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https://www.readbyqxmd.com/read/29642892/a-systematic-and-prospectively-validated-approach-for-identifying-synergistic-drug-combinations-against-malaria
#1
Yasaman KalantarMotamedi, Richard T Eastman, Rajarshi Guha, Andreas Bender
BACKGROUND: Nearly half of the world's population (3.2 billion people) were at risk of malaria in 2015, and resistance to current therapies is a major concern. While the standard of care includes drug combinations, there is a pressing need to identify new combinations that can bypass current resistance mechanisms. In the work presented here, a combined transcriptional drug repositioning/discovery and machine learning approach is proposed. METHODS: The integrated approach utilizes gene expression data from patient-derived samples, in combination with large-scale anti-malarial combination screening data, to predict synergistic compound combinations for three Plasmodium falciparum strains (3D7, DD2 and HB3)...
April 11, 2018: Malaria Journal
https://www.readbyqxmd.com/read/29613885/hormone-therapy-in-menopausal-women-with-fibroids-is-it-safe
#2
Vedhapriya Srinivasan, Mark G Martens
Menopause is an important transition in the life of women. It has been estimated that by the year 2030, worldwide 1.2 billion women will be menopausal. The most bothersome symptoms of menopause are believed to be due to declines in estrogen levels in postmenopausal women. Thus, hormone therapy is an effective treatment option for menopausal women, although prolonged use of hormone therapy is associated with a slightly increased risk of breast cancer, thromboembolism, and stroke. A literature search for studies evaluating the effects of hormone therapy in menopausal women with asymptomatic fibroids demonstrated variable effects of hormone therapy on the volume and size of the fibroids...
April 2, 2018: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/29610032/personalized-prevention-in-high-risk-individuals-managing-hormones-and-beyond
#3
D Gareth Evans, Sacha J Howell, Anthony Howell
Increasing numbers of women are being identified at 'high-risk' of breast cancer, defined by The National Institute of Health and Care Excellence (NICE) as a 10-year risk of ≥8%. Classically women have been so identified through family history based risk algorithms or genetic testing of high-risk genes. Recent research has shown that assessment of mammographic density and single nucleotide polymorphisms (SNPs), when combined with established risk factors, trebles the number of women reaching the high risk threshold...
March 30, 2018: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/29589250/novel-cationic-supersaturable-nanomicellar-systems-of-raloxifene-hydrochloride-with-enhanced-biopharmaceutical-attributes
#4
Atul Jain, Rajpreet Kaur, Sarwar Beg, Varun Kushwah, Sanyog Jain, Bhupinder Singh
The work describes systematic development of nanomicellar cationic supersaturable self-nanoemulsifying drug delivery systems (CS-SNEDDS) for augmenting oral biopharmaceutical performance of raloxifene hydrochloride. Plain SNEDDS formulation containing Capryol 90, Cremophor RH 40, and Transcutol HP was optimized using D-optimal mixture design. SNEDDS were characterized for emulsification time, globule size, in vitro drug release, and ex vivo permeation. The CS-SNEDDS formulation was prepared from the optimized SNEDDS by adding oleylamine as the cationic charge inducer and HPMC as the polymeric precipitation inhibitor...
March 27, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29579065/the-effect-of-estrogenic-compounds-on-psychosis-like-behaviour-in-female-rats
#5
Alyssa Sbisa, Maarten van den Buuse, Andrea Gogos
17β-estradiol treatment has shown benefit against schizophrenia symptoms, however long-term use may be associated with negative side-effects. Selective estrogen receptor modulators, such as raloxifene and tamoxifen, have been proposed as suitable alternatives to 17β-estradiol. An isomer of 17β-estradiol, 17α-estradiol, is considered less carcinogenic, and non-feminising in males, however little is known about its potential as a treatment for schizophrenia. Moreover, the mechanism underlying the therapeutic action of estrogens remains unclear...
