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Enzalutamide

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https://www.readbyqxmd.com/read/29165815/development-and-validation-of-a-liquid-chromatography-tandem-mass-spectrometry-analytical-method-for-the-therapeutic-drug-monitoring-of-eight-novel-anticancer-drugs
#1
M Herbrink, N de Vries, H Rosing, A D R Huitema, B Nuijen, J H M Schellens, J H Beijnen
To support therapeutic drug monitoring (TDM) of patients with cancer, a fast and accurate method for simultaneous quantification of the registered anticancer drugs afatinib, axitinib, ceritinib, crizotinib, dabrafenib, enzalutamide, regorafenib and trametinib in human plasma using liquid chromatography tandem mass spectrometry was developed and validated. Human plasma samples were collected from treated patients and stored at -20 (o) C. Analytes and internal standards (stable isotopically labeled analytes) were extracted with acetonitrile...
November 22, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29164346/impact-of-prior-androgen-receptor-axis-targeted-agents-on-the-clinical-activity-of-subsequent-docetaxel-in-patients-with-metastatic-castration-resistant-prostate-cancer-comparative-assessment-between-abiraterone-acetate-and-enzalutamide
#2
Hideaki Miyake, Yuto Matsushita, Keita Tamura, Daisuke Motoyama, Toshiki Ito, Takayuki Sugiyama, Atsushi Otsuka
The objective of this study was to investigate the impact of prior treatment with androgen receptor-axis-targeted (ARAT) agents, abiraterone acetate (AA) and enzalutamide (Enz), on the activity of subsequently introduced docetaxel in patients with metastatic castration-resistant prostate cancer (mCRPC). This study included a total of 114 mCRPC patients consisting of 54 and 60 who progressed following treatment with AA and Enz, respectively, prior to the introduction of docetaxel, and compared oncological outcomes with docetaxel between these two groups...
November 21, 2017: Medical Oncology
https://www.readbyqxmd.com/read/29158269/the-glucocorticoid-receptor-is-a-key-player-for-prostate-cancer-cell-survival-and-a-target-for-improved-anti-androgen-therapy
#3
Martin Puhr, Julia Hoefer, Andrea Eigentler, Christian Ploner, Florian Handle, Georg Schaefer, Jan Kroon, Angela Leo, Isabel M Heidegger, Iris E Eder, Zoran Culig, Gabri van der Pluijm, Helmut Klocker
PURPOSE: The major obstacle in the management of advanced prostate cancer (PCa) is the occurrence of resistance to endocrine-therapy. Although the androgen receptor (AR) has been linked to therapy failure, the underlying escape mechanisms have not been fully clarified. Being closely related to the AR, the glucocorticoid receptor (GR) has been suggested to play a role in enzalutamide and docetaxel resistance. Given that glucocorticoids are frequently applied to PCa patients, it is essential to unravel the exact role of the GR in PCa progression...
November 20, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29150561/influence-of-enzalutamide-on-cabazitaxel-pharmacokinetics-a-drug-drug-interaction-study-in-metastatic-castration-resistant-prostate-cancer-mcrpc-patients
#4
Bodine P S Belderbos, Sander Bins, Roelof W F van Leeuwen, Esther Oomen-de Hoop, Nelly van der Meer, Peter de Bruijn, Paul Hamberg, Esther N M Overkleeft, Wendy M van der Deure, Martijn Lolkema, Ronald de Wit, Ron H J Mathijssen
PURPOSE: In ongoing clinical research on metastatic castration-resistant prostate cancer (mCRPC) treatment, the potential enhanced efficacy of the combination of taxanes with AR-targeted agents, i.e. enzalutamide and abiraterone, is currently being explored. Since enzalutamide induces the CYP3A4 enzyme and taxanes are metabolized by this enzyme, a potential drug-drug interaction needs to be investigated. DESIGN: Therefore, we performed a pharmacokinetic cross-over study in mCRPC patients who were scheduled for treatment with cabazitaxel Q3W (25 mg/m(2))...
November 17, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29147733/-inhibitors-of-the-androgen-receptor-n%C3%A2-terminal-domain-therapies-targeting-the-achilles-heel-of-various-androgen-receptor-molecules-in-advanced-prostate-cancer
#5
REVIEW
M C Hupe, A Offermann, F Perabo, C Chandhasin, S Perner, A S Merseburger, M V Cronauer
Although prostate cancer responds well to primary endocrine therapies, tumor progression with castration resistant tumor cells almost invariably occurs within a few years. Unfortunately, some CRPC patients do not respond to second-line therapies with abiraterone or enzalutamide. Moreover, patients who initially responded well to second-line hormone therapy develop resistance to abiraterone and/or enzalutamide within a short period of time. Besides an increase of intracellular androgen receptor (AR) levels, the predominant resistance mechanisms include AR aberrations (point mutations, AR splice variants) occurring predominantly at the androgen or ligand binding domain of the AR...
