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https://www.readbyqxmd.com/read/28636139/review-of-hplc-and-lc-ms-ms-assays-for-the-determination-of-various-non-steroidal-anti-androgens-nsaa-used-in-the-treatment-of-prostate-cancer
#1
REVIEW
P S Suresh, Nuggehally R Srinivas, Ramesh Mullangi
Prostate cancer is the most common cancer and one of the leading causes for cancer deaths in men. One of the commonly used approaches to treat metastatic prostate cancer was via first generation non-steroidal anti-androgens (NSAA) namely flutamide, nilutamide, bicalutamide and topilutamide. Most of the prostate cancer patients who are initially responsive develop a most aggressive form of disease called castration-resistant prostate cancer (CRPC). Second generation NSAA receptor antagonists (enzalutamide, apalutamide and darolutamide) are emerging as additional new options to treat CRPC...
June 21, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28626511/assessment-of-real-world-central-nervous-system-events-in-patients-with-advanced-prostate-cancer-using-abiraterone-acetate-bicalutamide-enzalutamide-or-chemotherapy
#2
Dominic Pilon, Ajay S Behl, Lorie A Ellis, Marie-Noëlle Robitaille, Patrick Lefebvre, Nancy A Dawson
BACKGROUND: Central nervous system (CNS) events are frequently reported among patients with advanced prostate cancer as a consequence of the treatments used in this patient population. OBJECTIVE: To assess the incidence of CNS events in patients with advanced prostate cancer who initiated treatment with abiraterone acetate, bicalutamide, enzalutamide, or chemotherapy. METHODS: The Truven Health MarketScan Research databases were used to retrospectively identify patients with prostate cancer who initiated treatment with abiraterone acetate, enzalutamide, bicalutamide, or chemotherapy after September 1, 2012 (ie, the index date)...
May 2017: American Health & Drug Benefits
https://www.readbyqxmd.com/read/28607007/synergistic-activity-with-notch-inhibition-and-androgen-ablation-in-erg-positive-prostate-cancer-cells
#3
Ahmed A Mohamed, Shyh-Han Tan, Charles P Xavier, Shilpa Katta, Wei Huang, Lakshmi Ravindranath, Muhammad Jamal, Hua Li, Meera Srivastava, Eri S Srivatsan, Taduru L Sreenath, David G McLeod, Alagarsamy Srinivasan, Gyorgy Petrovics, Albert Dobi, Shiv Srivastava
The oncogenic activation of the ETS related gene (ERG) due to gene fusions is present in over half of prostate cancer (CaP) in Western countries. Due to its high incidence and oncogenic role, ERG and components of ERG network have emerged as potential drug targets for CaP. Utilizing gene expression datasets, from matched normal and prostate tumor epithelial cells, an association of NOTCH transcription factors with ERG expression status was identified; confirming that NOTCH factors are direct transcriptional targets of ERG...
June 12, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28571783/improving-the-physicochemical-properties-of-bicalutamide-by-complex-formation-with-bovine-serum-albumin
#4
Congbin Yang, Peiwen Di, JinPing Fu, Hui Xiong, Qiufang Jing, Guobin Ren, Yun Tang, Wenyun Zheng, Guixia Liu, Fuzheng Ren
Bicalutamide-bovine serum albumin (Bic-BSA) complexes were prepared by anti-solvent precipitation. Bovine serum albumin (BSA) was used as a stabilizer for particle growth. The physicochemical properties of Bic-BSA were analyzed by scanning electron microscopy, X-ray powder diffraction and differential scanning calorimetry. The interaction between Bic and BSA was characterized by Fourier transform infrared spectroscopy, Raman spectroscopy, fluorescence spectroscopy and molecular docking. The particle size could be easily reduced to 1-10μm with a good lognormal distribution...
