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https://www.readbyqxmd.com/read/29780751/metastatic-castration-resistant-prostate-cancer-and-the-challenge-of-a-patient-with-chronic-kidney-disease-in-hemodialysis
#1
Joana Simões, Isabel Augusto, Sara Meireles, Lurdes Vendeira, Carlos Silva
At a time when the population shows increasing longevity, entities such as cancer and chronic kidney disease (CKD) are more frequently connected. In the United States, approximately 6% of the patients on hemodialysis have cancer. The challenge to manage oncologic patients with CKD in a hemodialytic program represents a great shortage of available information on the choice of the best drug, timing, dosage adjustments, dialysis method, and treatment safety. We present the case of a patient with prostate cancer and terminal CKD in hemodialysis, and the treatment sequence after the development of resistance to hormonal blockade therapy, which included docetaxel, enzalutamide, and radium-223...
April 2018: Autopsy & Case Reports
https://www.readbyqxmd.com/read/29764892/intense-exercise-for-survival-among-men-with-metastatic-castrate-resistant-prostate-cancer-interval-gap4-a-multicentre-randomised-controlled-phase-iii-study-protocol
#2
Robert U Newton, Stacey A Kenfield, Nicolas H Hart, June M Chan, Kerry S Courneya, James Catto, Stephen P Finn, Rosemary Greenwood, Daniel C Hughes, Lorelei Mucci, Stephen R Plymate, Stephan F E Praet, Emer M Guinan, Erin L Van Blarigan, Orla Casey, Mark Buzza, Sam Gledhill, Li Zhang, Daniel A Galvão, Charles J Ryan, Fred Saad
INTRODUCTION: Preliminary evidence supports the beneficial role of physical activity on prostate cancer outcomes. This phase III randomised controlled trial (RCT) is designed to determine if supervised high-intensity aerobic and resistance exercise increases overall survival (OS) in patients with metastatic castrate-resistant prostate cancer (mCRPC). METHODS AND ANALYSIS: Participants (n=866) must have histologically documented metastatic prostate cancer with evidence of progressive disease on androgen deprivation therapy (defined as mCRPC)...
May 14, 2018: BMJ Open
https://www.readbyqxmd.com/read/29760584/lsd1-inhibition-attenuates-androgen-receptor-v7-splice-variant-activation-in-castration-resistant-prostate-cancer-models
#3
Sergio Regufe da Mota, Sarah Bailey, Rosemary A Strivens, Annette L Hayden, Leon R Douglas, Patrick J Duriez, M Teresa Borrello, Hanae Benelkebir, A Ganesan, Graham Packham, Simon J Crabb
Background: Castrate resistant prostate cancer (CRPC) is often driven by constitutively active forms of the androgen receptor such as the V7 splice variant (AR-V7) and commonly becomes resistant to established hormonal therapy strategies such as enzalutamide as a result. The lysine demethylase LSD1 is a co-activator of the wild type androgen receptor and a potential therapeutic target in hormone sensitive prostate cancer. We evaluated whether LSD1 could also be therapeutically targeted in CRPC models driven by AR-V7...
2018: Cancer Cell International
https://www.readbyqxmd.com/read/29752180/-177-lu-psma-617-radionuclide-treatment-in-patients-with-metastatic-castration-resistant-prostate-cancer-lupsma-trial-a-single-centre-single-arm-phase-2-study
#4
Michael S Hofman, John Violet, Rodney J Hicks, Justin Ferdinandus, Sue Ping Thang, Tim Akhurst, Amir Iravani, Grace Kong, Aravind Ravi Kumar, Declan G Murphy, Peter Eu, Price Jackson, Mark Scalzo, Scott G Williams, Shahneen Sandhu
BACKGROUND: Progressive metastatic castration-resistant prostate cancer is a highly lethal disorder and new effective therapeutic agents that improve patient outcomes are urgently needed. Lutetium-177 [177 Lu]-PSMA-617, a radiolabelled small molecule, binds with high affinity to prostate-specific membrane antigen (PSMA) enabling beta particle therapy targeted to metastatic castration-resistant prostate cancer. We aimed to investigate the safety, efficacy, and effect on quality of life of [177 Lu]-PSMA-617 in men with metastatic castration-resistant prostate cancer who progressed after standard treatments...
May 7, 2018: Lancet Oncology
https://www.readbyqxmd.com/read/29748619/eukaryotic-translation-initiation-factor-4-gamma-1-eif4g1-is-upregulated-during-prostate-cancer-progression-and-modulates-cell-growth-and-metastasis
#5
Praveen Kumar Jaiswal, Sweaty Koul, Prakash S T Shanmugam, Hari K Koul
eIF4G1, a critical component of the eIF4F complex, is required for cap-dependent mRNA translation, a process necessary for tumor growth and survival. However, the role of eIF4G1 has not been evaluated in Prostate Cancer (PCa). We observed an increased eIF4G1 protein levels in PCa tissues as compared to normal tissues. Analysis of the TCGA data revealed that eIF4G1 gene expression positively correlated with higher tumor grade and stage. Furthermore, eIF4G1 was over-expressed and or amplified, in 16% patients with metastatic PCa (SU2C/PCF Dream Team dataset) and in 59% of castration-resistant prostate cancer (CRPC) patients (Trento/Cornell/Broad dataset)...