2018: PloS One
https://www.readbyqxmd.com/read/29574654/serms-promote-anti-inflammatory-signaling-and-phenotype-of-cd14-cells
#6
Lauri Polari, Anu Wiklund, Sofia Sousa, Lauri Kangas, Tero Linnanen, Pirkko Härkönen, Jorma Määttä
Signaling via estrogen receptors (ER) is recognized as an essential part of the immune regulation, and ER-mediated signaling is involved in autoimmune reactions. Especially ERα activation in immune cells has been suggested to skew cytokine production toward Th2/M2-type mediators, which can have protective effect on inflammatory diseases and reduce Th1 and Th17 responses. These effects are caused by increased alternative activation of macrophages and changes in the activation of different T cell populations...
March 24, 2018: Inflammation
https://www.readbyqxmd.com/read/29571322/long-term-treatment-of-tamoxifen-and-raloxifene-alleviates-dystrophic-phenotype-and-enhances-muscle-functions-of-fkrp-dystroglycanopathy
#7
Bo Wu, Sapana N Shah, Peijuan Lu, Lauren E Bollinger, Anthony Blaeser, Susan Sparks, Amy D Harper, Qi L Lu
The third most common form of limb-girdle muscular dystrophies is caused by mutations of the Fukutin-related protein (FKRP) gene, with no effective therapy available. Selective estrogen receptor modulators, tamoxifen and raloxifene, have been widely used for human conditions for their anti-inflammatory, antifibrosis, prevention of bone loss, and muscle building effects (essential features for muscular dystrophy therapies). We evaluated therapeutic values of tamoxifen and raloxifene in FKRPP448L mutant mouse with severe dystrophic phenotype...
April 2018: American Journal of Pathology
https://www.readbyqxmd.com/read/29564735/real-world-effectiveness-of-osteoporosis-therapies-for-fracture-reduction-in-post-menopausal-women
#8
Akeem A Yusuf, Steven R Cummings, Nelson B Watts, Maurille Tepie Feudjo, J Michael Sprafka, Jincheng Zhou, Haifeng Guo, Akhila Balasubramanian, Cyrus Cooper
Studies examining real-world effectiveness of osteoporosis therapies are beset by limitations due to confounding by indication. By evaluating longitudinal changes in fracture incidence, we demonstrated that osteoporosis therapies are effective in reducing fracture risk in real-world practice settings. INTRODUCTION: Osteoporosis therapies have been shown to reduce incidence of vertebral and non-vertebral fractures in placebo-controlled randomized clinical trials. However, information on the real-world effectiveness of these therapies is limited...
March 21, 2018: Archives of Osteoporosis
https://www.readbyqxmd.com/read/29564555/treatment-patterns-in-patients-with-osteoporosis-at-high-risk-of-fracture-in-japan-retrospective-chart-review
#9
Saeko Fujiwara, Akimitsu Miyauchi, Etsuro Hamaya, Rebecca Jayne Nicholls, Adele Weston, Santwona Baidya, Lionel Pinto, Rich Barron, Junichi Takada
Osteoporosis (OP) causes reduced bone strength and increases risk of fractures. Medical records from specialist clinics in Japan of postmenopausal women with OP and high risk of fracture were analysed. Majority of patients were treated for OP as recommended and were prescribed OP medications soon after high-risk OP diagnosis. PURPOSE: The incidence of osteoporosis (OP) in Japan is predicted to increase significantly in coming decades. Resultant osteoporotic fractures are a significant contributor of economic and social burden among elderly osteoporosis patients...
March 22, 2018: Archives of Osteoporosis
https://www.readbyqxmd.com/read/29540634/identification-of-small-molecule-inhibitors-of-human-golgi-mannosidase-via-a-drug-repositioning-screen
#10
Ryosuke Koyama, Wataru Hakamata, Takako Hirano, Toshiyuki Nishio
Three Golgi mannosidases (GMs), namely Golgi α-mannosidases IA, IB, and IC, remove mannose residues from N-glycans and regulate the quality control and transportation of nascent proteins. GM inhibitors regulate several biological events such as cell-cell communication, differentiation, and apoptosis in cancer cells. As a result, GM inhibitor-based therapies have gained significant attention for cancer treatment. However, to date, no GM inhibitor has been approved and none is in clinical development for anti-cancer treatment...