May 29, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28562322/characterization-of-a-novel-androgen-receptor-ar-coregulator-ripk1-and-related-chemicals-that-suppress-ar-mediated-prostate-cancer-growth-via-peptide-and-chemical-screening
#5
Cheng-Lung Hsu, Jai-Shin Liu, Ting-Wei Lin, Ying-Hsu Chang, Yung-Chia Kuo, An-Chi Lin, Huei-Ju Ting, See-Tong Pang, Li-Yu Lee, Wen-Lung Ma, Chun-Cheng Lin, Wen-Guey Wu
Using bicalutamide-androgen receptor (AR) DNA binding domain-ligand binding domain as bait, we observed enrichment of FxxFY motif-containing peptides. Protein database searches revealed the presence of receptor-interacting protein kinase 1 (RIPK1) harboring one FxxFY motif. RIPK1 interacted directly with AR and suppressed AR transactivation in a dose-dependent manner. Domain mapping experiments showed that the FxxFY motif in RIPK1 is critical for interactions with AR and the death domain of RIPK1 plays a crucial role in its inhibitory effect on transactivation...
May 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28562037/computational-discovery-and-experimental-validation-of-inhibitors-of-the-human-intestinal-transporter-oatp2b1
#6
Natalia Khuri, Arik A Zur, Matthias B Wittwer, Lawrence Lin, Sook Wah Yee, Andrej Sali, Kathleen M Giacomini
Human organic anion transporters (OATPs) are vital for the uptake and efflux of drugs and endogenous compounds. Current identification of inhibitors of these transporters is based on experimental screening. Virtual screening remains a challenge due to a lack of experimental three-dimensional protein structures. Here, we describe a workflow to identify inhibitors of the OATP2B1 transporter in the DrugBank library of over 5,000 drugs and druglike molecules. OATP member 2B1 transporter is highly expressed in the intestine, where it participates in oral absorption of drugs...
June 15, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28552710/clinical-outcomes-and-testosterone-levels-following-continuous-androgen-deprivation-in-patients-with-relapsing-or-locally-advanced-prostate-cancer-a-post-hoc-analysis-of-the-iceland-study
#7
Bertrand Tombal, Erik B Cornel, Raj Persad, Anny Stari, Francisco Gómez Veiga, Claude Schulman
PURPOSE: Lower serum testosterone levels correlate with improved cause-specific survival and longer time to progression in the first year of continuous androgen deprivation in men with prostate cancer. ICELAND was a large, European study demonstrating the efficacy of leuprorelin (Eligard(®)) during continuous androgen deprivation. This post hoc analysis investigated serum testosterone levels within the first year of continuous androgen deprivation for survival and time to progression...
May 25, 2017: Journal of Urology
https://www.readbyqxmd.com/read/28512306/structure-based-docking-studies-towards-exploring-potential-anti-androgen-activity-of-selected-phytochemicals-against-prostate-cancer
#8
Anshika N Singh, Meghna M Baruah, Neeti Sharma
Prostate cancer (PCa) is the second most common malignancy amongst men worldwide. Under PCa maintenance therapy drugs acting as antagonists/partial agonists of hormone receptors against the prostate tissue are used in clinical practices. Prominent drugs being Cyproterone acetate, Flutamide, Bicalutamide, they not only cause acute and long-term toxicity, but also develops drug resistance among patients. Our focus has been on phytochemicals which do not exhibit any cytotoxicity and have significant androgen receptor (AR) inhibition activity...
May 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28500234/niclosamide-and-bicalutamide-combination-treatment-overcomes-enzalutamide-and-bicalutamide-resistant-prostate-cancer
#9
Chengfei Liu, Cameron M Armstrong, Wei Lou, Alan P Lombard, Vito Cucchiara, Xinwei Gu, Joy C Yang, Nagalakshmi Nadiminty, Chong-Xian Pan, Christopher P Evans, Allen C Gao
Activation of the androgen receptor (AR) and its splice variants is linked to advanced prostate cancer and drives resistance to antiandrogens. The roles of AR and AR variants in the development of resistance to androgen deprivation therapy (ADT) and bicalutamide treatment, however, are still incompletely understood. To determine whether AR variants play a role in bicalutamide resistance, we developed bicalutamide resistant LNCaP cells (LNCaP-BicR) and found that these resistant cells express significantly increased levels of AR variants, particularly AR-V7, both at the mRNA and protein levels...