May 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29742084/first-line-use-of-novel-hormonal-agents-in-prostate-cancer-a-critical-appraisal
#6
Derek Raghavan
Castration has been the hallmark of the treatment of advanced prostate cancer for nearly a century. Conventional surgical or medical castration for the management of metastatic prostate cancer has been associated with an initial response rate greater than 60% to 70%, depending on the criteria employed. The median duration of the initial response is usually less than 3 to 5 years, however, depending on the extent of disease. The failure of disease to respond to castration has been associated with an increase in the production of adrenal androgens and/or the evolution of upregulated or mutated androgen receptors...
April 2018: Clinical Advances in Hematology & Oncology: H&O
https://www.readbyqxmd.com/read/29741399/enzalutamide-and-analytical-interferences-in-digoxin-assays
#7
Marie Deguigne, Marion Brunet, Chadi Abbara, Alain Turcant, Gaël Le Roux, Bénédicte Lelièvre
OBJECTIVE: We report two cases of elevated digoxin plasma levels in patients receiving enzalutamide. Cases reported: The first patient, an 84-year-old male treated with enzalutamide, was hospitalized due to deterioration in his general state. Atrial fibrillation was discovered and treatment with digoxin was initiated. Supratherapeutic digoxin concentrations (4 µg/L and 3.5 µg/L 3 days later) led to treatment being stopped despite the lack of clinical or biological signs of overdose...
May 9, 2018: Clinical Toxicology
https://www.readbyqxmd.com/read/29734647/recent-advances-in-prostate-cancer-treatment-and-drug-discovery
#8
REVIEW
Ekaterina Nevedomskaya, Simon J Baumgart, Bernard Haendler
Novel drugs, drug sequences and combinations have improved the outcome of prostate cancer in recent years. The latest approvals include abiraterone acetate, enzalutamide and apalutamide which target androgen receptor (AR) signaling, radium-223 dichloride for reduction of bone metastases, sipuleucel-T immunotherapy and taxane-based chemotherapy. Adding abiraterone acetate to androgen deprivation therapy (ADT) in order to achieve complete androgen blockade has proven highly beneficial for treatment of locally advanced prostate cancer and metastatic hormone-sensitive prostate cancer (mHSPC)...
May 4, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29731997/androgen-receptor-a-potential-therapeutic-target-for-glioblastoma
#9
Nomi Zalcman, Tamar Canello, Haim Ovadia, Hanna Charbit, Bracha Zelikovitch, Anat Mordechai, Yakov Fellig, Stav Rabani, Tal Shahar, Alexander Lossos, Iris Lavon
The median survival time of patients with glioblastoma is still poor (14.6 month), partly due to a lack of effective treatment. We have observed that androgen receptor (AR) is amplified in glioblastomas at the DNA, RNA and protein levels. The AR gene was amplified in 27% of glioblastoma specimens from men (n=22) and of 38.2% from women (n=21). AR-RNA was overexpressed (>2.5 fold) in 93% (n=30), and AR-protein was induced (>two fold) in 56% of the glioblastomas samples (n=16). Thirty percent of the glioblastomas (n=21) also expressed a constitutively active AR-splice-variant (AR-V7/AR3) lacking the Ligand-Binding-Domain...
April 13, 2018: Oncotarget
https://www.readbyqxmd.com/read/29731989/statin-use-and-survival-in-patients-with-metastatic-castration-resistant-prostate-cancer-treated-with-abiraterone-or-enzalutamide-after-docetaxel-failure-the-international-retrospective-observational-staben-study
#10
Jacob A Gordon, Carlo Buonerba, Gregory Pond, Daniel Crona, Silke Gillessen, Giuseppe Lucarelli, Sabrina Rossetti, Tanya Dorff, Salvatore Artale, Jennifer A Locke, Davide Bosso, Matthew Ivan Milowsky, Mira Sofie Witek, Michele Battaglia, Sandro Pignata, Cyrus Cherhroudi, Michael E Cox, Pietro De Placido, Dario Ribera, Aurelius Omlin, Gaetano Buonocore, Kim Chi, Christian Kollmannsberger, Daniel Khalaf, Gaetano Facchini, Guru Sonpavde, Sabino De Placido, Bernhard J Eigl, Giuseppe Di Lorenzo
Background: Statins may potentiate the effects of anti-hormonal agents for metastatic castration-resistant prostate cancer (mCRPC) through further disruption of essential steroidogenic processes. We investigated the effects of statin use on clinical outcomes in patients with mCRPC receiving abiraterone or enzalutamide. Materials and methods: This was a retrospective multicenter study including patients that received abiraterone or enzalutamide for mCRPC. The effect of concurrent statin use on outcomes was evaluated...