March 13, 2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29537855/the-effect-of-piperine-pro-nano-lipospheres-on-direct-intestinal-phase-ii-metabolism-the-raloxifene-paradigm-of-enhanced-oral-bioavailability
#11
Dvora Izgelov, Irina Cherniakov, Gefen Aldouby Bier, Abraham J Domb, Amnon Hoffman
In recent years, Phase II metabolism, as a first pass metabolism process occurring to the parent drug, is gaining more and more attention. This is due to its acknowledged significance in drug development as well as drug-drug interactions. However, the predominant role of Phase I metabolism has always overshadowed Phase II metabolism, resulting in insufficient data regarding its mechanisms. In this paper, we investigate the effect of an advanced lipid based drug delivery system on Phase II metabolism at the intestinal level of the enterocytes monolayer...
March 14, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29503416/-effect-of-environmental-factors-on-the-ecotoxicity-of-pharmaceuticals-and-personal-care-products
#12
Kazumi Sugihara
 In recent years, pharmaceuticals and personal care products (PPCPs) have emerged as significant pollutants of aquatic environments and have been detected at levels in the range of ng/L to μg/L. The source of PPCPs is humans and livestock that have been administered pharmaceuticals and subsequently excreted them via urine and feces. Unlike agricultural chemicals, the environmental dynamics of PPCPs is not examined and they would undergo structural transformation by environmental factors, e.g., sunlight, microorganisms and treatments in sewage treatment plants (STPs)...
2018: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/29502066/-effects-of-raloxifene-at-two-different-doses-for-ovulation-induction-on-endometrial-pinopodes-in-mice-during-the-implantation-window
#13
Cai-Rong Chen, Qiu-Xia Yan, Xiu-Qin Zhou, Ying-Jie Xian, Xiao-Yan Guo, Song Quan
OBJECTIVE: To compare the expression of pinopodes, the marker of endometrial receptivity, during the implantation window in Kunming mice stimulated with two different doses of raloxifene (RAL). METHODS: Forty-eight 8-week-old female Kunming mice were randomly divided into 4 groups (n=12), namely saline group, clomiphene citrate (CC, 18 mg/kg) group, RAL (33 mg/kg) group and RAL (44 mg/kg group). In each group, the mice received intragastric administration of 1 mL of normal saline containing CC or RAL at the specified doses or saline only as indicated for ovulation induction, once daily for 2 days...
February 20, 2018: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/29501737/transdermal-delivery-of-raloxifene-hcl-via-ethosomal-system-formulation-advanced-characterizations-and-pharmacokinetic-evaluation
#14
Syed Mahmood, Uttam Kumar Mandal, Bappaditya Chatterjee
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method...
February 28, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29482944/synthesis-and-biological-evaluation-of-4-6-diaryl-2-pyrimidinamine-derivatives-as-anti-breast-cancer-agents
#15
Linyi Liu, Zhichao Tang, Chengze Wu, Xinyu Li, Ali Huang, Xiang Lu, Qidong You, Hua Xiang
Breast cancer is the most frequently diagnosed cancers and the leading causes of cancer death among females worldwide. Estrogen receptor positive has been identified as the predominant internal reasons, involving in more than 70% breast cancer patients and SERMs which competes with estradiol for the binding to ERα in breast tissue are widely used in the treatment of ER+ breast cancer, such as tamoxifen, raloxifene. However, many SERMs may cause negative side effects due to their estrogenic activity in other tissues and approximate 50% of patients with ER-positive tumors either initially do not respond or become resistant to these drugs...
December 30, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29467215/identification-of-intestinal-udp-glucuronosyltransferase-inhibitors-in-green-tea-camellia-sinensis-using-a-biochemometric-approach-application-to-raloxifene-as-a-test-drug-via-in-vitro-to-in-vivo-extrapolation
#16
Dan-Dan Tian, Joshua J Kellogg, Neşe Okut, Nicholas H Oberlies, Nadja B Cech, Danny D Shen, Jeannine S McCune, Mary F Paine
Green tea ( Camellia sinensis ) is a popular beverage worldwide, raising concern for adverse interactions when co-consumed with conventional drugs. Like many botanical natural products, green tea contains numerous polyphenolic constituents that undergo extensive glucuronidation. As such, the UDP-glucuronosyltransferases (UGTs), particularly intestinal UGTs, represent potential 'first-pass' targets for green tea-drug interactions. Candidate intestinal UGT inhibitors were identified using a biochemometrics approach, which combines bioassay and chemometric data...
