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https://www.readbyqxmd.com/read/28223020/synthesis-and-evaluation-of-prodrugs-of-corticotropin-releasing-factor-1-crf1-receptor-antagonist-bms-665053-leading-to-improved-oral-bioavailability
#1
Richard A Hartz, Vivekananda M Vrudhula, Vijay T Ahuja, James E Grace, Nicholas J Lodge, Joanne J Bronson, John E Macor
A series of phosphate and ester-based prodrugs of anilinopyrazinone 1 (BMS-665053) containing either a methylene or an (acyloxy)alkoxy linker was prepared and evaluated in rat pharmacokinetic studies with the goal of improving the oral bioavailability of the parent (1). The prodrugs, in general, had improved aqueous solubility and oral bioavailability compared to 1. Prodrug 12, which contains an (acyloxy)alkoxy linker, showed the greatest improvement in the oral bioavailability relative to the parent (1), with a seven-fold increase (from 5% to 36%) in rat pharmacokinetic studies...
February 10, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216278/outcomes-of-patients-with-metastatic-renal-cell-carcinoma-and-bone-metastases-in-the-targeted-therapy-era
#2
Sarathi Kalra, Jonathan Verma, Bradley J Atkinson, Surena F Matin, Christopher G Wood, Jose A Karam, Sue-Hwa Lin, Robert L Satcher, Pheroze Tamboli, Kanishka Sircar, Priya Rao, Paul G Corn, Nizar M Tannir, Eric Jonasch
BACKGROUND: Bone metastases (BMs) occur commonly in patients with metastatic renal cell carcinoma (mRCC). Tyrosine kinase inhibitors (TKIs) have improved the outcomes for patients with mRCC. However, data on the outcomes of mRCC patients with BMs treated with TKIs are limited. We describe the outcomes of patients with BMs treated with TKI therapy and compare them with the outcomes from a pre-TKI group. PATIENTS AND METHODS: Using an institutional tumor registry, a retrospective review of patients with mRCC from 2002 to 2003 and 2006 to 2007 was performed...
January 18, 2017: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/28215414/meta-analysis-of-comparison-of-drug-eluting-stents-and-bare-metal-stents-in-patients-on-dialysis
#3
Shan Li, Dan Ye, Guoping Chen, Weiwei Xu
Coronary artery disease is common in patients with end-stage renal disease who are on hemodialysis. The efficacy and safety of evidence regarding the use of drug-eluting stents (DES) and bare-metal stents (BMS) in patients with dialysis is unclear. We searched MEDLINE, EMBASE, Science Citation Index, CINAHL, and the Cochrane CENTRAL database of controlled clinical trials for controlled trials that compare DES and BMS in dialysis patients up to June 2016. We conducted a meta-analysis across 14 eligible studies (n = 62,250 patients)...
January 25, 2017: American Journal of Cardiology
https://www.readbyqxmd.com/read/28199919/relationships-between-oral-muc1-expression-and-salivary-hormones-in-burning-mouth-syndrome
#4
Jeong-Hyun Kang, Yoon-Young Kim, Ji-Youn Chang, Hong-Seop Kho
OBJECTIVES: To investigate possible relationships among oral mucosal epithelial MUC1 expression, salivary female gonadal hormones and stress markers, and clinical characteristics in patients with burning mouth syndrome (BMS). DESIGN: Thirty post-menopausal female patients with BMS (60.0±5.0 years) were included. Clinical and psychological evaluations were performed and the expression level of oral mucosal epithelial MUC1 was analyzed. The levels of cortisol, dehydroepiandrosterone (DHEA), 17β-estradiol, progesterone, chromogranin A, and blood contamination were determined from unstimulated whole saliva (UWS) and stimulated whole saliva (SWS) samples...