November 16, 2017: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/29138500/circulating-androgen-receptor-combined-with-18f-fluorocholine-pet-ct-metabolic-activity-and-outcome-to-androgen-receptor-signalling-directed-therapies-in-castration-resistant-prostate-cancer
#6
V Conteduca, E Scarpi, P Caroli, S Salvi, C Lolli, S L Burgio, C Menna, G Schepisi, S Testoni, G Gurioli, G Paganelli, V Casadio, F Matteucci, U De Giorgi
The association between choline uptake and androgen receptor (AR) expression is suggested by the upregulation of choline kinase-alpha in prostate cancer. Recently, detection of AR aberration in cell-free DNA as well as early 18F-fluorocholine positron emission tomography/computed tomography (FCH-PET/CT) were associated with outcome in metastatic castration-resistant prostate cancer (mCRPC) patients treated with abiraterone and enzalutamide. We aimed to make a direct comparison between circulating AR copy number (CN) and choline uptake at FCH-PET/CT...
November 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29137449/differential-side-effects-profile-in-patients-with-mcrpc-treated-with-abiraterone-or-enzalutamide-a-meta-analysis-of-randomized-controlled-trials
#7
REVIEW
Raphael B Moreira, Marcio Debiasi, Edoardo Francini, Pier V Nuzzo, Guillermo De Velasco, Fernando C Maluf, Andre P Fay, Joaquim Bellmunt, Toni K Choueiri, Fabio A Schutz
Background: Abiraterone and enzalutamide are currently approved for mCRPC patients. Both drugs have distinct mechanisms of action and may have different toxicity profile. There are limited data comparing the side effects of abiraterone and enzalutamide. We performed a meta-analysis of randomized controlled trials (RCT) to better characterize the risk of adverse events associated with both drugs. Methods: We performed a literature search on MEDLINE for studies reporting abiraterone and enzalutamide side effects from January 1966 to July 31, 2015...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29134684/enhanced-radiosensitization-of-enzalutamide-via-schedule-dependent-administration-to-androgen-sensitive-prostate-cancer-cells
#8
Maryam Ghashghaei, Miltiadis Paliouras, Mitra Heravi, Hamed Bekerat, Mark Trifiro, Tamim M Niazi, Thierry Muanza
BACKGROUND: Prostate cancer (PCa) is a progressive disease and the most diagnosed cancer in men. The current standard of care for high-risk localized PCa is a combination of androgen deprivation therapy (ADT) and radiation (XRT). The majority of these patients however become resistant due to incomplete responses to ADT as a result of selective cells maintaining androgen receptor (AR) activity. Improvement can be made if increasing radiosensitivity is realized. Therefore, the aim of this study is to investigate the efficacy of the next-generation PCa drug Enzalutamide (ENZA), as a radiosensitizer in XRT therapy...
November 14, 2017: Prostate
https://www.readbyqxmd.com/read/29134562/seom-clinical-guidelines-for-the-treatment-of-metastatic-prostate-cancer-2017
#9
J Cassinello, J Á Arranz, J M Piulats, A Sánchez, B Pérez-Valderrama, B Mellado, M Á Climent, D Olmos, J Carles, M Lázaro
Androgen deprivation treatment was the only treatment available for metastatic prostate cancer until recently, with docetaxel as the only treatment with a proven survival benefit in castration-resistant prostate cancer (CRPC). Several drugs have been approved in the castration-resistant disease (sipuleucel-T, cabazitaxel, abiraterone, enzalutamide, radium-223). More recently, docetaxel and abiraterone have been moved to the hormone-sensitive disease setting, achieving better patient survival. The purpose of this article is to define the state of the art in the treatment of prostate carcinoma...
November 13, 2017: Clinical & Translational Oncology
https://www.readbyqxmd.com/read/29129398/genomic-markers-in-prostate-cancer-decision-making
#10
REVIEW
Vito Cucchiara, Matthew R Cooperberg, Marc Dall'Era, Daniel W Lin, Francesco Montorsi, Jack A Schalken, Christopher P Evans
CONTEXT: Although the widespread use of prostate-specific antigen (PSA) has led to an early detection of prostate cancer (PCa) and a reduction of metastatic disease at diagnosis, PSA remains one of the most controversial biomarkers due to its limited specificity. As part of emerging efforts to improve both detection and management decision making, a number of new genomic tools have recently been developed. OBJECTIVE: This review summarizes the ability of genomic biomarkers to recognize men at high risk of developing PCa, discriminate clinically insignificant and aggressive tumors, and facilitate the selection of therapies in patients with advanced disease...