May 12, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28444169/androgen-receptor-regulation-of-local-growth-hormone-in-prostate-cancer-cells
#10
M V Recouvreux, B Wu, A C Gao, S Zonis, V Chesnokova, N Bhowmick, L W Chung, S Melmed
Prostate cancer (PCa) growth is mainly driven by androgen receptor (AR), and tumors that initially respond to androgen deprivation therapy (ADT) or AR inhibition usually relapse into a more aggressive, castration resistant stage (CRPC). Circulating growth hormone (GH) has a permissive role in PCa development in animal models and in human PCa xenograft growth. As GH and GH receptor (GHR) are both expressed in PCa cells, we assessed whether prostatic GH production is linked to AR activity and whether GH contributes to the castration resistant phenotype...
April 21, 2017: Endocrinology
https://www.readbyqxmd.com/read/28403781/design-synthesis-and-biological-evaluation-of-novel-1-3-thiazolidine-2-4-diones-as-anti-prostate-cancer-agents
#11
Ramakrishnan Elancheran, Kuppusamy Saravanan, Selvaraj Divakar, Sima Kumari, V Lenin Maruthanila, Senthamarikannan Kabilan, Muthaiah Ramanathan, Rajlakshmi Devi, Jibon Kotoky
Androgen receptor (AR) is an attractive target for the treatment of prostate cancer. Structural modification and molecular docking-based virtual screening approaches were imposed to identify the novel 1,3-thiazolidine-2,4-diones (TZDs) by using Schrödinger (Maestro 9.5). The best fit molecules (3-12 & 23-31) were synthesized and characterized using spectroscopic techniques, then in vitro antioxidant and anti-prostate cancer activities were evaluated. Further, the structure of the intermediate (18) was confirmed by single crystal XRD analysis...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28394498/degarelix-versus-goserelin-plus-bicalutamide-in-the-short-term-relief-of-lower-urinary-tract-symptoms-in-prostate-cancer-patients-results-of-a-pooled-analysis
#12
Malcolm Mason, Pierre Richaud, Zsolt Bosnyak, Anders Malmberg, Anders Neijber
OBJECTIVE: In patients with prostate cancer (PCa), prostate enlargement may give rise to lower urinary tract symptoms (LUTS); many patients suffer from moderate-to-severe symptoms. We compare the efficacy of degarelix and goserelin plus bicalutamide in improving LUTS in PCa patients. METHODS: Data were pooled from three Phase 3, randomized clinical trials of once-monthly treatment for 12 weeks with degarelix (240/80 mg; n = 289) or goserelin (3.6 mg) plus bicalutamide (50 mg; n = 174) for initial flare protection...
May 2017: Lower Urinary Tract Symptoms
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
#13
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/28363855/planetary-ball-milling-and-supercritical-fluid-technology-as-a-way-to-enhance-dissolution-of-bicalutamide
#14
Joanna Szafraniec, Agata Antosik, Justyna Knapik-Kowalczuk, Mateusz Kurek, Karolina Syrek, Krzysztof Chmiel, Marian Paluch, Renata Jachowicz
Dissolution of bicalutamide processed with polyvinylpyrrolidone by either supercritical carbon dioxide or ball milling has been investigated. Various compositions as well as process parameters were used to obtain binary systems of the drug with the carrier. Thermal analysis and powder X-ray diffractometry confirmed amorphization of bicalutamide mechanically activated by ball milling and the decrease in crystallinity of the supercritical carbon dioxide-treated drug. Both methods led to reduction of particles size what was confirmed by scanning electron microscopy and laser diffraction measurements...
March 28, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28324044/inverse-regulation-of-dht-synthesis-enzymes-5%C3%AE-reductase-types-1-and-2-by-the-androgen-receptor-in-prostate-cancer
#15
Étienne Audet-Walsh, Tracey Yee, Ingrid S Tam, Vincent Giguère
5α-Reductase types 1 and 2, encoded by SRD5A1 and SRD5A2, are the two enzymes that can catalyze the conversion of testosterone to dihydrotestosterone, the most potent androgen receptor (AR) agonist in prostate cells. 5α-Reductase type 2 is the predominant isoform expressed in the normal prostate. However, its expression decreases during prostate cancer (PCa) progression, whereas SRD5A1 increases, and the mechanism underlying this transcriptional regulatory switch is still unknown. Interrogation of SRD5A messenger RNA expression in three publicly available data sets confirmed that SRD5A1 is increased in primary and metastatic PCa compared with nontumoral prostate tissues, whereas SRD5A2 is decreased...