February 4, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/28197276/percutaneous-coronary-intervention-safety-of-methotrexate-and-its-possible-benefits-on-restenosis-after-bare-metal-stent-deployment
#5
Viviane Gouveia, Dinaldo C Oliveira, Emmanuele Tenorio, Norma Brito, Emanuel Sarinho
BACKGROUND: Percutaneous coronary intervention (PCI) revolutionized treatment of coronary artery disease. Drug-eluting stents are effective and safe but their cost is high, especially for some countries. The primary objective was to evaluate the safety of methotrexate (MTX) in patients who underwent PCI and the secondary goal was to evaluate the possibility that MTX has an impact on restenosis. METHODS: This was a transversal, prospective and descriptive study that recruited 16 patients in whom PCI was planned...
June 2016: Cardiology Research
https://www.readbyqxmd.com/read/28193005/mapping-the-energetic-epitope-of-an-antibody-interleukin-23-interaction-with-hydrogen-deuterium-exchange-fast-photochemical-oxidation-of-proteins-mass-spectrometry-and-alanine-shave-mutagenesis
#6
Jing Li, Hui Wei, Stanley R Krystek, Derek Bond, Ty M Brender, Daniel Cohen, Jena Feiner, Nels Hamacher, Johanna Harshman, Richard Y-C Huang, Susan H Julien, Zheng Lin, Kristina Moore, Luciano Mueller, Claire Noriega, Preeti Sejwal, Paul Sheppard, Brenda Stevens, Guodong Chen, Adrienne A Tymiak, Michael L Gross, Lumelle A Schneeweis
Epitope mapping the specific residues of an antibody/antigen interaction can be used to support mechanistic interpretation, antibody optimization, and epitope novelty assessment. Thus, there is a strong need for mapping methods, particularly integrative ones. Here, we report the identification of an energetic epitope by determining the interfacial hot-spot that dominates the binding affinity for an anti-interleukin-23 (anti-IL-23) antibody by using the complementary approaches of hydrogen/deuterium exchange mass spectrometry (HDX-MS), fast photochemical oxidation of proteins (FPOP), alanine shave mutagenesis, and binding analytics...
February 9, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28191875/clinical-outcomes-with-the-stentys-self-apposing-coronary-stent-in-patients-presenting-with-st-segment-elevation-myocardial-infarction-2-year-insights-from-the-appostion-iii-a-post-market-registry-to-assess-the-stentys-self-expanding-coronary-stent-in-acute
#7
Huangling Lu, Maik J Grundeken, Nicola S Vos, Alexander J J Ijsselmuiden, Robert-Jan van Geuns, Rainer Wessely, Thomas Dengler, Alessio La Manna, Johanne Silvain, Gilles Montalescot, René Spaargaren, Jan G P Tijssen, Giovanni Amoroso, Robbert J de Winter, Karel T Koch
AIMS: The APPOSITION III registry evaluated the feasibility and performance of the STENTYS self- apposing stent in a ST-segment elevation myocardial infarction (STEMI) population. This novel self- apposing stent device lowers stent strut malapposition rates and therefore bears the potential to prevent stent undersizing during primary percutaneous coronary intervention (PCI) in STEMI patients. Up to date, no long-term data is available using this device in the setting of STEMI. We aimed to evaluate long-term clinical outcomes of the APPOSITION III registry...
February 14, 2017: EuroIntervention
https://www.readbyqxmd.com/read/28185978/long-term-serial-changes-in-platelet-activation-indices-following-sirolimus-eluting-and-bare-metal-stents-implantation-in-patients-with-stable-coronary-artery-disease
#8
Maria Marketou, George E Kochiadakis, Aikaterini Giaouzaki, Katerini Sfiridaki, Stelios Petousis, Fragiskos Maragoudakis, Konstantinos Roufas, Despoina Vougia, John Logakis, Gregory Chlouverakis, Panos E Vardas
BACKGROUND: Platelet activation is crucial in the development of stent thrombosis following percutaneous coronary intervention (PCI). We carried out a long-term assessment of multiple factors implicated in the thrombotic process and markers of platelet activation, after implantation of sirolimus-eluting stents (SES) in patients with stable coronary artery disease (CAD), and we compared the results with those after bare-metal stent (BMS) implantation. METHODS: Forty-seven consecutive patients, aged <70 years, with severe stenosis (>70% narrowing of the lumen) of one major epicardial coronary artery and stable CAD, underwent successful elective PCI and were randomly allocated to SES (n=25) or BMS (n=22)...