April 13, 2018: Oncotarget
https://www.readbyqxmd.com/read/29730201/androgen-receptor-targeted-treatments-for-prostate-cancer-35-years-progress-with-antiandrogens
#11
REVIEW
E David Crawford, Paul F Schellhammer, David G McLeod, Judd W Moul, Celestia S Higano, Neal Shore, Louis Denis, Peter Iversen, Mario A Eisenberger, Fernand Labrie
PURPOSE: Antiandrogens inhibit the androgen receptor (AR) and play an important role in the treatment of prostate cancer (PC). This review provides a historical perspective on the development and clinical benefit of antiandrogens in the treatment of PC. MATERIALS AND METHODS: We searched PubMed® for clinical trials with the search terms "antiandrogens" and "prostate cancer" combined with drug names for antiandrogens. This article represents a collaboration of clinical investigators who have made critical scientific contributions leading to the approval of antiandrogens for treating patients with PC...
May 3, 2018: Journal of Urology
https://www.readbyqxmd.com/read/29713287/transcriptional-repression-and-protein-degradation-of-the-ca-2-activated-k-channel-k-ca-1-1-by-androgen-receptor-inhibition-in-human-breast-cancer-cells
#12
Anowara Khatun, Motoki Shimozawa, Hiroaki Kito, Mayu Kawaguchi, Mayu Fujimoto, Moe Ri, Junko Kajikuri, Satomi Niwa, Masanori Fujii, Susumu Ohya
The large-conductance Ca2+ -activated K+ channel KCa 1.1 plays an important role in the promotion of breast cancer cell proliferation and metastasis. The androgen receptor (AR) is proposed as a therapeutic target for AR-positive advanced triple-negative breast cancer. We herein investigated the effects of a treatment with antiandrogens on the functional activity, activation kinetics, transcriptional expression, and protein degradation of KCa 1.1 in human breast cancer MDA-MB-453 cells using real-time PCR, Western blotting, voltage-sensitive dye imaging, and whole-cell patch clamp recording...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29712692/identification-of-a-small-molecule-that-selectively-inhibits-erg-positive-cancer-cell-growth
#13
Ahmed A Mohamed, Charles P Xavier, Gauthaman Sukumar, Shyh-Han Tan, Lakshmi Ravindranath, Nishat Seraj, Vineet Kumar, Taduru L Sreenath, David G McLeod, Gyorgy Petrovics, Inger Rosner, Meera Srivastava, Jeffrey Strovel, Sanjay V Malhotra, Nicole A LaRonde, Albert Dobi, Clifton L Dalgard, Shiv Srivastava
Oncogenic activation of ERG by recurrent gene fusions (predominantlyTMPRSS2-ERG) is one of the most validated and prevalent genomic alterations present in early stages of prostate cancer. In this study, we screened small molecule libraries for inhibition of ERG protein in TMPRSS2-ERG harboring VCaP prostate cancer cells using an In-Cell Western Assay with the highly specific ERG-MAb (9FY). Among a subset of promising candidates, 1-[2-Thiazolylazo]-2-naphthol (NSC139021, here after ERGi-USU) was identified and further characterized...
April 30, 2018: Cancer Research
https://www.readbyqxmd.com/read/29709784/validation-of-an-lc-ms-ms-method-for-simultaneous-quantitation-of-enzalutamide-n-desmethylenzalutamide-apalutamide-darolutamide-and-orm-15341-in-mice-plasma-and-its-application-to-a-mice-pharmacokinetic-study
#14
Suresh P Sulochana, Neeraj Kumar Saini, Prasanthi Daram, Sai Babu Polina, Ramesh Mullangi
A sensitive and rapid LC-MS/MS method was developed and validated for the simultaneous quantitation of enzalutamide, N-desmethylenzalutamide (active metabolite of enzalutamide), apalutamide, darolutamide and ORM-15341 (active metabolite of darolutamide) in mice plasma as per regulatory guidelines. The analytes and the internal standard (I.S.: apalutamide-d3 ) were extracted from 50 μL mice plasma by simple protein precipitation using acetonitrile, followed by chromatographic separation using an Atlantis C18 column with an isocratic mobile (0...