February 21, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29428397/pyk2-deficiency-potentiates-osteoblast-differentiation-and-mineralizing-activity-in-response-to-estrogen-and-raloxifene
#17
Sumana Posritong, Jung Min Hong, Pierre P Eleniste, Patrick W McIntyre, Jennifer L Wu, Evan R Himes, Vruti Patel, Melissa A Kacena, Angela Bruzzaniti
Bone remodeling is controlled by the actions of bone-degrading osteoclasts and bone-forming osteoblasts (OBs). Aging and loss of estrogen after menopause affects bone mass and quality. Estrogen therapy, including selective estrogen receptor modulators (SERMs), can prevent bone loss and increase bone mineral density in post-menopausal women. Although investigations of the effects of estrogen on osteoclast activity are well advanced, the mechanism of action of estrogen on OBs is still unclear. The proline-rich tyrosine kinase 2 (Pyk2) is important for bone formation and female mice lacking Pyk2 (Pyk2-KO) exhibit elevated bone mass, increased bone formation rate and reduced osteoclast activity...
February 8, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29411304/efficacy-of-anti-osteoporotic-medications-in-patients-with-type-1-and-2-diabetes-mellitus-a-systematic-review
#18
REVIEW
Panagiotis Anagnostis, Stavroula A Paschou, Nifon N Gkekas, Aikaterini-Maria Artzouchaltzi, Konstantinos Christou, Dimitrios Stogiannou, Andromachi Vryonidou, Michael Potoupnis, Dimitrios G Goulis
PURPOSE: Both type 1 (T1DM) and type 2 diabetes mellitus (T2DM) have been associated with bone fragility and increased fracture risk. However, little is known regarding the effect of anti-osteoporotic treatment on bone mineral density (BMD) and/or fracture risk in these patients. We aimed to systematically investigate the efficacy of anti-osteoporotic medications in patients with diabetes in comparison with non-diabetic subjects. METHODS: MEDLINE and Scopus databases were searched (up to 31st October 2017)...
February 6, 2018: Endocrine
https://www.readbyqxmd.com/read/29395611/adjunctive-raloxifene-for-postmenopausal-women-with-schizophrenia-a-meta-analysis-of-randomized-double-blind-placebo-controlled-trials
#19
Xiao-Ming Zhu, Wei Zheng, Xiao-Hong Li, Dong-Bin Cai, Xin-Hu Yang, Gabor S Ungvari, Chee H Ng, Xiao-Ping Wang, Jayashri Kulkarni, Jasmin Grigg, Yu-Ping Ning, Yu-Tao Xiang
OBJECTIVE: Raloxifene, a selective estrogen receptor modulator, has been used in treating postmenopausal women with schizophrenia with inconsistent results. This meta-analysis of randomized, double-blind, placebo-controlled trials (RCTs) examined its efficacy and safety for postmenopausal women with schizophrenia. METHOD: Standardized mean differences (SMDs) and risk ratio (RR) together with their 95% confidence intervals (CIs) were calculated using the random effects model...
January 23, 2018: Schizophrenia Research
https://www.readbyqxmd.com/read/29340980/facile-synthesis-of-chitosan-capped-mesoporous-silica-nanoparticles-a-ph-responsive-smart-delivery-platform-for-raloxifene-hydrochloride
#20
Priya V Shah, Sadhana J Rajput
An encapsulation of model drug raloxifene hydrochloride (RAL) inside the chitosan decorated pH responsive mesoporous system has a greater potential for accumulating in the tumor cells. The present study involves synthesis of surface modified mesoporous silica nanoparticles (MSN) with the aim of achieving pH sensitive drug delivery system. A silanol skeleton of MSN has been productively modified to amine intermediate which served as a firm platform to adapt chitosan grafted assembly and systematically evaluated...
January 16, 2018: AAPS PharmSciTech
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