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Antiandrogen

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https://www.readbyqxmd.com/read/30536259/rp-hplc-uv-method-for-simultaneous-quantification-of-second-generation-non-steroidal-antiandrogens-along-with-their-active-metabolites-in-mice-plasma-application-to-a-pharmacokinetic-study
#1
Ashok Zakkula, Vinay Kiran, Umesh Todmal, Suresh P Sulochana, Ramesh Mullangi
A simple, specific and reproducible high-performance liquid chromatography (HPLC) assay method has been developed and validated for the quantitation of second generation antiandrogens and their active metabolites namely apalutamide, enzalutamide, N -desmethylenzalutamide (active metabolite of enzalutamide), darolutamide and ORM-15341 (active metabolite of darolutamide) in mice plasma. The method involves extraction of apalutamide, enzalutamide, N -desmethylenzalutamide, darolutamide and ORM-15341 along with internal standard (IS) from 100 µL mice plasma through a simple protein precipitation process...
December 10, 2018: Drug Research
https://www.readbyqxmd.com/read/30533337/three-may-be-better-than-two-a-proposal-for-metformin-addition-to-pi3k-akt-inhibitor-antiandrogen-combination-in-castration-resistant-prostate-cancer
#2
REVIEW
Mohamed Islam Delma
Prostate cancer is a prevalent malignant disease. Castration-resistant prostate cancer (CRPC) is a poor prognosis form that develops upon resistance to first-line androgen deprivation therapy. Intensive research is ongoing to find efficient therapeutics for this refractory state. Actually, the combination of PI3K/Akt inhibitors with new-generation antiandrogens is among the most promising therapeutic schemes, although not yet at the optimal level. Metformin effects on prostate cancer, notably its therapeutic targets shared with antiandrogens and/or PI3K/Akt inhibitors, are reviewed in this article...
October 2, 2018: Curēus
https://www.readbyqxmd.com/read/30523523/progress-in-developing-pharmacologic-agents-to-treat-bulimia-nervosa
#3
REVIEW
Susan L McElroy, Anna I Guerdjikova, Nicole Mori, Francisco Romo-Nava
This paper reviews past and current progress in developing pharmacologic agents for the treatment of individuals with bulimia nervosa (BN). We searched the literature and clinical trial registries for compounds studied in BN, the related condition, binge eating disorder (BED), and preclinical models of binge-eating behavior. Drug classes evaluated included antidepressants, antiepileptic drugs, stimulants and other medications for attention-deficit/hyperactivity disorder, opioid antagonists, and weight loss agents, among others...
December 6, 2018: CNS Drugs
https://www.readbyqxmd.com/read/30516808/association-of-surgical-risk-with-exogenous-hormone-use-in-transgender-patients-a-systematic-review
#4
Elizabeth R Boskey, Amir H Taghinia, Oren Ganor
Importance: A growing number of transgender patients are receiving gender-affirming hormone treatments. It is unclear whether the evidence supports the current practice of routinely discontinuing these hormones prior to surgery. Objective: To determine how medications used in cross-sex hormone treatment (CSHT) affect perioperative risk. Evidence Review: A series of searches were carried out in PubMed and Excerpta Medica Database to identify articles using each of the terms testosterone, estrogen, estradiol, oral contraceptive, spironolactone, cyproterone acetate, finasteride, dutasteride, leuprolide, goserelin, and histrelin, in combination with the terms surgery, perioperative, thrombosis, thromboembolism, and operative...
December 5, 2018: JAMA Surgery
https://www.readbyqxmd.com/read/30516672/incidental-18f-naf-uptake-in-drug-induced-gynecomastia
#5
Esha Kothekar, William Y Raynor, Abdullah Al-Zaghal, Thomas J Werner, Abass Alavi
Gynecomastia is not uncommon in men older than 50 years of age and is characterized by glandular proliferation of breast tissue. Non-physiologic gynecomastia is mostly caused by a variety of external medical interventions. Medications that belong to classes of antiandrogens, antipsychotics, or antibiotics alter the levels of estrogen and testosterone and are commonly implicated in patients with gynecomastia. We are presenting a case of bilateral F-NaF uptake in the breast tissue of a 56-year-old man with known history of prostate cancer...
