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https://www.readbyqxmd.com/read/28192078/the-pressure-temperature-phase-diagram-of-metacetamol-and-its-comparison-to-the-phase-diagram-of-paracetamol
#1
M Barrio, J Huguet, I B Rietveld, B Robert, R Céolin, J Ll Tamarit
Understanding the polymorphic behavior of active pharmaceutical ingredients is important for formulation purposes and regulatory reasons. Metacetamol is an isomer of paracetamol and it similarly exhibits polymorphism. In the present paper, it has been found that one of the polymorphs of metacetamol is only stable under increased pressure, which has led to the conclusion that metacetamol like paracetamol is a monotropic system under ordinary (= laboratory) conditions and that it becomes enantiotropic under pressure with the I-II-L triple point coordinates for metacetamol TI-II-L = 535±10 K and PI-II-L = 692±70 MPa...
February 9, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28190764/bicalutamide-with-radiotherapy-for-prostate-cancer
#2
Vicki Brower
No abstract text is available yet for this article.
February 9, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28162857/design-synthesis-and-biological-evaluation-of-2-4-phenylthiazol-2-yl-isoindoline-1-3-dione-derivatives-as-anti-prostate-cancer-agents
#3
K Saravanan, R Elancheran, S Divakar, S Athavan Alias Anand, M Ramanathan, Jibon Kotoky, N K Lokanath, S Kabilan
The structural modification and molecular docking-based screening approaches on thiazole-based isoindolinediones were imposed to find the novel 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives. The best fit compounds (6a-n) were synthesized and evaluated their antiproliferative activities on the prostate cancer cell lines (PC-3 & LNCaP). Among them, the compound, 6m exhibited good activity, particularly on LNCaP (IC50=5.96±1.6μM), moderately active against PC-3 cell lines as compared to bicalutamide...
January 25, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28146658/radiation-with-or-without-antiandrogen-therapy-in-recurrent-prostate-cancer
#4
RANDOMIZED CONTROLLED TRIAL
William U Shipley, Wendy Seiferheld, Himanshu R Lukka, Pierre P Major, Niall M Heney, David J Grignon, Oliver Sartor, Maltibehn P Patel, Jean-Paul Bahary, Anthony L Zietman, Thomas M Pisansky, Kenneth L Zeitzer, Colleen A F Lawton, Felix Y Feng, Richard D Lovett, Alexander G Balogh, Luis Souhami, Seth A Rosenthal, Kevin J Kerlin, James J Dignam, Stephanie L Pugh, Howard M Sandler
Background Salvage radiation therapy is often necessary in men who have undergone radical prostatectomy and have evidence of prostate-cancer recurrence signaled by a persistently or recurrently elevated prostate-specific antigen (PSA) level. Whether antiandrogen therapy with radiation therapy will further improve cancer control and prolong overall survival is unknown. Methods In a double-blind, placebo-controlled trial conducted from 1998 through 2003, we assigned 760 eligible patients who had undergone prostatectomy with a lymphadenectomy and had disease, as assessed on pathological testing, with a tumor stage of T2 (confined to the prostate but with a positive surgical margin) or T3 (with histologic extension beyond the prostatic capsule), no nodal involvement, and a detectable PSA level of 0...
2, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28133135/-a-case-of-synchronous-vp3-hepatocellular-carcinoma-and-prostate-cancer-accompanied-by-bone-metastases
#5
Hirotoshi Maruo, Yukio Usui
A 58-year-old man visited our hospital with a chief complaint of epigastric pain. Computed tomography of the abdomen revealed a tumor in the left lobe of the liver accompanied by portal vein tumor thrombus, and Vp3 hepatocellular carcinoma was diagnosed. Prostate cancer with multiple bone metastases was also identified, and synchronous double cancer of the prostate and liver was diagnosed. The treatment strategy was to prioritize surgery for the hepatocellular carcinoma, for which curative resection was becomingnearly impossible...
November 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28105499/cx4945-suppresses-the-growth-of-castration-resistant-prostate-cancer-cells-by-reducing-ar-v7-expression
#6
Chuangzhong Deng, Jieping Chen, Shengjie Guo, Yanjun Wang, Qianghua Zhou, Zaishang Li, Xingping Yang, Xingsu Yu, Zhenfeng Zhang, Fangjian Zhou, Hui Han, Kai Yao
PURPOSE: The aberrant expression of casein kinase 2 (CK2) has been reported to be involved in the tumorigenesis and progression of prostate cancer. The inhibition of CK2 activity represses androgen-dependent prostate cancer cells by attenuating the androgen receptor (AR) signaling pathway. In this study, we examined the effect of CK2 inhibition in castration-resistant prostate cancer (CRPC) cells, in which AR variants (ARVs) play a predominant role. METHODS: A newly synthetic CK2 selective inhibitor CX4945 was utilized to study the effect of CK2 inhibition in CRPC cells by CCK8 assay and colony formation assay...
