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Enzalutamide

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https://www.readbyqxmd.com/read/28228262/targeting-dna-damage-response-in-prostate-cancer-by-inhibiting-androgen-receptor-cdc6-atr-chk1-signaling
#1
Styliani Karanika, Theodoros Karantanos, Likun Li, Jianxiang Wang, Sanghee Park, Guang Yang, Xuemei Zuo, Jian H Song, Sankar N Maity, Ganiraju C Manyam, Bradley Broom, Ana M Aparicio, Gary E Gallick, Patricia Troncoso, Paul G Corn, Nora Navone, Wei Zhang, Shuhua Li, Timothy C Thompson
Cell division cycle 6 (CDC6), an androgen receptor (AR) target gene, is implicated in regulating DNA replication and checkpoint mechanisms. CDC6 expression is increased during prostate cancer (PCa) progression and positively correlates with AR in PCa tissues. AR or CDC6 knockdown, together with AZD7762, a Chk1/2 inhibitor, results in decreased TopBP1-ATR-Chk1 signaling and markedly increased ataxia-telangiectasia-mutated (ATM) phosphorylation, a biomarker of DNA damage, and synergistically increases treatment efficacy...
February 21, 2017: Cell Reports
https://www.readbyqxmd.com/read/28223364/protein-kinase-c-regulates-twist1-expression-via-nf-%C3%AE%C2%BAb-in-prostate-cancer
#2
Masaki Shiota, Akira Yokomizo, Ario Takeuchi, Eiji Kashiwagi, Takashi Dejima, Junichi Inokuchi, Katsunori Tatsugami, Takeshi Uchiumi, Masatoshi Eto
The progression of prostate cancer to metastatic and castration-resistant disease represents a critical step. We previously showed that protein kinase C (PKC) activation followed by Twist1 and androgen receptor (AR) induction played a critical role in castration resistance, but the precise molecular mechanism remains unknown. This study aimed to elucidate the relevant molecular mechanism, focusing on NF-κB transcription factor. We examined the activity of NF-κB after PKC inhibition, and the expression of Twist1 and AR after inhibition of NF-κB in human prostate cancer cells...
February 21, 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28219796/simultaneous-quantitation-of-abiraterone-enzalutamide-n-desmethyl-enzalutamide-and-bicalutamide-in-human-plasma-by-lc-ms-ms
#3
Kyu-Pyo Kim, Robert A Parise, Julianne L Holleran, Lionel D Lewis, Leonard Appleman, Nielka van Erp, Michael J Morris, Jan H Beumer
Inhibiting the androgen receptor (AR) pathway is an important clinical strategy in metastatic prostate cancer. Novel agents including abiraterone acetate and enzalutamide have been shown to prolong life in men with metastatic, castration-resistant prostate cancer (mCRPC). To evaluate the pharmacokinetics of AR-targeted agents, we developed and validated an LC-MS/MS assay for the quantitation of enzalutamide, N-desmethyl enzalutamide, abiraterone and bicalutamide in 0.05mL human plasma. After protein precipitation, chromatographic separation was achieved with a Phenomenex Synergi Polar-RP column and a linear gradient of 0...
February 13, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28216075/-androgen-receptors-in-breast-cancer-expression-value-and-therapeutic-prospects
#4
REVIEW
Delphine Héquet, Slim Mzoughi, Roman Rouzier, Ernesto Guccione
Triple-negative (TN) breast cancer are characterized by lack of estrogen receptor (OR) and progesterone receptor (PR) expression, and the absence of overexpression of human epidermal growth factor receptor 2 (HER2). It is a heterogeneous group of tumors with a more pejorative prognosis than other subtypes of breast cancer. Androgen receptors (AR) are nuclear receptors whose expression varies from 80 to 85% of primary breast cancers and 60 to 75% of metastatic cancers. Among the TN breast cancers, the luminal androgen receptor (LAR) subtype expresses AR more frequently, up to 53% of the cases...
February 16, 2017: Bulletin du Cancer
https://www.readbyqxmd.com/read/28209757/cdk4-6-therapeutic-intervention-and-viable-alternative-to-taxanes-in-crpc
#5
James P Stice, Suzanne E Wardell, John D Norris, Alexander P Yllanes, Holly M Alley, Victoria O Haney, Hannah S White, Rachid Safi, Peter S Winter, Kimberly J Cocce, Rigel J Kishton, Scott A Lawrence, Jay C Strum, Donald P McDonnell
: Resistance to second generation AR antagonists and CYP17 inhibitors in patients with castrationresistant prostate cancer (CRPC) develops rapidly through reactivation of the androgen signaling axis and has been attributed to androgen receptor (AR) overexpression, production of constitutively active AR splice variants, or the selection for AR mutants with altered ligand binding specificity. It has been established that androgens induce cell cycle progression, in part, through upregulation of cyclin D1 (CCND1) expression and subsequent activation of cyclin-dependent kinases 4 and 6 (CDK4/6)...