April 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28323036/targeting-androgen-receptor-versus-targeting-androgens-to-suppress-castration-resistant-prostate-cancer
#16
Changcheng Guo, Shuyuan Yeh, Yuanjie Niu, Gonghui Li, Junhua Zheng, Lei Li, Chawnshang Chang
Prostate cancer (PCa) is the 2nd leading cause of cancer-related death among men in the United States and its progression is tightly associated with the androgen/androgen receptor (AR) signals. Men castrated before puberty (eunuchs) or men with inherited deficiency of type II 5α-reductase (with failure to convert testosterone to the more potent dihydrotestosterone) (DHT) do not develop PCa. To date, androgen deprivation therapy (ADT) with anti-androgen treatments to reduce or prevent androgens from binding to the AR remains the main therapeutic option for advanced PCa since its discovery by Huggins and Hodges in 1941...
July 1, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28319807/targeting-nf-kappa-b-signaling-by-artesunate-restores-sensitivity-of-castrate-resistant-prostate-cancer-cells-to-antiandrogens
#17
Jessica J Nunes, Swaroop K Pandey, Anjali Yadav, Sakshi Goel, Bushra Ateeq
Androgen deprivation therapy (ADT) is the most preferred treatment for men with metastatic prostate cancer (PCa). However, the disease eventually progresses and develops resistance to ADT in majority of the patients, leading to the emergence of metastatic castration-resistant prostate cancer (mCRPC). Here, we assessed artesunate (AS), an artemisinin derivative, for its anticancer properties and ability to alleviate resistance to androgen receptor (AR) antagonists. We have shown AS in combination with bicalutamide (Bic) attenuates the oncogenic properties of the castrate-resistant (PC3, 22RV1) and androgen-responsive (LNCaP) PCa cells...
April 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28293633/combined-ligand-structure-based-virtual-screening-and-molecular-dynamics-simulations-of-steroidal-androgen-receptor-antagonists
#18
Yuwei Wang, Rui Han, Huimin Zhang, Hongli Liu, Jiazhong Li, Huanxiang Liu, Paola Gramatica
The antiandrogens, such as bicalutamide, targeting the androgen receptor (AR), are the main endocrine therapies for prostate cancer (PCa). But as drug resistance to antiandrogens emerges in advanced PCa, there presents a high medical need for exploitation of novel AR antagonists. In this work, the relationships between the molecular structures and antiandrogenic activities of a series of 7α-substituted dihydrotestosterone derivatives were investigated. The proposed MLR model obtained high predictive ability...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28270124/cyproterone-acetate-enhances-trail-induced-androgen-independent-prostate-cancer-cell-apoptosis-via-up-regulation-of-death-receptor-5
#19
Linjie Chen, Dennis W Wolff, Yan Xie, Ming-Fong Lin, Yaping Tu
BACKGROUND: Virtually all prostate cancer deaths occur due to obtaining the castration-resistant phenotype after prostate cancer cells escaped from apoptosis and/or growth suppression initially induced by androgen receptor blockade. TNF-related apoptosis-inducing ligand (TRAIL) was an attractive cancer therapeutic agent due to its minimal toxicity to normal cells and remarkable apoptotic activity in tumor cells. However, most localized cancers including prostate cancer are resistant to TRAIL-induced apoptosis, thereby creating a therapeutic challenge of inducing TRAIL sensitivity in cancer cells...
March 7, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28231007/molecular-dynamics-recrystallization-behavior-and-water-solubility-of-the-amorphous-anticancer-agent-bicalutamide-and-its-polyvinylpyrrolidone-mixtures
#20
Justyna Szczurek, Marzena Rams-Baron, Justyna Knapik-Kowalczuk, Agata Antosik, Joanna Szafraniec, Witold Jamróz, Mateusz Dulski, Renata Jachowicz, Marian Paluch
In this paper, we investigated the molecular mobility and physical stability of amorphous bicalutamide, a poorly water-soluble drug widely used in prostate cancer treatment. Our broadband dielectric spectroscopy measurements and differential scanning calorimetry studies revealed that amorphous BIC is a moderately fragile material with a strong tendency to recrystallize from the amorphous state. However, mixing the drug with polymer polyvinylpyrrolidone results in a substantial improvement of physical stability attributed to the antiplasticizing effect governed by the polymer additive...
April 3, 2017: Molecular Pharmaceutics
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