December 3, 2018: Clinical Nuclear Medicine
https://www.readbyqxmd.com/read/30511964/targeting-foxa1-mediated-repression-of-tgf-%C3%AE-signaling-suppresses-castration-resistant-prostate-cancer-progression
#6
Bing Song, Su-Hong Park, Jonathan C Zhao, Ka-Wing Fong, Shangze Li, Yongik Lee, Yeqing A Yang, Subhasree Sridhar, Xiaodong Lu, Sarki A Abdulkadir, Robert L Vessella, Colm Morrissey, Timothy M Kuzel, William J Catalona, Ximing J Yang, Jindan Yu
Prostate cancer (PCa) progressed to castration resistance (CRPC) is a fatal disease. CRPC tumors develop resistance to new-generation anti-androgen enzalutamide through lineage plasticity, characterized by epithelial-mesenchymal transition (EMT) and basal-like phenotype. FOXA1 is a transcription factor essential for epithelial lineage differentiation. Here, we demonstrate that FOXA1 loss leads to remarkable up-regulation of transforming growth factor beta 3 (TGFB3), which encodes a ligand of TGF-β pathway...
December 4, 2018: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/30507748/sensitivity-of-fluorine-18-fluoromethylcholine-pet-ct-to-prostate-specific-antigen-over-different-plasma-levels-a-retrospective-study-in-a-cohort-of-192-patients-with-prostate-cancer
#7
Giampiero Giovacchini, Elisabetta Giovannini, Elisa Borsò, Patrizia Lazzeri, Mattia Riondato, Rossella Leoncini, Valerio Duce, Maria Picchio, Andrea Ciarmiello
PURPOSE: Several factors have been identified that predict positive fluorine-18-fluoromethylcholine (F-FCH) PET/CT result in patients with prostate cancer undergoing PET/CT for biochemical failure. Among these factors, prostate-specific antigen (PSA) is the single factor most consistently associated with the prediction of positive F-FCH PET/CT. In this study, we wished to confirm this finding and expand it in a large series of patients. PATIENTS AND METHODS: We retrospectively analyzed 192 patients with prostate cancer who were recruited from the Nuclear Medicine Department of the Sant'Andrea Hospital of La Spezia, Italy, from March 2013 to March 2018 and who underwent F-FCH PET/CT owing to biochemical failure after radical prostatectomy...
November 29, 2018: Nuclear Medicine Communications
https://www.readbyqxmd.com/read/30497883/androgen-deprivation-therapies-and-changes-in-comorbidity-a-comparison-of-gonadotropin-releasing-hormone-agonists-and-antiandrogen-monotherapy-as-primary-therapy-in-men-with-high-risk-prostate-cancer
#8
Kerri Beckmann, Hans Garmo, Jan Adolfsson, Cecilia Bosco, Eva Johansson, David Robinson, Lars Holmberg, Par Stattin, Mieke Van Hemelrijck
BACKGROUND: Some studies suggest that gonadotropin-releasing hormone (GnRH) agonists are associated with higher risk of adverse events than antiandrogens (AAs) monotherapy. However, it has been unclear whether this is due to indication bias. OBJECTIVE: To investigate rates of change in comorbidity for men on GnRH agonists versus AA monotherapy in a population-based register study. DESIGN, SETTING, AND PARTICIPANTS: Men with advanced nonmetastatic prostate cancer (PCa) who received primary AA (n=2078) or GnRH agonists (n=4878) and age- and area-matched PCa-free men were selected from Prostate Cancer Database Sweden 3...
November 26, 2018: European Urology
https://www.readbyqxmd.com/read/30485050/caring-for-transgender-and-gender-diverse-persons-what-clinicians-should-know
#9
David A Klein, Scott L Paradise, Emily T Goodwin
Persons whose experienced or expressed gender differs from their sex assigned at birth may identify as transgender. Transgender and gender-diverse persons may have gender dysphoria (i.e., distress related to this incongruence) and often face substantial health care disparities and barriers to care. Gender identity is distinct from sexual orientation, sex development, and external gender expression. Each construct is culturally variable and exists along continuums rather than as dichotomous entities. Training staff in culturally sensitive terminology and transgender topics (e...