February 16, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28208518/re-genomic-alterations-in-cell-free-dna-and-enzalutamide-resistance-in-castration-resistant-prostate-cancer
#6
Samir S Taneja
No abstract text is available yet for this article.
March 2017: Journal of Urology
https://www.readbyqxmd.com/read/28191869/aberrant-corticosteroid-metabolism-in-tumor-cells-enables-gr-takeover-in-enzalutamide-resistant-prostate-cancer
#7
Jianneng Li, Mohammad Alyamani, Ao Zhang, Kai-Hsiung Chang, Michael Berk, Zhenfei Li, Ziqi Zhu, Marianne Petro, Cristina Magi-Galluzzi, Mary-Ellen Taplin, Jorge A Garcia, Kevin Courtney, Eric A Klein, Nima Sharifi
Prostate cancer is driven by androgen stimulation of the androgen receptor (AR). The next-generation AR antagonist, enzalutamide, prolongs survival, but resistance and lethal disease eventually prevail. Emerging data suggest that the glucocorticoid receptor (GR) is upregulated in this context, stimulating expression of AR-target genes that permit continued growth despite AR blockade. However, countering this mechanism by administration of GR antagonists is problematic because GR is essential for life. We show that enzalutamide treatment in human models of prostate cancer and patient tissues is accompanied by a ubiquitin E3-ligase, AMFR, mediating loss of 11β-hydroxysteroid dehydrogenase-2 (11β-HSD2), which otherwise inactivates cortisol, sustaining tumor cortisol concentrations to stimulate GR and enzalutamide resistance...
February 13, 2017: ELife
https://www.readbyqxmd.com/read/28188090/independent-association-between-time-to-prostate-specific-antigen-psa-nadir-and-psa-progression-free-survival-in-patients-with-docetaxel-na%C3%A3-ve-metastatic-castration-resistant-prostate-cancer-receiving-abiraterone-acetate-but-not-enzalutamide
#8
Hideaki Miyake, Takuto Hara, Keita Tamura, Takayuki Sugiyama, Hiroshi Furuse, Seiichiro Ozono, Masato Fujisawa
PURPOSE: The objective of this study was to compare the prognostic effect of time to prostate-specific antigen (PSA) nadir (TTPN) after treatment with abiraterone acetate (AA) and enzalutamide (Enz) in patients with docetaxel-naïve, metastatic castration-resistant prostate cancer (mCRPC). METHODS: This study included a total of 297 consecutive patients with mCRPC, of whom 125 and 172 received AA and Enz, respectively, without previous treatment with docetaxel and subsequently achieved any degree of PSA reduction after the administration of either agent...
February 7, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/28183253/optimal-management-of-prostate-cancer-based-on-its-natural-clinical-history
#9
Gaetano Facchini, Francesco Perri, Gabriella Misso, Carmine D Aniello, Giuseppina Della Vittoria Scarpati, Sabrina Rossetti, Chiara Della Pepa, Salvatore Pisconti, Gerhard Unteregger, Alessia Cossu, Michele Caraglia, Massimiliano Berretta, Carla Cavaliere
Prostate cancer is the most common malignancy in males and, despite a marked improvement in diagnostic techniques, a not small percentage of prostate tumours is still diagnosed in advanced stage. It is now clear that prostate cancer passes through distinct phases during its natural history, starting from an initial phase, in which the disease has a locoregional extent, until a very late phase when it becomes refractory to hormone therapy. It is important to distinguish between local disease, in which tumor may be considered localized in the gland and a systemic disease characterized by high tumor burden and/or dissemination of circulating tumour cells...
February 8, 2017: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/28181296/molecular-dynamics-studies-on-the-enzalutamide-resistance-mechanisms-induced-by-androgen-receptor-mutations
#10
Hongli Liu, Lingyan Wang, Jiaqi Tian, Jiazhong Li, Huanxiang Liu
The second-generation antiandrogen enzalutamide, targeting androgen receptor (AR), was approved to treat castration resistant prostate cancer (CRPC) in 2012. Its resistance was observed when it was in the clinical research stage. AR mutation is the main factor of enzalutamide resistance. AR F876L and F876L_T877A mutations were reported to switch enzalutamide from AR antagonist to agonist, but W741C cannot. There are various mutations in the ligand binding domain of androgen receptor (AR LBD), such as L701H, W741L, H874Y, T877A and M895T, if these mutations can lead to drug resistance problem or not is not known...
