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https://read.qxmd.com/read/30854946/synthesis-of-deuterium-labeled-5-5-dimethyl-3-%C3%AE-%C3%AE-%C3%AE-trifluoro-4-nitro-m-tolyl-hydantoin
#1
Ratna Sekhar Bolla, Narasimha Murthy Gandikota, Ivaturi Venkata Kasi Viswanath
OBJECTIVE: Stable and non-radioactive isotope labeled compounds gained significance in recent drug discovery and other various applications such as bio-analytical studies. The modern bioanalytical techniques can study the adverse therapeutic effects of drugs by comparing isotopically labeled internal standards. A well-designed labeled compound can provide high-quality information about the identity and quantification of drug-related compounds in biological samples. This information can be very useful at key decision points in drug development...
2019: Current Radiopharmaceuticals
https://read.qxmd.com/read/30853808/efficacy-and-safety-of-combined-androgen-blockade-with-antiandrogen-for-advanced-prostate-cancer
#2
Y Yang, R Chen, T Sun, L Zhao, F Liu, S Ren, H Wang, X Lu, X Gao, C Xu, Y Sun
Background: Combined androgen blockade (cab) is a promising treatment modality for prostate cancer (pca). In the present meta-analysis, we compared the efficacy and safety of first-line cab using an antiandrogen (aa) with castration monotherapy in patients with advanced pca. Methods: PubMed, embase, Cochrane, and Google Scholar were searched for randomized controlled trials (rcts) published through 12 December 2016. Hazard ratios (hrs) with 95% confidence intervals (cis) were determined for primary outcomes: overall survival (os) and progression-free survival (pfs)...
February 2019: Current Oncology
https://read.qxmd.com/read/30820126/autistic-undisciplined-thinking-in-the-practice-of-medical-trichology
#3
Ralph Michel Trüeb, Hudson Dutra, Maria Fernanda Reis Gavazzoni Dias
Medical trichology is the branch of dermatology that deals with the scientific study of the hair and scalp in health and disease. As any discipline, the practice of medical trichology is not immune to malpractice, either deliberately or carelessly. In his publication "Autistic Undisciplined Thinking in Medicine and How to Overcome It," Swiss psychiatrist Eugen Bleuler describes yet another form of malpractice in medicine reflecting autistic-undisciplined thinking. Autism is not limited to psychopathology, but inherent to the thinking of man throughout history in his drive for knowledge, with thousands of theories lacking any basis in reality...
January 2019: International Journal of Trichology
https://read.qxmd.com/read/30818232/endocrine-disrupting-chemical-exposure-and-maladaptive-behavior-during-adolescence
#4
Jessica R Shoaff, Antonia M Calafat, Susan L Schantz, Susan A Korrick
BACKGROUND: Studies suggest that exposure to endocrine disrupting chemicals (EDCs), including phthalates, phenols, and parabens may influence childhood behavior, but the relationship during adolescence has not been assessed. OBJECTIVE: We investigated the association between urinary biomarker concentrations of potential EDCs, including some phthalate and bisphenol A replacement chemicals, and behavior in adolescents. METHODS: Participants were from the New Bedford Cohort (NBC), a prospective birth cohort of residents near the New Bedford Harbor Superfund site in Massachusetts...
December 22, 2018: Environmental Research
https://read.qxmd.com/read/30811143/cortexolone-17%C3%AE-propionate-clascoterone-is-an-androgen-receptor-antagonist-in-dermal-papilla-cells-in-vitro
#5
Caridad Rosette, Niccolette Rosette, Alessandro Mazzetti, Luigi Moro, Mara Gerloni
Cortexolone 17α-propionate (clascoterone) is a novel androgen antagonist that is currently being analyzed in a large phase 2 clinical trial for the topical treatment of androgenetic alopecia (AGA). While the pathogenesis of AGA is still debated, the consensus is that AGA is an androgen-dependent hair disorder with strong genetic links, and that the testosterone metabolite, dihydrotestosterone (DHT), plays a causal role in its development. DHT binds to the androgen receptor (AR) in scalp dermal papilla cells (DPC) to induce AR-mediated transcription of genes that contribute to AGA in genetically predisposed individuals...
