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https://www.readbyqxmd.com/read/29216878/adaptive-phenotype-drives-resistance-to-androgen-deprivation-therapy-in-prostate-cancer
#1
Nicoletta Ferrari, Ilaria Granata, Matteo Capaia, Marina Piccirillo, Mario Rosario Guarracino, Roberta Venè, Antonella Brizzolara, Andrea Petretto, Elvira Inglese, Martina Morini, Simonetta Astigiano, Adriana Agnese Amaro, Francesco Boccardo, Cecilia Balbi, Paola Barboro
BACKGROUND: Prostate cancer (PCa), the second most common cancer affecting men worldwide, shows a broad spectrum of biological and clinical behaviour representing the epiphenomenon of an extreme heterogeneity. Androgen deprivation therapy is the mainstay of treatment for advanced forms but after few years the majority of patients progress to castration-resistant prostate cancer (CRPC), a lethal form that poses considerable therapeutic challenges. METHODS: Western blotting, immunocytochemistry, invasion and reporter assays, and in vivo studies were performed to characterize androgen resistant sublines phenotype in comparison to the parental cell line LNCaP...
December 8, 2017: Cell Communication and Signaling: CCS
https://www.readbyqxmd.com/read/29214142/molecular-mechanisms-of-enzalutamide-resistance-in-prostate-cancer
#2
REVIEW
Zoran Culig
Purpose of Review: Compensatory mechanisms leading to increased androgen receptor expression and activity after androgen ablation or anti-androgen treatment have been identified in prostate cancer. After hydroxyflutamide and bicalutamide were used in therapy of prostate cancer over many years, novel anti-androgen enzalutamide showed improved clinical activity. However, enzalutamide resistance develops over a certain time period, and molecular mechanisms responsible for this process are heterogeneous...
2017: Current Molecular Biology Reports
https://www.readbyqxmd.com/read/29212868/painful-testicular-metastasis-from-prostate-adenocarcinoma
#3
Karla A Lee, Erik Mayer, Vincent Khoo
A 60-year-old man presented with unilateral testicular pain and urinary frequency. His presenting prostate-specific antigen (PSA) was 100 ng/mL, and a biopsy revealed Gleason 4+4 prostate adenocarcinoma. The significance of his initial PSA was somewhat complicated by possible prostatitis and early initiation of bicalutamide. PSA rose on two occasions prior to radiotherapy but coincided with a flare of testicular pain on one of these. Whole-body staging diffusion-weighted MRI scan was negative. He was treated with 3 years of androgen deprivation therapy (ADT) and radical radiotherapy...
December 5, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/29211888/combined-oral-contraception-and-bicalutamide-in-polycystic-ovary-syndrome-and-severe-hirsutism-a-double-blind-rtc
#4
Costanzo Moretti, Laura Guccione, Paola Di Giacinto, Ilaria Simonelli, Caterina Exacoustos, Vincenzo Toscano, Cecilia Motta, Vincenzo De Leo, Felice Petraglia, Andrea Lenzi
Background: Hirsutism is frequently expressed in women affected by polycystic ovary syndrome (PCOS). The efficacy of oral contraceptive pill (OC) plus anti-androgens in the treatment of its severe expression is controversial due to the lack of randomized double-blind long-term studies. Aim: The primary outcome was the reduction of hirsutism in PCOS women objectively measured by videodermoscopy (VD) on the androgen-sensitive skin areas assessed by the modified Ferriman&Gallwey (mF&G) total score, after 12 months of therapy with OC+Bicalutamide (BC) versus OC plus placebo (P)...
December 1, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29211833/a-prospective-phase-ii-study-of-combined-androgen-blockade-in-patients-with-androgen-receptor-positive-metastatic-or-locally-advanced-unresectable-salivary-gland-carcinoma
#5
C Fushimi, Y Tada, H Takahashi, T Nagao, H Ojiri, T Masubuchi, T Matsuki, K Miura, D Kawakita, H Hirai, E Hoshino, S Kamata, T Saotome
Background: There is no standard first-line chemotherapy for recurrent/metastatic or unresectable locally advanced salivary gland carcinoma (SGC). Patients and methods: We conducted a single institution, open-label, single arm, phase II trial of combined androgen blockade (CAB) for androgen receptor (AR)-positive SGC. Leuprorelin acetate was administered subcutaneously at a dose of 3.75 mg every 4 weeks. Bicalutamide was administered orally at a daily dose of 80 mg...