December 1, 2018: American Family Physician
https://www.readbyqxmd.com/read/30462228/biomarkers-of-exposure-to-pyrimethanil-after-controlled-human-experiments
#10
Moosa Faniband, Eva Ekman, Margareta Littorin, Margareta Maxe, Estelle Larsson, Christian H Lindh
Pyrimethanil (PYM) is a fungicide used pre- and post-harvest on many crops. It has a low acute toxicity but is of toxicological concern because of its antiandrogenic properties. The aim of the current work was to investigate some metabolism and estimate elimination kinetics of PYM in humans after experimental oral and dermal exposure. A liquid chromatography triple quadrupole mass spectrometry (LC-MS-MS) method was developed and validated for the analysis of PYM and its metabolite 4-hydroxypyrimethanil (OH-PYM) in human urine...
November 14, 2018: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/30425003/results-of-a-prospective-phase-2-pilot-trial-of-177-lu-psma-617-therapy-for-metastatic-castration-resistant-prostate-cancer-including-imaging-predictors-of-treatment-response-and-patterns-of-progression
#11
Louise Emmett, Megan Crumbaker, Bao Ho, Kathy Willowson, Peter Eu, Lalith Ratnayake, Richard Epstein, Ashley Blanksby, Lisa Horvath, Alex Guminski, Kate Mahon, Craig Gedye, Charlotte Yin, Phillip Stricker, Anthony M Joshua
BACKGROUND: 177 Lu-PSMA-617 (Lu-PSMA) is an emerging therapy in men with metastatic castration-resistant prostate cancer. Paired theranostic agents have the potential to visually identify phenotypes that will respond to targeted therapy. This study examined the value of 68 Ga-HBEDD PSMA-11; prostate-specific membrane antigen (PSMA) positron emission tomography (PET) in predicting treatment response and disease progression in Lu-PSMA therapy within the context of a phase 2 prospective pilot trial...
September 27, 2018: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/30423407/targeting-ar-beclin-1-complex-modulated-growth-factor-signaling-increases-the-antiandrogen-enzalutamide-sensitivity-to-better-suppress-the-castration-resistant-prostate-cancer-growth
#12
Meng Zhang, Yin Sun, Jialin Meng, Li Zhang, Chaozhao Liang, Chawnshang Chang
While the recently developed antiandrogen Enzalutamide (Enz) can extend survival for 4.8 months in castration-resistant prostate cancer (CRPC) patients, eventually most of these CRPC patients may develop resistance to the Enz without a clear mechanism. Here we found the expression of Beclin 1 was decreased in both Enz-resistant (EnzR) cell lines (EnzR1-C4-2 and EnzR2-C4-2B) as compared to their parental Enz-sensitive (EnzS) (EnzS1-C4-2 and EnzS2-C4-2B) cells, and targeting the Beclin 1 could lead to increase the Enz-sensitivity in these two CRPC cell lines...
November 10, 2018: Cancer Letters
https://www.readbyqxmd.com/read/30398479/apalutamide-for-the-treatment-of-patients-with-castration-resistant-prostate-cancer
#13
R Hauke
Patients with recurrent, nonmetastatic prostate cancer after curative intent therapy can experience a heterogeneous clinical course ranging from indolent disease that can be observed for years to a rapidly progressive disease that is metastatic in a relatively short time. Patients with short prostate-specific antigen (PSA) doubling times are at risk for early development of metastatic disease and are frequently placed on androgen deprivation therapy. Although castration-resistant disease inevitably occurs in these patients, most therapies for castration-resistant disease have shown benefit in the metastatic setting...
October 2018: Drugs of Today
https://www.readbyqxmd.com/read/30374010/-endocrine-therapy-for-prostate-cancer
#14
Naoya Nagaya, Shigeo Horie
Endocrine therapy for prostate cancer is androgen deprivation therapy and antiandrogens, which are the standard treatment for advanced prostate cancer. Endocrine therapy is effective in most prostate cancers, but as treatment continues, most patients eventually experience resistant to endocrine therapy and disease progression. Patients in this state are said to have castration-resistant prostate cancer. This review outlines the types of endocrine therapy for prostate cancer, the physiological mechanisms of endocrine therapy, its clinical use in Japan and the United States and Europe, new endocrine therapy for castration-resistant prostate cancer, and the side effects to be noted in endocrine therapy...