November 9, 2017: European Urology
https://www.readbyqxmd.com/read/29129028/improved-cancer-specific-free-survival-and-overall-free-survival-in-contemporary-metastatic-prostate-cancer-patients-a-population-based-study
#11
Marco Bandini, Raisa S Pompe, Michele Marchioni, Emanuele Zaffuto, Giorgio Gandaglia, Nicola Fossati, Luca Cindolo, Francesco Montorsi, Alberto Briganti, Fred Saad, Pierre I Karakiewicz
OBJECTIVES: Over the past decade, several systemic agents as docetaxel, cabazitaxel, sipuleucel-T, abiraterone and enzalutamide have improved overall survival (OS) in metastatic prostate cancer (mPCa) patients. However, to date the OS benefit was not demonstrated in population-based analysis. METHODS: Between 2004 and 2014, 19,047 men with de novo mPCa were identified within the Surveillance Epidemiology and End Results database. Median year of diagnosis resulted in two groups: historical (2004-2008) and contemporary (2009-2014)...
November 11, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/29126837/antiandrogens-reduce-intratumoral-androgen-concentrations-and-induce-androgen-receptor-expression-in-castration-resistant-prostate-cancer-xenografts
#12
Matias Knuuttila, Arfa Mehmood, Riikka Huhtaniemi, Emrah Yatkin, Merja R Häkkinen, Riikka Oksala, Teemu D Laajala, Henrik Ryberg, David J Handelsman, Tero Aittokallio, Seppo Auriola, Claes Ohlsson, Asta Laiho, Laura L Elo, Petra Sipilä, Sari I Mäkelä, Matti Poutanen
The development of castration-resistant prostate cancer (CRPC) is associated with the activation of intratumoral androgen biosynthesis and an increase in androgen receptor (AR) expression. We recently demonstrated that similarly to the clinical CRPC, orthotopically grown castration-resistant VCaP (CR-VCaP) xenografts express high levels of AR and retain intratumoral androgen concentrations similar to tumors grown in intact mice. Here, we show that antiandrogen treatment (enzalutamide or ARN-509) significantly reduced (10-fold, P < 0...
November 7, 2017: American Journal of Pathology
https://www.readbyqxmd.com/read/29125926/anticoagulation-and-enzalutamide-caution-over-convenience
#13
Hanny Al-Samkari, Jean M Connors
No abstract text is available yet for this article.
November 2017: Journal of Oncology Practice
https://www.readbyqxmd.com/read/29125924/anticoagulants-could-be-a-victim-of-enzalutamide
#14
Krishna Gundabolu
No abstract text is available yet for this article.
November 2017: Journal of Oncology Practice
https://www.readbyqxmd.com/read/29125921/management-of-anticoagulation-in-patients-with-prostate-cancer-receiving-enzalutamide
#15
Joseph J Shatzel, Molly M Daughety, Sven R Olson, Tomasz M Beer, Thomas G DeLoughery
Enzalutamide, a novel, oral androgen receptor antagonist used for the treatment of metastatic, castration-resistant prostate cancer, has been shown to improve overall and progression-free survival, prolong time to initiation of chemotherapy, reduce skeletal-related events, and carry a favorable adverse effect profile. Metastatic prostate cancer is a disease of older men, a population with an increased incidence of medical comorbidities warranting anticoagulation. Prostate cancer itself, along with some of its therapies, is also prothrombotic...
November 2017: Journal of Oncology Practice
https://www.readbyqxmd.com/read/29121144/positron-emission-tomography-computed-tomography-based-assessments-of-androgen-receptor-expression-and-glycolytic-activity-as-a-prognostic-biomarker-for-metastatic-castration-resistant-prostate-cancer
#16
Josef J Fox, Somali C Gavane, Estelle Blanc-Autran, Sadek Nehmeh, Mithat Gönen, Brad Beattie, Hebert A Vargas, Heiko Schöder, John L Humm, Samson W Fine, Jason S Lewis, Stephen B Solomon, Joseph R Osborne, Darren Veach, Charles L Sawyers, Wolfgang A Weber, Howard I Scher, Michael J Morris, Steven M Larson
Importance: Androgen receptor-signaling inhibitor (ARSi) drugs prolong life in metastatic castration-resistant prostate cancer (mCRPC), but such tumors eventually become resistant and progress. Comprehensive positron emission tomography/computed tomography (PET/CT) imaging using fluoro-2-D-deoxyglucose F 18 ([18F]-FDG) for glycolysis (Glyc) and fluorodihydrotestosterone F 18 ([18F]-FDHT) for androgen receptor (AR) expression determine heterogeneity of imaging phenotypes, which may be useful in distinguishing patients who will benefit from ARSi drugs from those who need alternative treatments...