January 19, 2017: World Journal of Urology
https://www.readbyqxmd.com/read/28086774/androgenic-effects-of-aqueous-and-methanolic-extracts-of-ficus-asperifolia-in-male-wistar-rats
#7
Pierre Watcho, Hermine Meli Watio, Modeste Wankeu-Nya, Esther Ngadjui, Patrick Deeh Defo, Pepin Alango Nkeng-Efouet, Telesphore Benoit Nguelefack, Albert Kamanyi
BACKGROUND: Androgen deficiency is a clinical syndrome resulting from the inability of the testes to produce physiological levels of testosterone due to a disturbance occurring at one or more levels of the hypothalamic-pituitary-testicular axis. The present study was undertaken to evaluate the androgenic properties of aqueous and methanolic extracts of Ficus asperifolia on normal and castrated immature rats. METHODS: Normal rats were treated either per os with aqueous or methanolic extract of Ficus asperifolia (100 mg/kg or 500 mg/kg b...
January 13, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28063195/first-line-non-cytotoxic-therapy-in-chemotherapy-naive-patients-with-metastatic-castration-resistant-prostate-cancer-a-systematic-review-of-ten-randomised-clinical-trials
#8
REVIEW
Michiel H F Poorthuis, Robin W M Vernooij, R Jeroen A van Moorselaar, Theo M de Reijke
OBJECTIVE: To systematically evaluate all available treatment options in chemotherapy-naive patients with metastatic castration-resistant prostate cancer (mCRPC). METHODS: We systematically searched PubMed, EMBASE, and the Cochrane libraries up to March 1, 2016 for peer-reviewed publications on randomised clinical trials (RCTs). RCTs were included if progression-free survival (PFS), overall survival (OS), quality of life (QoL), or adverse events (AEs) were quantitatively evaluated...
January 6, 2017: BJU International
https://www.readbyqxmd.com/read/28034074/does-enzalutamide-really-reduce-the-risk-of-progression-compared-with-bicalutamide-in-patients-with-castration-resistant-prostate-cancer
#9
Mehmet Ali Nahit Şendur, Bülent Yalçın
No abstract text is available yet for this article.
January 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28034067/enzalutamide-versus-bicalutamide-in-castration-resistant-prostate-cancer-the-strive-trial-there-is-no-significant-reduction-in-death-yet
#10
Jorg Michels
No abstract text is available yet for this article.
January 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28011482/galectin-3-is-implicated-in-tumor-progression-and-resistance-to-anti-androgen-drug-through-regulation-of-androgen-receptor-signaling-in-prostate-cancer
#11
Tsogt-Ochir Dondoo, Tomoharu Fukumori, Kei Daizumoto, Tomoya Fukawa, Miho Kohzuki, Minoru Kowada, Yoshito Kusuhara, Hidehisa Mori, Hiroyoshi Nakatsuji, Masayuki Takahashi, Hiro-Omi Kanayama
BACKGROUND: Castration-resistant prostate cancer (CRPC)-related deaths are increasing worldwide. Therefore, clarification of the mechanisms of hormone-related tumor progression and resistance to anti-androgen drugs is useful in order to develop strategies for appropriate treatment of CRPC. Galectin-3 has been shown to be correlated with tumor progression in a variety of cancer types through the regulation of tumor proliferation, angiogenesis, and apoptosis. MATERIALS AND METHODS: We examined tumor cell invasion and migration using the xCELLigence system...
2017: Anticancer Research
https://www.readbyqxmd.com/read/27994514/the-correlation-between-parp1-and-brca1-in-ar-positive-triple-negative-breast-cancer
#12
Jiayan Luo, Juan Jin, Fang Yang, Zijia Sun, Wenwen Zhang, Yaqin Shi, Jing Xu, Xiaoxiang Guan
Triple-negative breast cancer (TNBC) lacks estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER-2) expression and thus cannot benefit from conventional hormonal or anti-HER2 targeted therapies. Anti-androgen therapy has shown a certain effect on androgen receptor (AR) positive TNBC. The emerging researches have proved that poly (ADP-ribose) polymerase (PARP) inhibitor is effective in BRCA1-deficient breast cancers. We demonstrated that combination of AR antagonist (bicalutamide) and PARP inhibitor (ABT-888) could inhibit cell viability and induce cell apoptosis significantly whatever in vitro or in vivo setting in AR-positive TNBC...
2016: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/27987794/bioflavonoid-hesperetin-overcome-bicalutamide-induced-toxicity-by-co-delivery-in-novel-snedds-formulations-optimization-in-vivo-evaluation-and-uptake-mechanism
#13
Abhishek Arya, Hafsa Ahmad, Sachin Tulsankar, Satish Agrawal, Naresh Mittapelly, Rajkumar Boda, Rabi S Bhatta, Kalyan Mitra, Anil K Dwivedi
In the present study, we designed Bicalutamide (BCT) and Hesperetin (HSP) co-loaded self nano-emulsifying drug delivery system (SNEDDS) to encounter the problem of BCT induced toxicity, low solubility, and bioavailability. Optimized BCT-HSP SNEDDS would produce an emulsion of globule size 30.84±1.24nm with a high encapsulation efficiency of BCT (91.29%) and HSP (88.19%), and showed rapid drug release. DPPH assay confirmed the retention of antioxidant potential of HSP in SNEDDS. DCFH-DA confirmed intense green fluorescence in HSP treated groups due to the generation of reactive oxygen species...