February 1, 2019: Journal of Drugs in Dermatology: JDD
https://read.qxmd.com/read/30800265/cardiovascular-profile-of-pharmacological-agents-used-for-the-management-of-polycystic-ovary-syndrome
#6
REVIEW
Huda Alalami, Thozhukat Sathyapalan, Stephen L Atkin
Women with polycystic ovary syndrome (PCOS) have an adverse metabolic profile with an increased risk of prediabetes and type 2 diabetes (T2DM); however, it is unclear if PCOS is associated with increased cardiovascular events in later years independent of the presence of T2DM. Many therapies have been used to treat the differing facets of PCOS, including those for menstrual irregularity, hirsutism, acne and anovulatory infertility. The aim of this review was to evaluate the cardiovascular profiles associated with the medications used in the management of PCOS and evaluate whether they have cardiovascular benefit, detriment or are neutral...
2019: Therapeutic Advances in Endocrinology and Metabolism
https://read.qxmd.com/read/30785992/female-pattern-hair-loss-and-androgen-excess-a-report-from-the-multidisciplinary-androgen-excess-and-pcos-committee
#7
E Carmina, R Azziz, W Bergfeld, H F Escobar Morreale, W Futterweit, H Huddleston, R A Lobo, E Olsen
OBJECTIVE: To determine the current state of knowledge and provide evidence-based recommendations that could be valid for all specialists taking care of female pattern hair loss (FPHL), a common form of hair loss in women that is characterized by the reduction of hair density in the central area of the scalp, while the frontal hairline is generally well conserved. PARTICIPANTS: An expert task force appointed by Androgen Excess and PPCOS society, which included specialists from dermatology, endocrinology, and reproductive endocrinology...
February 20, 2019: Journal of Clinical Endocrinology and Metabolism
https://read.qxmd.com/read/30779277/impact-of-access-to-novel-therapies-on-the-initial-management-of-castrate-resistant-prostate-cancer-an-australian-multicentre-study
#8
E M Kwan, M C Semira, A R T Bergin, C Muttiah, S Beck, A Anton, D Campbell, S Wong, M Rosenthal, P Gibbs, B Tran
BACKGROUND: The impact of regulatory approvals of new therapies for castration-resistant prostate cancer (CRPC) in Australia is unclear. AIMS: To determine if changes in novel therapy access in Australia affected how clinicians initially managed men with newly-diagnosed CRPC. METHODS: Data from patients diagnosed with CRPC from 2013-2016 across three Australian hospitals were retrospectively collected. Baseline clinicopathological factors and initial management decision at time of CRPC development (early treatment [ET] vs deferred treatment [DT]) were recorded...
February 18, 2019: Internal Medicine Journal
https://read.qxmd.com/read/30747897/targeting-metastatic-hormone-sensitive-prostate-cancer-chemohormonal-therapy-and-new-combinatorial-approaches
#9
Shivashankar Damodaran, Joshua M Lang, David F Jarrard
PURPOSE: Androgen deprivation therapy(ADT) alone has been the standard of care for metastatic hormone sensitive prostate cancer(mHSPC) for the last 75 years. This review focuses on recent trials and mechanisms that highlight a new paradigm, combining ADT with other agents, changing the management of prostate cancer patients with advanced disease. METHODS: A PubMed and Web of Science database search on peer-reviewed literature was performed through January 2018 using the keywords "metastatic hormone sensitive prostate cancer", " metastatic castration sensitive prostate cancer", "docetaxel", "abiraterone" and "senescence in cancer"...
February 7, 2019: Journal of Urology
https://read.qxmd.com/read/30742279/the-evolving-systemic-treatment-landscape-for-patients-with-advanced-prostate-cancer
#10
REVIEW
Martina Pagliuca, Carlo Buonerba, Karim Fizazi, Giuseppe Di Lorenzo
Prostate cancer (PC) is a major health issue in developed countries, with, on the one hand, men suffering from sequelae related to unnecessary treatment of non-lethal PC, and, on the other hand, still dying because of advanced PC that progresses to castration-resistant disease. Systemic treatment is the mainstay of therapy of castration-resistant PC (CRPC). To date, a multitude of systemic agents have been tested and many of these have failed to provide a clinically meaningful benefit in CRPC, while others have been approved by the US Food and Drug Administration and/or the European Medicines Agency, including antiandrogen hormonal drugs (abiraterone, enzalutamide, apalutamide), chemotherapy (docetaxel and cabazitaxel), immunotherapy (Sipuleucel-T), and radiopharmaceutical (Radium-223) agents...