February 6, 2017: Hellenic Journal of Cardiology: HJC, Hellēnikē Kardiologikē Epitheōrēsē
https://www.readbyqxmd.com/read/28185793/establishment-of-an-adjusted-prognosis-analysis-model-for-initially-diagnosed-non-small-cell-lung-cancer-with-brain-metastases-from-sun-yat-sen-university-cancer-center
#9
Xiao-Xiao Dinglin, Shu-Xiang Ma, Fang Wang, De-Lan Li, Jian-Zhong Liang, Xin-Ru Chen, Qing Liu, Yin-Duo Zeng, Li-Kun Chen
BACKGROUND: The current published prognosis models for brain metastases (BMs) from cancer have not addressed the issue of either newly diagnosed non-small-cell lung cancer (NSCLC) with BMs or the lung cancer genotype. We sought to build an adjusted prognosis analysis (APA) model, a new prognosis model specifically for NSCLC patients with BMs at the initial diagnosis using adjusted prognosis analysis (APA). PATIENTS AND METHODS: The model was derived using data from 1158 consecutive patients, with 837 in the derivation cohort and 321 in the validation cohort...
January 13, 2017: Clinical Lung Cancer
https://www.readbyqxmd.com/read/28185168/polymer-free-drug-coated-coronary-stents-in-patients-with-stable-coronary-artery-disease-at-high-bleeding-risk
#10
REVIEW
Hemang B Panchal, Ramesh Daggubati, David Zhao, Sunil V Rao, Timir Paul
PURPOSE OF REVIEW: Patients with stable coronary artery disease (CAD) and a high risk of bleeding are not ideal candidates for a polymer-based drug-eluting stent (DES) because it requires 6-12 months of dual antiplatelet therapy (DAPT) following percutaneous coronary intervention (PCI). The purpose of this review is to assess the angiographic and clinical outcomes of polymer-free drug-coated stents (PF-DCS) in stable CAD patients with a high bleeding risk. RECENT FINDINGS: Several randomized controlled trials (RCTs) have compared angiographic and clinical outcomes of PF-DCS with bare-metal stents (BMS), permanent polymer (PP)-DES, or biodegradable polymer (BP)-DES...
February 2017: Current Cardiology Reports
https://www.readbyqxmd.com/read/28174212/drug-eluting-stents-versus-bare-metal-stents-in-acute-myocardial-infarction-with-cardiogenic-shock
#11
Jakob Ledwoch, Georg Fuernau, Steffen Desch, Ingo Eitel, Christian Jung, Suzanne de Waha, Janine Poess, Steffen Schneider, Gerhard Schuler, Karl Werdan, Uwe Zeymer, Holger Thiele
OBJECTIVES: The aim of the present study was to assess the outcome of patients with acute myocardial infarction (AMI) complicated by cardiogenic shock (CS) receiving drug-eluting stents (DES) compared with bare-metal stents (BMS). Data comparing these two stent technologies in AMI with CS were limited. METHODS: A total of 783 patients with AMI and CS undergoing early revascularisation were included in the randomised Intra-aortic Balloon Pump in Cardiogenic Shock II trial (n=600) and the associated registry (n=183)...
February 7, 2017: Heart: Official Journal of the British Cardiac Society
https://www.readbyqxmd.com/read/28168885/methylnaltrexone-versus-naloxone-for-opioid-induced-constipation-in-the-medical-intensive-care-unit
#12
Cristian Merchan, Diana Altshuler, John Papadopoulos
BACKGROUND: Opioid-induced constipation (OIC) is common in critically ill patients; it leads to complications that can increase hospital stay and, rarely, bowel perforation. Opioid antagonists are considered a logical approach to treat OIC; however, the agent of choice has yet to be determined. OBJECTIVE: To assess the effectiveness and safety of enteral naloxone (NTX) versus subcutaneous methylnaltrexone (MNTX) for the treatment of OIC in the medical intensive care unit...
