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Raloxifene

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https://www.readbyqxmd.com/read/29428397/pyk2-deficiency-potentiates-osteoblast-differentiation-and-mineralizing-activity-in-response-to-estrogen-and-raloxifene
#1
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
#2
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
#3
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
#4
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
https://www.readbyqxmd.com/read/29338533/enhanced-solubility-oral-bioavailability-and-anti-osteoporotic-effects-of-raloxifene-hcl-in-ovariectomized-rats-by-igepal-co-890-nanomicelles
#5
Jaleh Varshosaz, Vahab Ziaei, Mohsen Minaiyan, Ali Jahanian, Leila Seyed Tabatabaei
The purpose of the present study was to enhance the bioavailability and anti-osteoporotic effects of raloxifene HCl (RH) by increasing its solubility and inhibition of the p-glycoprotein-pump using surfactant micelles of Igepal CO-890. The micelles were prepared by the direct method and their critical micellar concentration, drug dissolution rate, saturated solubility, drug loading and surface morphology were defined. The cytotoxicity of Igepal CO-890 and its ability to inhibit the p-glycoprotein pump were studied on Caco-2 cells...
January 16, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29321530/the-effect-of-raloxifene-augmentation-in-men-and-women-with-a-schizophrenia-spectrum-disorder-a-systematic-review-and-meta-analysis
#6
REVIEW
Janna de Boer, Merel Prikken, Wan U Lei, Marieke Begemann, Iris Sommer
Recognizing the robust sex differences in schizophrenia prevalence, the selective estrogen receptor modulator (SERM) raloxifene is a likely candidate for augmentation therapy in this disorder. Therefore, a systematic search was performed using PubMed (Medline), Embase, PsychInfo, and Cochrane Database of Systematic Reviews. Randomized controlled trials investigating the effect of raloxifene in schizophrenia spectrum disorders were included in the quantitative analyses. Outcome measures were psychotic symptom severity, depression, and cognition...
January 10, 2018: NPJ Schizophrenia
https://www.readbyqxmd.com/read/29303860/mandibular-osteonecrosis-associated-with-raloxifene
#7
Hélder Antônio Rebelo Pontes, Lucas Lacerda de Souza, Daniel Cavalléro Colares Uchôa, João Mateus Mendes Cerqueira
Osteonecrosis is a disease with diverse pathophysiology, clinical presentation, and management. It may be associated with some medications used to treat systemic issues with bone metabolism. A few cases of jaw bone osteonecrosis have been associated with raloxifene. In this paper, the authors present a clinical report of a 64-year-old woman who presented with a necrosis foci in the right alveolar ridge of the mandible, associated with continued raloxifene use.
January 4, 2018: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/29298488/engineered-cellular-uptake-and-controlled-drug-delivery-using-two-dimensional-nanoparticle-and-polymer-for-cancer-treatment
#8
Sudipta Senapati, Rashmi Shukla, Arun Kumar Mahanta, Dipak Rana, Pralay Maiti, Yamini B Tripathi
Two major problems in chemotherapy, poor bioavailability of hydrophobic anti-cancer drug and its adverse side effects causing nausea, are taken into accounts by developing sustained drug release vehicle along with enhanced bioavailability using two-dimensional layered double hydroxides (LDHs) with appropriate surface charge and its subsequent embedment in polymer matrix. A model hydrophobic anti-cancer drug, raloxifene hydrochloride (RH), is intercalated into a series of zinc iron LDHs with varying anion charge densities using ion exchange technique...
January 4, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29237391/utility-of-pooled-cryopreserved-human-enterocytes-as-an-in-vitro-model-for-assessing-intestinal-clearance-and-drug-drug-interactions
#9
Zhengyin Yan, Susan Wong, Jane Kelly, Hoa Le, Ning Liu, Mika Kosaka, Suzanne Tey, Peter Vuong, Albert Li
A recent advancement in isolation and cryopreservation has resulted in commercially available primary human enterocytes that express various drug metabolizing enzymes (DMEs) and transporters. The main objective of this study was to further evaluate the utility of pooled cryopreserved enterocytes, specifically MetMax™ cryopreserved human enterocytes (In Vitro ADMET Laboratories), as an in vitro model for assessing intestinal clearance in comparison to hepatocytes. It was found that, for CYP3A4 substrates such as midazolam, amprenavir and loperamide, in vitro metabolic clearance is generally lower in enterocytes compared to that of hepatocytes, which is consistent with the relative abundance of the enzyme between the intestine and liver...