February 9, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28174422/antarlides-f-h-new-members-of-the-antarlide-family-produced-by-streptomyces-sp-bb47
#11
Shun Saito, Takahiro Fujimaki, Watanalai Panbangred, Ryuichi Sawa, Yasuhiro Igarashi, Masaya Imoto
Castration-resistant prostate cancer (CRPC) is the most aggressive form of this disease. CRPC remains dependent on androgen receptor (AR) signaling. Therefore, a novel AR antagonist, enzalutamide, is used clinically for the treatment of men with metastatic CRPC. However, enzalutamide-resistant AR has appeared, and a new type of AR antagonist is desired. Previously, in the course of screening for a new type of AR antagonist, we isolated a series of compounds, designated antarlides A-E, that share a novel 22-membered-ring macrocyclic structure and are produced by Streptomyces sp...
February 8, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28171710/clinical-outcomes-and-survival-surrogacy-studies-of-prostate-specific-antigen-declines-following-enzalutamide-in-men-with-metastatic-castration-resistant-prostate-cancer-previously-treated-with-docetaxel
#12
Andrew J Armstrong, Fred Saad, De Phung, Carl Dmuchowski, Neal D Shore, Karim Fizazi, Mohammad Hirmand, David Forer, Howard I Scher, Johann De Bono
BACKGROUND: In the AFFIRM trial, enzalutamide significantly increased overall survival (OS) for men with metastatic castration-resistant prostate cancer (mCRPC) after chemotherapy versus placebo and significantly decreased prostate-specific antigen (PSA) levels. The goal of this post hoc analysis was to associate levels of PSA decline from baseline after enzalutamide with clinical outcomes in the postchemotherapy mCRPC setting. METHODS: Men in the AFFIRM trial (n = 1199) were grouped by maximal PSA decline in the first 90 days of treatment...
February 7, 2017: Cancer
https://www.readbyqxmd.com/read/28151719/neoadjuvant-enzalutamide-prior-to-prostatectomy
#13
Bruce Montgomery, Maria S Tretiakova, Anthony Michael Joshua, Martin E Gleave, Neil Fleshner, Glenn J Bubley, Elahe A Mostaghel, Kim N Chi, Daniel Lin, Martin Sanda, William Novotny, Kenneth Wu, Philip W Kantoff, Brett Marck, Steve Plymate, Steven P Balk, Peter S Nelson, Alvin M Matsumoto, Rosina T Lis, Adam Kibel, Gabriel P Haas, Andrew Krivoshik, Alison Hannah, Mary-Ellen Taplin
PURPOSE: Prostate cancer is dependent on androgen receptor (AR) activation. Optimal AR antagonism may effectively cytoreduce local disease and suppress or eliminate micrometastases. We evaluated neoadjuvant therapy prior to prostatectomy with the potent AR antagonist enzalutamide (enza) either alone or in combination with dutasteride and leuprolide (enza/dut/LHRHa). EXPERIMENTAL DESIGN: Forty-eight of 52 men with intermediate or high-risk localized prostate cancer proceeded to prostatectomy after neoadjuvant enza or enza/dut/LHRHa for 6 months...
November 9, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28147927/a-case-report-of-enzalutamide-administration-in-a-dialysis-dependent-patient-with-castration-resistant-prostate-cancer
#14
Erica S Tsang, Marie de Haan, Bernhard J Eigl
Enzalutamide, an androgen receptor signaling inhibitor, is a standard of care treatment for metastatic castration-resistant prostate cancer. We present the first reported case of enzalutamide in a patient with end-stage renal disease, on dialysis. While there were no significant toxicities, a sustained increase in systolic blood pressure was maintained after starting enzalutamide, suggestive of a degree of drug accumulation. Further evaluation of novel hormonal agents in end-stage renal disease patients should be encouraged as this population is typically excluded from clinical trials...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28144973/minnelide-inhibits-androgen-dependent-castration-resistant-prostate-cancer-growth-by-decreasing-expression-of-androgen-receptor-full-length-and-splice-variants
#15
Sumit Isharwal, Shrey Modi, Nivedita Arora, Charles Uhlrich, Bhuwan Giri, Usman Barlass, Ayman Soubra, Rohit Chugh, Scott M Dehm, Vikas Dudeja, Ashok Saluja, Sulagna Banerjee, Badrinath Konety
BACKGROUND: With almost 30,000 deaths per year, prostate cancer is the second-leading cause of cancer-related death in men. Androgen Deprivation Therapy (ADT) has been the corner stone of prostate cancer treatment for decades. However, despite an initial response of prostate cancer to ADT, this eventually fails and the tumors recur, resulting in Castration Resistant Prostate Cancer (CRPC). Triptolide, a diterpene triepoxide, has been tested for its anti-tumor properties in a number of cancers for over a decade...