December 1, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29194687/serum-free-complete-medium-an-alternative-medium-to-mimic-androgen-deprivation-in-human-prostate-cancer-cell-line-models
#6
Michael V Fiandalo, John H Wilton, Krystin M Mantione, Carol Wrzosek, Kristopher M Attwood, Yue Wu, James L Mohler
BACKGROUND: Almost all men who present with advanced prostate cancer (CaP) and some men who fail therapy for clinically localized CaP are treated with androgen deprivation therapy (ADT). CaP cell lines are used to identify and characterize new agents for ADT or investigate mechanisms of ADT resistance. CaP cell lines are maintained in culture medium that contains fetal bovine serum, which contains testosterone (T). Androgen deprivation experiments are performed using media supplemented with androgen-free serum, such as charcoal stripped fetal bovine serum (CS-FBS)...
December 1, 2017: Prostate
https://www.readbyqxmd.com/read/29155192/external-genital-development-urethra-formation-and-hypospadias-induction-in-guinea-pig-a-double-zipper-model-for-human-urethral-development
#7
Shanshan Wang, Mingxin Shi, Dongqing Zhu, Ranjiv Mathews, Zhengui Zheng
OBJECTIVES: To determine whether the guinea pig phallus would be an appropriate model of human penile development, we characterized the embryology and sexual differentiation of guinea pig external genitalia and attend to induce hypospadias in males and tubular urethra formation in females pharmacologically. MATERIALS AND METHODS: The external genitalia of guinea pig were collected from genital swelling initiation to newborn stages and Scanning Electronic Microscopy and histology were performed to visualize the morphology and structure...
November 16, 2017: Urology
https://www.readbyqxmd.com/read/29119053/enzalutamide-as-an-androgen-receptor-inhibitor-prevents-urothelial-tumorigenesis
#8
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/29118987/massive-adrenal-incidentalomas-and-late-diagnosis-of-congenital-adrenal-hyperplasia-in-prostate-cancer
#9
Xin Feng, Gregory Kline
In a 61-year-old Caucasian male with prostate cancer, leuprolide and bicalutamide failed to suppress the androgens. He presented to endocrinology with persistently normal testosterone and incidental massive (up to 18 cm) bilateral adrenal myelolipomas on CT scan. Blood test did not reveal metanephrine excess. The patient was noted to have short stature (151 cm) and primary infertility. Elementary school photographs demonstrated precocious puberty. Physical examination revealed palpable abdominal (adrenal) masses...
2017: Endocrinology, Diabetes & Metabolism Case Reports
https://www.readbyqxmd.com/read/29074061/anticancer-activity-and-tolerance-of-treatments-received-beyond-progression-in-men-treated-upfront-with-androgen-deprivation-therapy-with-or-without-docetaxel-for-metastatic-castration-na%C3%A3-ve-prostate-cancer-in-the-getug-afu-15-phase-3-trial
#10
Pernelle Lavaud, Gwenaëlle Gravis, Stéphanie Foulon, Florence Joly, Stéphane Oudard, Frank Priou, Igor Latorzeff, Loïc Mourey, Michel Soulié, Remy Delva, Ivan Krakowski, Brigitte Laguerre, Christine Théodore, Jean Marc Ferrero, Philippe Beuzeboc, Muriel Habibian, Frédéric Rolland, Gael Deplanque, Damien Pouessel, Sylvie Zanetta, Jean François Berdah, Jerome Dauba, Marjorie Baciuchka, Christian Platini, Claude Linassier, Nicole Tubiana-Mathieu, Jean Pascal Machiels, Claude El Kouri, Alain Ravaud, Etienne Suc, Jean Christophe Eymard, Ali Hasbini, Guilhem Bousquet, Stéphane Culine, Jean-Marie Boher, Gabrielle Tergemina-Clain, Clémence Legoupil, Karim Fizazi
BACKGROUND: Androgen deprivation therapy (ADT) plus docetaxel is the standard of care in fit men with metastatic castration-naive prostate cancer (mCNPC) following results from GETUG-AFU 15, CHAARTED, and STAMPEDE. No data are available on the efficacy of treatments used for metastatic castration-resistant prostate cancer (mCRPC) in men treated upfront with ADT plus docetaxel for mCNPC. OBJECTIVE: To investigate the efficacy and tolerance of subsequent treatments in patients treated upfront with chemo-hormonal therapy for mCNPC...