February 11, 2019: Drugs
https://read.qxmd.com/read/30739263/comparative-assessment-of-prognostic-outcomes-between-first-generation-antiandrogens-and-novel-androgen-receptor-axis-targeted-agents-in-patients-with-non-metastatic-castration-resistant-prostate-cancer
#11
Hideaki Miyake, Yuto Matsushita, Hiromitsu Watanabe, Keita Tamura, Daisuke Motoyama, Toshiki Ito, Takayuki Sugiyama, Atsushi Otsuka
BACKGROUND: To compare the prognostic outcomes between first-generation antiandrogen (FGA) and novel androgen-receptor-axis-targeted agent (ARATA) as first-line therapy in patients with non-metastatic castration-resistant prostate cancer (nmCRPC). METHODS: This study retrospectively included a total of 103 consecutive nmCRPC patients consisting of 47 (45.6%) and 56 (54.4%) who received FGA (bicalutamide or flutamide) and ARATA (abiraterone acetate or enzalutamide), respectively, as the first-line agent after the failure of primary androgen deprivation therapy (ADT)...
February 9, 2019: International Journal of Clinical Oncology
https://read.qxmd.com/read/30711833/rational-drug-design-for-androgen-receptor-and-glucocorticoids-receptor-dual-antagonist
#12
Meng Wu, Yongli Xie, Xiangling Cui, Chenchao Huang, Rongyu Zhang, Yang He, Xiaoyu Li, Mingliang Liu, Shan Cen, Jinming Zhou
Prostate cancer (PCa) is the most frequently diagnosed male malignant tumor and remains the second leading cause of male cancer mortality in the western countries. The second-generation antiandrogen enzalutamide (ENZa) can prolong survival time for patients with mCRPC. However, the overexpression of glucocorticoids receptor (GR) in mCRPC cells causes the resistance of antiandrogen and leads to the failure of androgen receptor (AR) targeting therapy. Herein, based on the chemical structures of antiandrogen and crystal structure of GR, we set up to develop GR/AR (GR and AR) dual antagonist by virtual screening and biological evaluation...
March 15, 2019: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/30695006/polycystic-ovary-syndrome-diagnosis-and-management
#13
Mary Lauren Pfieffer
Polycystic ovary syndrome (PCOS) is a common endocrine disorder. Patients may present with a combination of hyperandrogenism symptoms, menstrual irregularities, metabolic syndrome, infertility, acne, and obesity. PCOS diagnosis is based on three diagnostic guidelines. Treatment options include oral contraceptive pills, antiandrogens, and metformin. NPs can improve diagnosed patients' quality of life through education about this disorder.
March 2019: Nurse Practitioner
https://read.qxmd.com/read/30693539/effect-of-monoamine-oxidase-a-maoa-inhibitors-on-androgen-sensitive-and-castration-resistant-prostate-cancer-cells
#14
Shikha Gaur, Mitchell E Gross, Chun-Peng Liao, Bin Qian, Jean C Shih
BACKGROUND: Monoamine oxidase A (MAOA) is best known for its role in neuro-transmitter regulation. Monoamine oxidase inhibitors are used to treat atypical depression. MAOA is highly expressed in high grade prostate cancer and modulates tumorigenesis and progression in prostate cancer. Here, we investigated the potential role of MAOA inhibitors (MAOAIs) in relation to the androgen receptor (AR) pathway and resistance to antiandrogen treatment in prostate cancer. METHODS: We examined MAOA expression and the effect of MAOI treatment in relation to AR-targeted treatments using the LNCaP, C4-2B, and 22Rv1 human prostate cancer cell lines...
January 28, 2019: Prostate
https://read.qxmd.com/read/30692044/preclinical-study-using-androgen-receptor-ar-degradation-enhancer-to-increase-radiotherapy-efficacy-via-targeting-radiation-increased-ar-to-better-suppress-prostate-cancer-progression
#15
Fu-Ju Chou, Yuhchyau Chen, Dong Chen, Yuanjie Niu, Gonghui Li, Peter Keng, Shuyuan Yeh, Chawnshang Chang
BACKGROUND: While androgen deprivation therapy (ADT) and radiotherapy (RT) are currently used together to treat locally advanced prostate cancer (PCa), RT might have the adverse effect of increasing the PCa androgen receptor (AR) protein expression, which might then increase the resistance to continued RT. METHODS: We used multiple assays for RT sensitivity, protein and RNA expression of AR and related DDR genes, ROS level, DNA damage/repair level, cell cycle and apoptosis...