April 24, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29700003/inhibition-of-the-wnt-%C3%AE-catenin-pathway-overcomes-resistance-to-enzalutamide-in-castration-resistant-prostate-cancer
#15
Zhuangzhuang Zhang, Lijun Cheng, Jie Li, Elia Farah, Nadia M Atallah, Pete E Pascuzzi, Sanjay Gupta, Xiaoqi Liu
Enzalutamide is a second-generation nonsteroidal antiandrogen clinically approved for the treatment of castration-resistant prostate cancer (CRPC), yet resistance to endocrine therapy has limited its success in this setting. Although the androgen receptor (AR) has been associated with therapy failure, the mechanisms underlying this failure have not been elucidated. Bioinformatics analysis predicted that activation of the Wnt/β-catenin pathway and its interaction with AR play a major role in acquisition of enzalutamide resistance...
April 26, 2018: Cancer Research
https://www.readbyqxmd.com/read/29695920/profile-of-apalutamide-in-the-treatment-of-metastatic-castration-resistant-prostate-cancer-evidence-to-date
#16
REVIEW
Julio T Chong, William K Oh, Bobby C Liaw
Advances in therapies have led to the approval of six therapeutic agents since 2004, each demonstrating overall survival benefit in randomized studies, and these have significantly improved the outlook for men facing metastatic castration-resistant prostate cancer (CRPC). More recently, efforts have been directed at trying to effect change at earlier phases of the disease. Apalutamide (ARN-509), a second-generation androgen receptor antagonist, recently received approval in the nonmetastatic (M0) CRPC space...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29688882/withdrawn-disparity-in-public-funding-of-therapies-for-metastatic-castrate-resistant-prostate-cancer-across-canadian-provinces
#17
Dixon T S Woon, Thenappan Chandrasekar, Lorne Aaron, Naveen S Basappa, Kim N Chi, Henry J Conter, Brita Danielson, Sebastien J Hotte, Shawn Malone, Fred Saad, Bobby Shayegan, Laura Park-Wyllie, Robert J Hamilton
Ahead of print article withdrawn by publisher.
April 12, 2018: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
https://www.readbyqxmd.com/read/29682197/synthesis-and-anticancer-activity-of-the-derivatives-of-marine-compound-rhizochalin-in-castration-resistant-prostate-cancer
#18
Sergey A Dyshlovoy, Katharina Otte, Kseniya M Tabakmakher, Jessica Hauschild, Tatyana N Makarieva, Larisa K Shubina, Sergey N Fedorov, Carsten Bokemeyer, Valentin A Stonik, Gunhild von Amsberg
Development of resistance to standard therapies complicates treatment of advanced prostate cancer. Alternative splicing variants of the androgen receptor (AR), e.g. AR-V7 can mediate resistance to AR-targeting substances abiraterone and enzalutamide. Semi-synthetic marine natural compound rhizochalinin decreases the expression of AR-V7 in human castration-resistant prostate cancer cells and thus resensitizes cells to enzalutamide. In the current study, we modified the structure of rhizochalin in order to determine structure-activity relationships (SAR) and optimize anticancer properties...
March 30, 2018: Oncotarget
https://www.readbyqxmd.com/read/29682196/testosterone-metabolites-inhibit-proliferation-of-castration-and-therapy-resistant-prostate-cancer
#19
Felix Bremmer, Hubertus Jarry, Valerie Unterkircher, Silke Kaulfuss, Peter Burfeind, Heinz-Joachim Radzun, Philipp Ströbel, Paul Thelen
Novel treatments for castration-resistant prostate cancer (CRPC) such as abiraterone acetate (AA) or enzalutamide effectively target the androgen pathway to arrest aberrant signalling and cell proliferation. Testosterone is able to inhibit tumour cell growth in CRPC. Estrogen receptor-beta (ERβ) binds the testosterone-metabolites 3β-androstanediol and 3α-androstanediol in parallel to the canonical estradiol. In the prostate it is widely accepted that ERβ regulates estrogen signalling, mediating anti-proliferative effects...
March 30, 2018: Oncotarget
https://www.readbyqxmd.com/read/29673712/update-on-systemic-prostate-cancer-therapies-management-of-metastatic-castration-resistant-prostate-cancer-in-the-era-of-precision-oncology
#20
REVIEW
Philipp Nuhn, Johann S De Bono, Karim Fizazi, Stephen J Freedland, Maurizio Grilli, Philip W Kantoff, Guru Sonpavde, Cora N Sternberg, Srinivasan Yegnasubramanian, Emmanuel S Antonarakis
CONTEXT: Introduction of novel agents for the management of advanced prostate cancer provides a range of treatment options with notable benefits for men with metastatic castration-resistant prostate cancer (mCRPC). At the same time, understanding of optimal patient selection, effective sequential use, and development of resistance patterns remains incomplete. OBJECTIVE: To review current systemic therapies and recent advances in drug development for mCRPC and strategies to aid in patient selection and optimal sequencing...
April 16, 2018: European Urology
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