October 23, 2017: European Urology
https://www.readbyqxmd.com/read/29069648/androgen-receptor-expression-and-bicalutamide-antagonize-androgen-receptor-inhibit-%C3%AE-catenin-transcription-complex-in-estrogen-receptor-negative-breast-cancer
#11
Rui Huang, Jiguang Han, Xiaoshuan Liang, Shanshan Sun, Yongdong Jiang, Bingshu Xia, Ming Niu, Dalin Li, Jian Zhang, Shuo Wang, Wei Wei, Qing Liu, Wei Zheng, Guoqiang Zhang, Yanni Song, Da Panga
BACKGROUND/AIMS: Little is known about the potential mechanism of action for androgen receptor (AR) targeting treatment in estrogen receptor (ER)-negative breast cancer. This study aimed to evaluate AR status and its prognosis in four breast cancer subtypes. Bicalutamide has been identified as an AR antagonist and used for treating AR+/ER- breast cancer in a phase II trial. Our studies will clarify its mechanism in breast cancer treatment. METHODS: A total of 510 consecutive cases of invasive ductal cancer (IDC) were evaluated in this study...
October 25, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29050220/characterization-of-a-novel-androgen-receptor-ar-coregulator-ripk1-and-related-chemicals-that-suppress-ar-mediated-prostate-cancer-growth-via-peptide-and-chemical-screening
#12
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...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/28981251/development-of-5n-bicalutamide-a-high-affinity-reversible-covalent-antiandrogen
#13
Felipe de Jesus Cortez, Phuong Nguyen, Charles Truillet, Boxue Tian, Kristopher M Kuchenbecker, Michael J Evans, Paul Webb, Matthew P Jacobson, Robert J Fletterick, Pamela M England
Resistance to clinical antiandrogens has plagued the evolution of effective therapeutics for advanced prostate cancer. As with the first-line therapeutic bicalutamide (Casodex), resistance to newer antiandrogens (enzalutamide, ARN-509) develops quickly in patients, despite the fact that these drugs have ∼10-fold better affinity for the androgen receptor than bicalutamide. Improving affinity alone is often not sufficient to prevent resistance, and alternative strategies are needed to improve antiandrogen efficacy...
November 2, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28971491/plumbagin-improves-the-efficacy-of-androgen-deprivation-therapy-in-prostate-cancer-a-pre-clinical-study
#14
Parisa Abedinpour, Véronique T Baron, Adrian Chrastina, Gaelle Rondeau, Jennifer Pelayo, John Welsh, Per Borgström
BACKGROUND: Plumbagin is a candidate drug for the treatment of prostate cancer. Previous observations indicated that it may improve the efficacy of androgen deprivation therapy (ADT). This study evaluates the effectiveness of treatment with combinations of plumbagin and alternative strategies for ADT in mouse models of prostate cancer to support its clinical use. METHODS: Plumbagin was administered per oral in a new sesame oil formulation. Standard toxicology studies were performed in rats...
December 2017: Prostate
https://www.readbyqxmd.com/read/28943399/testosterone-bicalutamide-antagonism-at-the-predicted-extracellular-androgen-binding-site-of-zip9
#15
Ahmed Bulldan, Viveka Nand Malviya, Neha Upmanyu, Lutz Konrad, Georgios Scheiner-Bobis
ZIP9 is a Zn(2+) transporter, testosterone receptor, and mediator of signaling events through G-proteins. Despite these pivotal properties, however, its physiological and pathophysiological significance has not yet been comprehensively addressed. Using a cell line that lacks the classical androgen receptor we show that ZIP9-mediated phosphorylation of Erk1/2, CREB, or ATF-1 and expression of claudin-5 and zonula occludens-1 by testosterone can be completely antagonized by bicalutamide (Casodex), an anti-androgen of significant clinical impact...
December 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28875700/one-pot-synthesis-of-%C3%AE-hydroxysulfones-and-its-application-in-the-preparation-of-anticancer-drug-bicalutamide
#16
Yajun Wang, Wei Jiang, Congde Huo
An efficient one-pot multistep strategy has been developed, comprising auto-oxidative difunctionalization of alkenes, oxidation of sulfides, and a further reduction of peroxides for the synthesis of complex β-hydroxysulfone derivatives from phenthiols and alkenes. This method has several advantageous characteristics, including readily available substrates, low-cost and environmental benign reagents, nontoxic and renewable solvents, and mild reaction conditions. The application of this transformation to the multigram-scale preparation of the anticancer drug bicalutamide is accomplished...