February 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27979508/re-efficacy-and-safety-of-enzalutamide-versus-bicalutamide-for-patients-with-metastatic-prostate-cancer-terrain-a-randomised-double-blind-phase-2-study
#14
https://www.readbyqxmd.com/read/27943566/impact-of-androgen-deprivation-therapy-on-volume-reduction-and-lower-urinary-tract-symptoms-in-patients-with-prostate-cancer
#15
Satoshi Washino, Masaru Hirai, Kimitoshi Saito, Yutaka Kobayashi, Yoshiaki Arai, Tomoaki Miyagawa
OBJECTIVE: To evaluate the impact of androgen deprivation therapy (ADT) on prostate volume, lower urinary tract symptoms (LUTS), and LUTS-related quality of life (QOL) in patients with prostate cancer. METHODS: Patients with prostate cancer (PCa) were treated with goserelin and bicalutamide for 24 weeks. Changes in the total prostate volume (TPV), International Prostate Symptom Score (IPSS), and QOL score for urinary symptoms were assessed every 12 weeks. Of the 42 patients enrolled, 8 patients withdrew and 2 were excluded, so 32 patients were analyzed...
December 12, 2016: Lower Urinary Tract Symptoms
https://www.readbyqxmd.com/read/27942507/impact-of-enzalutamide-on-patient-related-outcomes-in-metastatic-castration-resistant-prostate-cancer-current-perspectives
#16
REVIEW
Jia Luo, Julie N Graff
Prostate cancer claims the lives of more than 25,000 men in the United States yearly, most from metastatic disease. In the past decade, several new medications have been approved for the treatment of metastatic prostate cancer including the antiandrogen enzalutamide. In addition, there has been mounting interest in evaluating health-related quality of life (QoL) in patients with cancer including new more detailed recommendations released by the Prostate Cancer Working Group 3 on how to evaluate patient-related outcomes in clinical trials...
2016: Research and Reports in Urology
https://www.readbyqxmd.com/read/27919966/multimodal-primary-treatment-of-metastatic-prostate-cancer-with-androgen-deprivation-and-radiation
#17
Timo Joensuu, Greetta Joensuu, Kalevi Kairemo, Timo Kiljunen, Maigo Riener, Aili Aaltonen, Martti Ala-Opas, Aki Kangasmäki, Tuomo Alanko, Lauri Taipale, Petteri Hervonen, Anna Bützow, Irene Virgolini, Akseli Hemminki
AIM: We combined anti-androgen therapy with radiotherapy in a first-line setting for metastatic prostate cancer aiming to cause maximal cancer-cell death to delay the emergence of castration-resistant disease. MATERIALS AND METHODS: In this non-randomized retrospective series of 46 patients, the initial median prostate-specific antigen (PSA) was 98.5 μg/l (range=6.7-15,500), median Gleason score 9 and most men had at least T3N1M1 disease. All patients received luteinizing hormone releasing hormone analog or degarelix with bicalutamide...
2016: Anticancer Research
https://www.readbyqxmd.com/read/27870564/risk-associated-with-high-dose-bicalutamide
#18
Charles G Drake
No abstract text is available yet for this article.
February 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/27848066/molecular-mechanism-of-r-bicalutamide-switching-from-androgen-receptor-antagonist-to-agonist-induced-by-amino-acid-mutations-using-molecular-dynamics-simulations-and-free-energy-calculation
#19
Hongli Liu, Rui Han, Jiazhong Li, Huanxiang Liu, Lifang Zheng
R-bicalutamide, a first generation antiandrogen, was used to treat prostate cancer for decades. Although it is very effective at the beginning, resistance appears after 2-3 years of treatment. Mutation of androgen receptor (AR) is considered a main reason for drug resistance. It is reported that AR W741C, W741L, W741C_T877A, T877A, F876L, F876L_T877A and L701H mutations can convert R-bicalutamide from AR antagonist to agonist, but the switching mechanisms are not clear. In this study, molecular dynamics simulations and molecular mechanics generalized Born surface area (MM-GBSA) calculations were performed to analyze the interaction mechanisms between R-bicalutamide and wild type/mutant ARs...
December 2016: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/27771244/a-study-of-combination-bicalutamide-and-raloxifene-for-patients-with-castration-resistant-prostate-cancer
#20
Thai H Ho, Rafael Nunez-Nateras, Yue-Xian Hou, Alan H Bryce, Donald W Northfelt, Amylou C Dueck, Bryan Wong, Melissa L Stanton, Richard W Joseph, Erik P Castle
BACKGROUND: Prostate tissue expresses 2 estrogen receptor (ER) isoforms, ER-α and ER-β, and estrogen-based therapies have shown activity in preclinical studies. Raloxifene, a selective ER modulator, has inhibited the growth of prostate cancer xenograft models and was tested in a phase II trial of castration-resistant prostate cancer (CRPC), with some patients achieving stable disease. However, no studies have examined the safety of the combination of bicalutamide plus raloxifene for CRPC...
September 8, 2016: Clinical Genitourinary Cancer
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