients from a high-volume cancer center to validate a previous observation that faster alkaline phosphatase (AP) kinetics are predictive of OS and BMFS in this second cohort of patients...
April 11, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/28410543/probing-the-prostate-tumour-microenvironment-ii-impact-of-hypoxia-on-a-cell-model-of-prostate-cancer-progression
#12
Claire Tonry, John Armstrong, Stephen Pennington
Approximately one in six men are diagnosed with Prostate Cancer every year in the Western world. Although it can be well managed and non-life threatening in the early stages, over time many patients cease to respond to treatment and develop castrate resistant prostate cancer (CRPC). CRPC represents a clinically challenging and lethal form of prostate cancer. Progression of CRPC is, in part, driven by the ability of cancer cells to alter their metabolic profile during the course of tumourgenesis and metastasis so that they can survive in oxygen and nutrient-poor environments and even withstand treatment...
February 28, 2017: Oncotarget
https://www.readbyqxmd.com/read/28392837/denosumab-treatment-in-the-management-of-patients-with-advanced-prostate-cancer-clinical-evidence-and-experience
#13
REVIEW
Miriam Hegemann, Jens Bedke, Arnulf Stenzl, Tilman Todenhöfer
Osteoprotective therapies have become an essential component in the management of advanced prostate cancer (PC) patients as bone metastases (BMs) have a major impact on morbidity and mortality. Denosumab is a fully humanized antibody targeting the receptor activator of nuclear factor κB ligand (RANKL), which has been approved by the European Medicines Agency (EMA) in Europe and the United States (US) Food and Drug Administration (FDA) in the US for prevention of skeletal-related events (SREs) in patients with solid tumors and BMs, including PC...
March 2017: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/28392539/headache-caused-by-brain-metastases-of-castration-resistant-prostate-cancer-during-cabazitaxel-therapy
#14
Keitaro Watanabe, Takeo Kosaka, Hiroshi Hongo, Satoshi Tamaki, Mototsugu Oya
We describe the case of a 55-year-old man who underwent four cycles of cabazitaxel therapy for castration-resistant prostate cancer (CRPC). After the fourth cycle of cabazitaxel, the patient experienced severe headaches. Brain gadolinium (Gd) contrast-enhanced magnetic resonance imaging (MRI) revealed multiple brain metastases. A few days later, the patient suffered impaired consciousness that progressed rapidly. The patient was treated for the symptoms of increased intracranial pressure and underwent whole-brain radiation...
April 7, 2017: Keio Journal of Medicine
https://www.readbyqxmd.com/read/28389619/differential-expression-of-oatp1b3-mediates-unconjugated-testosterone-influx
#15
Tristan M Sissung, Ariel M Ley, Jonathan D Strope, Edel M McCrea, Shaunna L Beedie, Cody J Peer, Suneet Shukla, Jennifer C van Velkinburgh, Kelie Reece, Sarah Troutman, Tessa Campbell, Elena Fernandez, Phoebe Huang, Jordan Smith, Nilay Thakkar, David Venzon, Steffan Brenner, Wooin Lee, Maria J Merino, Ji Luo, Walter Jager, Cindy H Chau, Douglas K Price, William D Figg
Castration resistant prostate cancer (CRPC) has greater intratumoral testosterone concentrations than similar tumors from eugonadal men; simple diffusion does not account for this observation. The present study was undertaken to ascertain the androgen uptake kinetics, functional, and clinical relevance of de novo expression of the steroid hormone transporter OATP1B3 (SLCO1B3). Experiments testing the cellular uptake of androgens suggest that testosterone is an excellent substrate of OATP1B3 (KM=23.2µM; VMAX=321...
April 7, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28389515/androgen-signaling-in-prostate-cancer
#16
Charles Dai, Hannelore Heemers, Nima Sharifi
The androgen-signaling axis plays a pivotal role in the pathogenesis of prostate cancer. Since the landmark discovery by Huggins and Hodges, gonadal depletion of androgens has remained a mainstay of therapy for advanced disease. However, progression to castration-resistant prostate cancer (CRPC) typically follows and is largely the result of restored androgen signaling. Efforts to understand the mechanisms behind CRPC have revealed new insights into dysregulated androgen signaling and intratumoral androgen synthesis, which has ultimately led to the development of several novel androgen receptor (AR)-directed therapies for CRPC...