December 12, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29236162/bisphosphonates-prevent-age-related-weight-loss-in-japanese-postmenopausal-women
#10
Tomohiko Urano, Masataka Shiraki, Tatsuhiko Kuroda, Shiro Tanaka, Fumihiko Urano, Kazuhiro Uenishi, Satoshi Inoue
Decline of body weight with aging is a major risk factor for frailty, osteoporosis and fracture, suggesting that treatment for osteoporosis may affect body composition. Recently, we have shown that 5-year treatment with raloxifene prevented age-related weight loss, suggesting some other drugs for osteoporosis may also prevent a decrease in body weight with aging. The present study aimed to identify the relationship between bisphosphonate treatment and body composition markers. We measured bone mineral density (BMD), body composition, and bone remodeling markers in 551 Japanese postmenopausal women with bisphosphonate treatment, which included risedronate or alendronate treatment (BP-treatment group; N = 193) and without treatment by any osteoporosis drug (no-treatment group; N = 358) for 4-7 years (mean observation periods; 5...
December 13, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29229198/combined-raloxifene-and-letrozole-for-breast-cancer-patients
#11
Divya Vohora, Abul Kalam, Ankita Leekha, Sushama Talegaonkar, Anita Kamra Verma
Raloxifene, an anti-osteoporotic drug, is recently approved for prevention of breast cancer in postmenopausal women and thus the drug may be employed to combat the bony adverse effects of letrozole, another anticancer drug. However, the cytotoxic effect of their combination on human breast cancer (MCF-7) and human embryonic kidney (HEK) cell lines is not known. MCF-7 and HEK cell lines were treated with different graded doses of letrozole, raloxifene and their combination, then incubated for 24-48 h. MTT assay was performed to check the cytotoxicity of the drugs...
December 8, 2017: Archives of Medical Research
https://www.readbyqxmd.com/read/29227547/a-network-meta-analysis-on-the-short-term-efficacy-and-adverse-events-of-different-anti-osteoporosis-drugs-for-the-treatment-of-postmenopausal-osteoporosis
#12
Gui-Feng Liu, Zong-Qiang Wang, Lin Liu, Bu-Tian Zhang, Ying-Ying Miao, Shao-Nan Yu
A network meta-analysis was conducted to compare the short-term efficacy and adverse events of different drugs for the treatment of postmenopausal osteoporosis (PMO), providing a more effective treatment for PMO. We initially searched through various databases like PubMed, Cochrane Library and EMBASE from inception till October 2016. All randomized controlled trials (RCTs) of drugs for the treatment of PMO were included for direct and indirect comparison. A combination of direct and indirect evidence of different inhibitors of antidiabetic drugs for treatment of PMO were considered for calculating the weighted mean difference (WMD) value or odd ratio (OR) value and to draw surface under the cumulative ranking (SUCRA) curves...
December 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29214794/retraction-paper-comparison-of-effects-of-alendronate-and-raloxifene-on-lumbar-bone-mineral-density-bone-turnover-and-lipid-metabolism-in-elderly-women-with-osteoporosis-by-iwamoto-j-et-al-yonsei-med-j-2008-49-1-119-128
#13
https://www.readbyqxmd.com/read/29210666/a-newly-synthetized-ferrocenyl-derivative-selectively-induces-apoptosis-in-all-lymphocytes-through-mitochondrial-estrogen-receptors
#14
Marjan Aghvami, Jalal Pourahmad, Afshin Zarghi, Peyman Eshghi, Mohammad Hadi Zarei, Shabnam Farzaneh, Fatemeh Sattari
BACKGROUND: Estrogens, as the main female steroid hormones have multiple proven effects on reproductive and non- reproductive systems. Expression of ERα and ERβ, two dominant estrogen receptors, in peripheral blood mononuclear cells in certain B-cell malignancies and the existence of estrogens receptors on mitochondria is open to question that estrogen likely has an impact on the cancerous lymphocytes life span. Acute lymphoblastic leukemia (ALL) is the frequent pediatric malignity which is recurrent and hardly curable in many cases...
December 5, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29199359/risk-of-venous-thromboembolism-among-users-of-different-anti-osteoporosis-drugs-a-population-based-cohort-analysis-including-over-200-000-participants-from-spain-and-the-uk
#15
E Martín-Merino, I Petersen, S Hawley, A Álvarez-Gutierrez, S Khalid, A Llorente-Garcia, A Delmestri, M K Javaid, T P Van Staa, A Judge, C Cooper, D Prieto-Alhambra
The venous thromboembolism risk among anti-osteoporotics is unknown. In this primary care study, the risk with other bisphosphonates [1.05 (0.94-1.18) and 0.96 (0.78-1.18)], strontium [0.90 (0.61-1.34) and 1.19 (0.82-1.74)], in the UK and Spain respectively, and denosumab [1.77 (0.25-12.66)] and teriparatide [1.27 (0.59-2.71)] in Spain, did not differ versus alendronate. INTRODUCTION: Most of the known adverse drug reactions described for anti-osteoporosis medication (AOM) have been described in studies comparing AOM users to non-users...