January 25, 2019: EBioMedicine
https://read.qxmd.com/read/30674872/preclinical-study-using-circular-rna-17-and-micro-rna-181c-5p-to-suppress-the-enzalutamide-resistant-prostate-cancer-progression
#16
Gang Wu, Yin Sun, Zhendong Xiang, Keliang Wang, Bo Liu, Guangqian Xiao, Yuanjie Niu, Denglong Wu, Chawnshang Chang
Androgen-deprivation therapy (ADT) with newly developed antiandrogen enzalutamide (Enz) may increase the castration-resistant prostate cancer (CRPC) patients survival an extra 4.8 months. Yet eventually most patients may fail with development of Enz resistance. While recent clinical studies indicated that the increased expression of the androgen receptor (AR) splicing variant ARv7 might have key roles for the development of Enz resistance in CRPC, its detailed mechanism, especially its linkage to the circular RNAs (circRNAs), a form of non-coding RNA, however, remains unclear...
January 15, 2019: Cell Death & Disease
https://read.qxmd.com/read/30671393/gender-affirmative-care-of-transgender-people-a-single-center-s-experience-in-korea
#17
Hyun Hye Lim, Yun Ha Jang, Gyu Yeon Choi, Jeong Jae Lee, Eun Sil Lee
Objective: To investigate the clinical characteristics and medical management of transgender people in South Korea. Methods: The electronic medical records of 54 transgender persons who had visited Soonchunhyang University Hospital from January 2016 to December 2017 for medical care were retrospectively reviewed. We identified patient demographics and gender identity-related characteristics. Moreover, we compared our hospital protocol with official guidelines. Results: At the time of the medical record search, the average age of these 52 transgender persons was 27 years, and 46 (88...
January 2019: Obstetrics & Gynecology Science
https://read.qxmd.com/read/30666456/combined-hormonal-influence-of-cyproterone-acetate-and-nomegestrol-acetate-on-meningioma-a-case-report
#18
Pierre-Olivier Champagne, Thibault Passeri, Sebastien Froelich
Cyproterone acetate (CPA) is an antiandrogenic drug which has recently been recognized to promote the occurrence and growth of intracranial meningiomas. Nomegestrol acetate (NOMAC) is a widely used progestin-like drug that could be suggested as an alternative for patients taking CPA. We report a case of CPA-related meningioma for which relay from CPA to NOMAC led to further tumor growth and cessation of NOMAC-induced tumor shrinkage. We suggest NOMAC can have a similar effect than CPA on meningiomas. The use of NOMAC as replacement for CPA in the presence of a meningioma should be discouraged until further evidence becomes available on the role of NOMAC in such instances...
January 22, 2019: Acta Neurochirurgica
https://read.qxmd.com/read/30661420/co-crystallization-for-enhanced-dissolution-rate-of-bicalutamide-preparation-and-evaluation-of-rapidly-disintegrating-tablets
#19
Ebtessam A Essa, Aya R Elbasuony, Abdelaziz E Abdelaziz, Gamal M El Maghraby
OBJECTIVES: Enhance the dissolution rate of bicalutamide via co-crystallization with sucralose (sweetener), with the aim to develop rapidly disintegrating tablets with subsequent prompt dissolution. SIGNIFICANCE: Bicalutamide is antiandrogenic agent for treatment of prostate cancer but has low and variable oral bioavailability, mainly attributed to poor dissolution. Co-crystallization with benign excipients is promising for dissolution enhancement with the additive serving dual functions...
January 19, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/30660434/usefulness-of-18f-fluorocoline-pet-ct-in-prostate-cancer-patients-with-biochemical-recurrence-influence-of-psa-kinetics-and-hormone-therapy
#20
Eva María Triviño-Ibáñez, Ignacio Puche-Sanz, Manuel Gómez-Río, José Manuel Cózar Olmo, José Manuel Llamas-Elvira, Antonio Rodríguez-Fernández
PURPOSE: To evaluate the capacity of 18f-fluorocholine positron emission tomography/computed tomography (FCH PET/CT) to detect biochemical recurrence of prostate cancer and to determine the correlation with PSA kinetics and influence of antiandrogen hormone therapy. PATIENTS AND METHODS: Observational and retrospective study, which included patients with prostate cancer and criteria for biochemical recurrence and/or resistance to castration, according to the European Association of Urology...
January 16, 2019: Medicina Clínica
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