September 14, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28851578/moving-towards-precision-urologic-oncology-targeting-enzalutamide-resistant-prostate-cancer-and-mutated-forms-of-the-androgen-receptor-using-the-novel-inhibitor-darolutamide-odm-201
#17
Hendrik Borgmann, Nada Lallous, Deniz Ozistanbullu, Eliana Beraldi, Naman Paul, Kush Dalal, Ladan Fazli, Axel Haferkamp, Pascale Lejeune, Artem Cherkasov, Martin E Gleave
Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist with a chemical structure distinctly different from currently approved AR antagonists that targets both wild-type and mutated ligand binding domain variants to inhibit AR nuclear translocation. Here, we evaluate the activity of darolutamide in enzalutamide-resistant castration resistant prostate cancer (CRPC) as well as in AR mutants detected in patients after treatment with enzalutamide, abiraterone, or bicalutamide. Darolutamide significantly inhibited cell growth and AR transcriptional activity in enzalutamide-resistant MR49F cells in vitro, and led to decreased tumor volume and serum prostate-specific antigen levels in vivo, prolonging survival in mice bearing enzalutamide-resistant MR49F xenografts...
August 26, 2017: European Urology
https://www.readbyqxmd.com/read/28840192/androgen-receptor-as-a-mediator-and-biomarker-of-radioresistance-in-triple-negative-breast-cancer
#18
Corey Speers, Shuang G Zhao, Ben Chandler, Meilan Liu, Kari Wilder-Romans, Eric Olsen, Shyam Nyati, Cassandra Ritter, Prasanna G Alluri, Vishal Kothari, Daniel F Hayes, Theodore S Lawrence, Daniel E Spratt, Daniel R Wahl, Lori J Pierce, Felix Y Feng
Increased rates of locoregional recurrence have been observed in triple-negative breast cancer despite chemotherapy and radiation therapy. Thus, approaches that combine therapies for radiosensitization in triple-negative breast cancer are critically needed. We characterized the radiation therapy response of 21 breast cancer cell lines and paired this radiation response data with high-throughput drug screen data to identify androgen receptor as a top target for radiosensitization. Our radiosensitizer screen nominated bicalutamide as the drug most effective in treating radiation therapy-resistant breast cancer cell lines...
2017: NPJ Breast Cancer
https://www.readbyqxmd.com/read/28835168/structure-activity-relationship-analysis-of-carbobicyclo-and-oxabicyclo-succinimide-analogues-as-potential-androgen-receptor-antagonists
#19
Lingyan Wang, Jiazhong Li
Prostate cancer (PCa) is a frequently diagnosed male cancer and the second leading cause of cancer-related death in many countries. Due to various amino acid mutations occurred in the ligand binding domain of androgen receptor (AR), the patients were observed insensitive, even resistant to the marketed antiandrogens such as bicalutamide and enzalutamide, which emphasizes the urgent need for novel antiandrogens to solve drug resistance problem. Recently a series of carbobicyclo and oxabicyclo succinimide analogues were reported to effectively antagonize AR...
August 23, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28827103/efficacy-and-safety-of-enzalutamide-vs-bicalutamide-in-younger-and-older-patients-with-metastatic-castration-resistant-prostate-cancer-in-the-terrain-trial
#20
D Robert Siemens, Laurence Klotz, Axel Heidenreich, Simon Chowdhury, Arnauld Villers, Benoit Baron, Steve van Os, Nahla Hasabou, Fong Wang, Ping Lin, Neal D Shore
PURPOSE: Enzalutamide significantly prolonged median progression-free survival vs bicalutamide in chemotherapy naïve men with metastatic castration resistant prostate cancer in the TERRAIN (Enzalutamide versus Bicalutamide in Castrate Men with Metastatic Prostate Cancer) trial. In this post hoc analysis we investigated the influence of age on the efficacy and safety of enzalutamide vs bicalutamide in this population. MATERIALS AND METHODS: Patients were randomized 1:1 to enzalutamide 160 mg per day or bicalutamide 50 mg per day...
August 19, 2017: Journal of Urology
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