April 7, 2017: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/28386843/differential-expression-of-ap-1-transcription-factors-in-human-prostate-lncap-and-pc-3-cells-role-of-fra-1-in-transition-to-crpc-status
#17
K Kavya, M Naveen Kumar, Rajeshwari H Patil, Shubha M Hegde, K M Kiran Kumar, Rashmi Nagesh, R L Babu, Govindarajan T Ramesh, S Chidananda Sharma
Androgen receptor (AR) signaling axis plays a vital role in the development of prostate and critical in the progression of prostate cancer. Androgen withdrawal initially regresses tumors but eventually develops into aggressive castration-resistant prostate cancer (CRPC). Activator Protein-1 (AP-1) transcription factors are most likely to be associated with malignant transformation in prostate cancer. Hence, to determine the implication of AR and AP-1 in promoting the transition of prostate cancer to the androgen-independent state, we used AR-positive LNCaP and AR-negative PC-3 cells as an in vitro model system...
April 6, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28384066/clinical-significance-of-androgen-receptor-splice-variant-7-mrna-detection-in-circulating-tumor-cells-of-men-with-metastatic-castration-resistant-prostate-cancer-treated-with-first-and-second-line-abiraterone-and-enzalutamide
#18
Emmanuel S Antonarakis, Changxue Lu, Brandon Luber, Hao Wang, Yan Chen, Yezi Zhu, John L Silberstein, Maritza N Taylor, Benjamin L Maughan, Samuel R Denmeade, Kenneth J Pienta, Channing J Paller, Michael A Carducci, Mario A Eisenberger, Jun Luo
Purpose We reported previously that the detection of androgen receptor splice variant-7 (AR-V7) mRNA in circulating tumor cells (CTCs) correlated with poor outcomes from the use of abiraterone and enzalutamide in patients with castration-resistant prostate cancer (CRPC). Here, we expanded our cohort size to better characterize the prognostic significance of AR-V7 in this setting. Methods We prospectively enrolled 202 patients with CRPC starting abiraterone or enzalutamide and investigated the prognostic value of CTC detection (+ v -) and AR-V7 detection (+ v -) using a CTC-based AR-V7 mRNA assay...
April 6, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28380417/prospects-of-estrogen-receptor-%C3%AE-activation-in-the-treatment-of-castration-resistant-prostate-cancer
#19
Julia Gehrig, Silke Kaulfuß, Hubertus Jarry, Felix Bremmer, Mark Stettner, Peter Burfeind, Paul Thelen
Advanced prostate cancer can develop into castration-resistant prostate cancer (CRPC). This process is mediated either by intratumoral ligand synthesis or by mutations or aberrations of the androgen receptor (AR) or its cofactors. To date, no curative therapy for CRPC is available, as AR-targeted therapies eventually result in the development of resistance. The human prostate cancer cell line VCaP (vertebral cancer of the prostate) overexpresses AR and its splice variants (ARVs) as a mechanism of resistance to androgen-deprivation therapy (ADT) of external and intratumoral origin...
March 23, 2017: Oncotarget
https://www.readbyqxmd.com/read/28377721/prostate-cancer-and-aspirin-use-synopsis-of-the-proposed-molecular-mechanisms
#20
REVIEW
Nadeem Bilani, Hisham Bahmad, Wassim Abou-Kheir
Background: Prostate cancer (PCa) is a critical health burden, impacting the morbidity and mortality of millions of men around the world. Most of the patients with PCa have their disease at first sensitive to androgen deprivation treatments, but later they develop resistance to therapy and eventually die of metastatic castration-resistant prostate cancer (CRPC). Although the newly developed anti-androgen therapies are effectively alleviating symptoms and prolonging lives of patients, there are still no curable treatments for CRPC...
2017: Frontiers in Pharmacology
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