2018: Clinical Calcium
https://www.readbyqxmd.com/read/30339554/the-rationality-of-combining-second-generation-antiandrogens-with-177lu-psma-or-its-alpha-emitting-congeners-for-better-and-durable-results-will-this-dominate-the-therapeutic-landscape-and-be-an-upfront-consideration-in-metastatic-castration-resistant-prostate
#15
https://www.readbyqxmd.com/read/30319126/-enzalutamide-in-castration-resistant-prostate-cancer
#16
Emilio Ríos González, Luis Martínez-Piñeiro
Androgen deprivation therapy is part of the initial treatment of patients with metastatic prostate cancer. Nevertheless, after an initial response and despite maintaining an effective testosterone suppression, the tumor is able to continue growing.Enzalutamide is an oral second generation pure antiandrogen that acts at various levels in the signal activation cascade of the androgen receptor and has demonstrated being effective in this phase of the disease. In the clinical trials completed, it has demonstrated benefits in overall patient survival in patients with the diagnosis of metastatic castration resistant prostate cancer...
September 2018: Archivos Españoles de Urología
https://www.readbyqxmd.com/read/30300430/endocrine-disruptor-compounds-in-environment-as-a-danger-for-children-health
#17
REVIEW
Monika Beszterda, Rafał Frański
Endocrine disrupting compounds (EDCs) are heterogenous in structure and include synthetic organic compounds such as pharmaceutical agents, plant protection products, plastics, plasticizers, polychlorinated biphenyls, dioxins, flame-retardants, and antifoulant paint additive, as well, as natural plant-derived EDCs termed phytoestrogens and mycoestrogens. Children and adults are exposed daily to EDCs during drinking contaminated water, eating, breathing polluted air or direct contact with chemicals. Prenatal and perinatal period, infancy, childhood, and puberty are critical time of development during which maturing systems are particularly sensitive to hormonal disruptions (small elimination of xenobiotics)...
2018: Pediatric Endocrinology, Diabetes, and Metabolism
https://www.readbyqxmd.com/read/30279580/impact-of-age-on-exposure-to-oral-antiandrogen-therapies-in-clinical-practice
#18
Marie-Rose B S Crombag, Merel van Nuland, Andries M Bergman, Hilde Rosing, Jan H M Schellens, Alwin D R Huitema, Jos H Beijnen
BACKGROUND: Oral antiandrogen therapies are predominantly used in older men, but real-life studies evaluating the impact of age on pharmacokinetic exposure are lacking. This study aims to evaluate the impact of age on the pharmacokinetic profiles of abiraterone acetate and enzalutamide in clinical practice. PATIENTS AND METHODS: Retrospective observational study to evaluate the impact of age on the first steady-state sample of patients treated with abiraterone acetate or enzalutamide in routine daily clinical practice...
October 2, 2018: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/30256230/gender-affirming-hormone-therapy-for-transgender-females
#19
John F Randolph
The provision of hormone therapy, both estrogens and antiandrogens, to adult transgender females is well within the scope of practice of the obstetrician gynecologist. The goal is to induce feminizing changes and suppress previously developed masculinization. Estrogens in sufficient doses will usually achieve both goals with augmentation by antiandrogens. The primary short-term risk of estrogens is thrombosis, but long-term risk in transgender females is unclear. Optimal care requires pretreatment education and assessment, individualized dosing, ongoing routine monitoring, and standard breast and prostate cancer screening...
December 2018: Clinical Obstetrics and Gynecology
https://www.readbyqxmd.com/read/30231802/new-onset-lupus-nephritis-after-male-to-female-sex-reassignment-surgery
#20
L T Pontes, D T Camilo, M R De Bortoli, R S S Santos, W M Luchi
We report an original case of a 27-year-old transgender woman who developed lupus nephritis after male-to-female sex reassignment surgery. The patient had been taking hormones to induce feminization since the age of 18. She was admitted with malar "butterfly" rash, anasarca and hypertension, associated with an increase in serum creatinine (1.7 mg/dl). Renal involvement was characterized by nephritic and nephrotic syndrome. Autoantibody tests were positive for antinuclear antibodies and anti-double-stranded DNA, and complement levels were markedly reduced...
November 2018: Lupus
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