November 9, 2017: JAMA Oncology
https://www.readbyqxmd.com/read/29119053/enzalutamide-as-an-androgen-receptor-inhibitor-prevents-urothelial-tumorigenesis
#17
Takashi Kawahara, Satoshi Inoue, Eiji Kashiwagi, Jinbo Chen, Hiroki Ide, Taichi Mizushima, Yi Li, Yichun Zheng, Hiroshi Miyamoto
Emerging preclinical evidence suggests the critical role of androgen-mediated androgen receptor (AR) signals in the development of bladder cancer. However, little is known about the efficacy of enzalutamide, an AR signaling inhibitor, in androgen-induced urothelial tumorigenesis. We therefore aimed to assess the effects of enzalutamide on neoplastic transformation of urothelial cells. An immortalized normal urothelial cell line SVHUC stably expressing wild-type AR (SVHUC-AR) was exposed to a chemical carcinogen 3-methylcholanthrene (MCA) to induce neoplastic transformation, and subsequently cultured for 6 weeks in the presence of anti-androgens, including enzalutamide, hydroxyflutamide, and bicalutamide...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/29117897/exploring-the-tetrahydroisoquinoline-thiohydantoin-scaffold-blockade-the-androgen-receptor-as-potent-anti-prostate-cancer-agents
#18
Xi Xu, Raoling Ge, Lei Li, Jubo Wang, Xiaoyu Lu, Siqi Xue, Xijing Chen, Zhiyu Li, Jinlei Bian
Prostate cancer (PC) is a major cause of cancer-related male death in worldwide and the identification of new and improved potent anti-PC molecules is constantly required. A novel scaffold of tetrahydroisoquinoline thiohydantoin was rationally designed based on the enzalutamide structures and our pre-work, leading to the discovery of a series of new antiproliferative compounds. Several new analogues displayed improved androgen receptor (AR) antagonistic activity, while maintaining the higher selective toxicity toward LNCaP cells (AR-rich) versus DU145 cells (AR-deficient) compared to enzalutamide...
October 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29110971/the-effects-of-enzalutamide-and-abiraterone-on-skeletal-related-events-and-bone-radiological-progression-free-survival-in-castration-resistant-prostate-cancer-patients-an-indirect-comparison-of-randomized-controlled-trials
#19
REVIEW
Sergio Rizzo, Antonio Galvano, Francesco Pantano, Michele Iuliani, Bruno Vincenzi, Francesco Passiglia, Silvia Spoto, Giuseppe Tonini, Viviana Bazan, Antonio Russo, Daniele Santini
Two new drugs, the CYP17 inhibitor abiraterone acetate and the androgen receptor (AR) antagonist enzalutamide, have recently shown to prolong OS prior chemotherapy or in docetaxel treated mCRPC patients, using steroidal therapy or placebo as control group. Updated analyses underlined the role of these new agents on two prostate-specific endpoints as radiographic progression-free survival (rPFS) and time to first skeletal-related event (tSRE). On the basis of these reports, we made an indirect comparison between abiraterone and enzalutamide...
October 16, 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/29110617/degradation-of-androgen-receptor-through-small-molecules-for-prostate-cancer
#20
Raoling Ge, Xi Xu, Pengfei Xu, Lei Li, Zhiyu Li, Jinlei Bian
Prostate cancer is the most common carcinoma among aged males in western countries and more aggressive and lethal castration resistant prostate cancer often occurs after androgen deprivation therapy. The high expression of androgens and androgen receptor is closely related to prostate cancer. Efficient androgen receptor antagonists, such as enzalutamide and ARN-509, could be employed as potent anti-prostate cancer agents. Nevertheless, recent studies have revealed that F876L mutation in androgen receptor converts the action of enzalutamide and ARN-509 from an antagonist to agonist, so that novel strategies are urgent to address this resistance mechanism...
November 6, 2017: Current Cancer Drug Targets
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