February 1, 2017: Prostate
https://www.readbyqxmd.com/read/28126272/prostate-specific-antigen-response-in-black-and-white-patients-treated-with-abiraterone-acetate-for-metastatic-castrate-resistant-prostate-cancer
#16
Sundhar Ramalingam, Michael S Humeniuk, Rachel Hu, Julia Rasmussen, Patrick Healy, Yuan Wu, Michael R Harrison, Andrew J Armstrong, Daniel J George, Tian Zhang
PURPOSE: Evidence suggests differences in androgen receptor AR signaling between black (B) and white (W) patients with prostate cancer, but pivotal trials of abiraterone acetate (AA) for patients with metastatic castration-resistant prostate cancer (mCRPC) enrolled few black patients, a population with a higher mortality from prostate cancer. Our primary objective was to determine differences in response to AA between B and W patients. METHODS: We performed a retrospective case-control study of B vs...
January 23, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/28125362/duration-of-treatment-in-prostate-cancer-patients-treated-with-abiraterone-acetate-or-enzalutamide
#17
Dominic Pilon, Ajay S Behl, Lorie A Ellis, Bruno Emond, Patrick Lefebvre, Nancy A Dawson
BACKGROUND: Abiraterone acetate (AA) and enzalutamide (ENZ) are oral therapies offering survival benefit to metastatic castration-resistant prostate cancer (mCRPC) patients. Despite the availability of multiple treatment options for mCRPC, there is a lack of information on the effect that being initiated on AA or ENZ has on the combined prostate cancer treatment duration. OBJECTIVE: To compare the combined duration of prostate cancer treatments of patients initiated on AA with that of patients initiated on ENZ...
February 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28123517/role-of-free-testosterone-levels-in-patients-with-metastatic-castration-resistant-prostate-cancer-receiving-second-line-therapy
#18
Christoph A von Klot, Markus A Kuczyk, Alena Boeker, Christoph Reuter, Florian Imkamp, Thomas R W Herrmann, Hossein Tezval, Mario W Kramer, Sven Perner, Axel S Merseburger
A range of new treatment options has recently become available for patients with advanced metastatic castration-resistant prostate cancer (mCRPC). Androgen deprivation therapy (ADT) with luteinizing hormone-releasing hormone is continued when performing chemotherapy or androgen deprivation with new second-generation therapeutic agents such as enzalutamide or abiraterone acetate. Despite the fact that free testosterone (FT) is the biologically active form, it is common practice that androgen suppression is monitored via total testosterone levels only...
January 2017: Oncology Letters
https://www.readbyqxmd.com/read/28117849/cardiovascular-toxicities-of-systemic-treatments-of-prostate-cancer
#19
REVIEW
Antonello Veccia, Francesca Maines, Stefania Kinspergher, Enzo Galligioni, Orazio Caffo
Prostate cancer is the most common cancer in men, with an incidence that is expected to increase in the coming years. Prostate cancer is usually diagnosed in men >65 years of age, thus the concurrent presence of cardiovascular diseases might influence the treatment, owing to the increased risk of cardiovascular mortality. The introduction of new drugs, such as abiraterone and enzalutamide for the management of metastatic disease has created further interest in treatment-related cardiovascular toxicities, although limited data from trials specifically designed to identify cardiovascular toxicities of these agents are currently available...
January 24, 2017: Nature Reviews. Urology
https://www.readbyqxmd.com/read/28117385/radiographic-progression-with-nonrising-psa-in-metastatic-castration-resistant-prostate-cancer-post-hoc-analysis-of-prevail
#20
A H Bryce, J J Alumkal, A Armstrong, C S Higano, P Iversen, C N Sternberg, D Rathkopf, Y Loriot, J de Bono, B Tombal, S Abhyankar, P Lin, A Krivoshik, D Phung, T M Beer
BACKGROUND: Advanced prostate cancer is a phenotypically diverse disease that evolves through multiple clinical courses. PSA level is the most widely used parameter for disease monitoring, but it has well-recognized limitations. Unlike in clinical trials, in practice, clinicians may rely on PSA monitoring alone to determine disease status on therapy. This approach has not been adequately tested. METHODS: Chemotherapy-naive asymptomatic or mildly symptomatic men (n=872) with metastatic castration-resistant prostate cancer (mCRPC) who were treated with the androgen receptor inhibitor enzalutamide in the PREVAIL study were analyzed post hoc for rising versus nonrising PSA (empirically defined as >1...
January 24, 2017: Prostate Cancer and Prostatic Diseases
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