December 3, 2017: Osteoporosis International
https://www.readbyqxmd.com/read/29198613/mechanochemically-induced-solid-state-transformations-the-case-of-raloxifene-hydrochloride
#16
Yara Santiago de Oliveira, Alcemira Conceição Oliveira, Alejandro Pedro Ayala
Raloxifene hydrochloride is a benzothiophene derivative mainly used in the prevention and treatment of osteoporosis, but exhibits a low bioavailability hindered by its poor water solubility. In this study, a mechanochemical approach based on neat and liquid-assisted grinding was applied to produce new solid forms of raloxifene hydrochloride. The solids obtained were characterized by several solid-state techniques, such as powder X-ray diffraction, thermal analysis, infrared and Raman spectroscopy. These results showed that depending on the processing conditions solvated or amorphous forms can be produced...
November 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29196083/the-good-and-the-bad-about-the-2017-american-college-of-physicians-osteoporosis-guidelines
#17
Violet Lagari, Tara Gavcovich, Silvina Levis
PURPOSE: The American College of Physicians (ACP) published a set of guidelines on how to prevent fractures in men and women with low bone density or osteoporosis. As the population ages, the overall risk of fractures increases, thus burdening the health care system. These guidelines review current evidence for osteoporosis management, providing an update to the previous 2008 ACP's guidelines. METHODS: The ACP put forth 6 recommendations addressing the complexities in osteoporosis management based on evidence available through October 2016 with a focus on bisphosphonates, calcium, vitamin D, and estrogen...
January 2018: Clinical Therapeutics
https://www.readbyqxmd.com/read/29196024/poly-methyl-vinyl-ether-co-maleic-acid-for-enhancement-of-solubility-oral-bioavailability-and-anti-osteoporotic-effects-of-raloxifene-hydrochloride
#18
Jaleh Varshosaz, Mohsen Minaiyan, Ladan Dayyani
Raloxifene HCl (RH) has poor water solubility and due to its extensive first pass metabolism; its bioavailability is only 2%. The purpose of the present study was to enhance the aqueous solubility, oral bioavailability and anti-osteoporotic effects of RH by electro-sprayed nanoparticles (NPs) in ovariectomized rats. NPs containing RH and different ratio of poly(methyl vinyl ether-co-maleic acid) (PMVEMA) were electrosprayed. The voltage, distance of needle to the collector, flow rate of the solution and polymeric percentage were optimized according to the size of NPs and drug solubility...
January 15, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29194351/identification-of-a-raloxifene-analog-that-promotes-ahr-mediated-apoptosis-in-cancer-cells
#19
Hyo Sang Jang, Martin Pearce, Edmond F O'Donnell, Bach Duc Nguyen, Lisa Truong, Monica J Mueller, William H Bisson, Nancy I Kerkvliet, Robert L Tanguay, Siva Kumar Kolluri
We previously reported that raloxifene, an estrogen receptor modulator, is also a ligand for the aryl hydrocarbon receptor (AhR). Raloxifene induces apoptosis in estrogen receptor-negative human cancer cells through the AhR. We performed structure-activity studies with seven raloxifene analogs to better understand the structural requirements of raloxifene for induction of AhR-mediated transcriptional activity and apoptosis. We identified Y134 as a raloxifene analog that activates AhR-mediated transcriptional activity and induces apoptosis in MDA-MB-231 human triple negative breast cancer cells...
December 1, 2017: Biology
https://www.readbyqxmd.com/read/29181706/self-assembling-raloxifene-loaded-mixed-micelles-formulation-optimization-in-vitro-cytotoxicity-and-in-vivo-pharmacokinetics
#20
Radhika Kanade, Mithila Boche, Varsha Pokharkar
Raloxifene (RLX) has been strongly recommended for postmenopausal women at high risk of invasive breast cancer and for prevention of osteoporosis. However, low aqueous solubility and reduced bioavailability hinder its clinical application. The objective of this study was to explore the potential of RLX loaded mixed micelles (RLX-MM) using Pluronic F68 and Gelucire 44/14 for enhanced bioavailability and improved anticancer activity on human breast cancer cell line (MCF-7). RLX-MM were prepared by solvent evaporation method and optimized using 32 factorial design...
November 27, 2017: AAPS PharmSciTech
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