March 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28168845/beyond-restenosis-patients-preference-for-drug-eluting-or-bare-metal-stents
#13
Mohammed Qintar, Adnan K Chhatriwalla, Suzanne V Arnold, Fengming Tang, Donna M Buchanan, Ali Shafiq, Yashashwi Pokharel, Dave deBronkart, Javed M Ashraf, John A Spertus
OBJECTIVES: To assess patients' perspective about factors associated with stent choice. BACKGROUND: Drug eluting stents (DES) markedly reduce the risk of repeat percutaneous coronary intervention (PCI), but necessitate a longer duration of dual anti-platelet therapy (DAPT) as compared with bare metal stents (BMS). Thus, understanding patients' perspective about factors associated with stent choice is paramount. METHODS: Patients undergoing angiography rated, on a 10-point scale, the importance (1 = not important, 10 = most important) of avoiding repeat revascularization and avoiding the following potential DAPT drawbacks: bleeding/bruising, more pills/day, medication costs and delaying elective surgery...
February 7, 2017: Catheterization and Cardiovascular Interventions
https://www.readbyqxmd.com/read/28163269/successful-endovascular-treatment-of-aortoiliac-bifurcation-stenosis-using-an-empirically-based-t-and-protrude-stenting-with-self-and-balloon-expandable-stents
#14
Ken-Ichiro Sasaki, Hidetoshi Chibana, Takafumi Ueno, Naoki Itaya, Masahiro Sasaki, Yoshihiro Fukumoto
A 73-year-old woman with arteriosclerosis obliterans (ASO) was underwent a crossover stenting for an aortoiliac bifurcation from the right common iliac artery (CIA) with a self-expandable bare-metal stent (SE-BMS); however, a new stenosis later occurred just behind the bifurcation of the left CIA. An ex vivo experiment demonstrated that culotte-stenting by additional implantation of a balloon-expandable bare-metal stent (BE-BMS) through stent struts of the SE-BMS would be empirically infeasible. Although we had initially planned a T-stenting for the additional implantation of a BE-BMS in the left CIA, we finally deployed the stent in the CIA with the proximal end protruding into the previously-implanted SE-BMS through the stent struts to avoid incomplete coverage of the stenosis by reference to the ex vivo experiments...
February 6, 2017: Kurume Medical Journal
https://www.readbyqxmd.com/read/28161258/pathology-of-chronic-total-occlusion-in-bare-metal-versus-drug-eluting-stents-implications-for-revascularization
#15
Hiroyoshi Mori, Christoph Lutter, Kazuyuki Yahagi, Emanuel Harari, Robert Kutys, David R Fowler, Elena Ladich, Michael Joner, Renu Virmani, Aloke V Finn
OBJECTIVES: The aim of this study was to explore the pathology of in-stent chronic total occlusion (IS-CTO) in bare-metal (BMS) versus drug-eluting stents (DES). BACKGROUND: Despite a relatively high prevalence of IS-CTO, little is known about the underlying etiology and histopathologic characteristics of the occlusion. METHODS: From CVPath Institute's stent registry of human native coronary arteries, the authors identified 56 lesions (32 BMS and 24 DES) from 54 patients with IS-CTO...
January 25, 2017: JACC. Cardiovascular Interventions
https://www.readbyqxmd.com/read/28155628/matrix-gelatinases-in-atherosclerosis-and-diabetic-nephropathy-progress-and-challenges
#16
Grigorios G Dimas, Triantafyllos P Didangelos, Dimitrios M Grekas
Matrix metalloproteinases (MMPs) are zinc-dependent proteases that degrade components of the extracellular matrix (ECM). In glomerular disease, MMPs are major regulators of ECM degradation as well as structural and functional integrity in the glomerulus. In altered matrix composition diseases, glomerular damage is due to increased degradation of kidney and vessel basement membranes (BMs) by MMPs. MMP -2 and -9 are both considered as the main enzymes that degrade collagen type-IV (coll-IV), which represents the key collagenous component of ECM and constitutes the architectural structure of vessels and glomerular BM...
February 2, 2017: Current Vascular Pharmacology
https://www.readbyqxmd.com/read/28154600/the-control-of-drug-release-and-vascular-endothelialization-after-hyaluronic-acid-coated-paclitaxel-multi-layer-coating-stent-implantation-in-porcine-coronary-restenosis-model
#17
In-Ho Bae, Myung Ho Jeong, Ju Han Kim, Yong Hwan Park, Kyung Seob Lim, Dae Sung Park, Jae Won Shim, Jung Ha Kim, Youngkeun Ahn, Young Joon Hong, Doo Sun Sim
BACKGROUND AND OBJECTIVES: Hyaluronic acid (HA) is highly biocompatible with cells and the extracellular matrix. In contrast to degradation products of a synthetic polymer, degradation products of HA do not acidify the local environment. The aim of this study was to fabricate an HA-coated paclitaxel (PTX)-eluting stent via simple ionic interactions and to evaluate its effects in vitro and in vivo. MATERIALS AND METHODS: HA and catechol were conjugated by means of an activation agent, and then the stent was immersed in this solution (resulting in a HA-coated stent)...
January 2017: Korean Circulation Journal
https://www.readbyqxmd.com/read/28154599/effect-of-stents-coated-with-artemisinin-or-dihydroartemisinin-in-a-porcine-coronary-restenosis-model
#18
Suyoung Jang, Myung Ho Jeong, Kyung Seob Lim, In Ho Bae, Jun-Kyu Park, Dae Sung Park, Jae Won Shim, Jung Ha Kim, Hyun Kuk Kim, Doo Sun Sim, Young Joon Hong, Youngkeun Ahn, Jung Chaee Kang
BACKGROUND AND OBJECTIVES: Artemisinin and dihydroartemisinin are drugs used to treat malaria. These drugs suppress inflammatory reactions. The aim of this study was to examine the anti-intima hyperplasia effect of a novel drug-eluting stent with artemisinin or dihydroartemisinin in a porcine coronary restenosis model. MATERIALS AND METHODS: Pigs were randomized into four groups; in the first, the coronary arteries (20 pigs, a total of 40 coronary arteries, with 10 coronary arteries in each group) was implanted with bare metal stents (BMS, n=10); the second group was given polymer-coated stents (PCS, n=10); the third group was treated with artemisinin-eluting stents (AES, n=10); and the fourth group was given dihydroartemisinin-eluting stents (DAES, n=10)...
January 2017: Korean Circulation Journal
https://www.readbyqxmd.com/read/28153215/the-interrelationship-between-sleep-and-depression-a-secondary-analysis-of-a-randomized-controlled-trial-on-mind-body-spirit-intervention
#19
Xiao Wen Ji, Celia H Y Chan, Bobo H P Lau, Jessie S M Chan, Cecilia L W Chan, Ka-Fai Chung
OBJECTIVES: To conduct a secondary analysis of a randomized controlled trial (RCT) that aims to understand the mediating effects embedded in a mind-body-spirit intervention for sleep and mood disturbances. METHODS: 126 adults with mild to moderate depression and subjective sleep disturbance, defined as Center for Epidemiologic Studies Depression Scale (CESD) scores from 10 to 34 and Pittsburgh Sleep Quality Index (PSQI) score > 5, participated in a waitlist-controlled RCT of an integrative mind-body-spirit intervention (I-BMS)...
January 2017: Sleep Medicine
https://www.readbyqxmd.com/read/28149758/defining-the-endpoints-how-to-measure-the-efficacy-of-drugs-that-are-active-against-central-nervous-system-metastases
#20
REVIEW
Alessandra Fabi, Antonello Vidiri
Brain metastases (BMs) are the most common cause of malignant central nervous system (CNS) tumors in adults. In the recent past, patients with BMs were excluded from clinical trials, but now, with the advent of new biological and immunological drugs, their inclusion is more common. In the last era response and progression criteria used across clinical trials have defined the importance to consider not only measurement changes of brain lesions but also the modification of parameters related to the metastases such as metabolism of tissue and its pathological features...
December 2016: Translational Lung Cancer Research
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