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https://www.readbyqxmd.com/read/28326559/a-phase-1-study-to-evaluate-the-safety-and-ldl-cholesterol-lowering-effects-of-rg7652-a-fully-human-monoclonal-antibody-against-proprotein-convertase-subtilisin-kexin-type-9
#1
Amos Baruch, Diana Luca, Robert S Kahn, Kyra J Cowan, Maya Leabman, Nageshwar R Budha, Cecilia P C Chiu, Yan Wu, Daniel Kirchhofer, Andrew Peterson, John C Davis, Whittemore G Tingley
BACKGROUND: Proprotein convertase subtilisin/kexin type 9 (PCSK9) downregulates low-density lipoprotein (LDL) receptors, thereby leading to a rise in circulating LDL cholesterol (LDL-C). RG7652 is a fully human monoclonal antibody against PCSK9. This placebo-controlled, phase 1 ascending-dose study in healthy subjects evaluated the safety of RG7652 and its efficacy as a potential LDL-C-lowering drug. HYPOTHESIS: Anti-PCSK9 antibody therapy safely and effectively reduces LDL-C...
March 22, 2017: Clinical Cardiology
https://www.readbyqxmd.com/read/28322941/small-dosing-clinical-study-pharmacokinetic-pharmacogenomic-slco2b1-and-abcg2-and-interaction-atorvastatin-and-grapefruit-juice-profiles-of-five-probes-for-oatp2b1-and-bcrp
#2
Yushi Kashihara, Ichiro Ieiri, Takashi Yoshikado, Maeda Kazuya, Masato Fukae, Miyuki Kimura, Takeshi Hirota, Shunji Matsuki, Shin Irie, Noritomo Izumi, Hiroyuki Kusuhara, Yuichi Sugiyama
The aims of this study were (1) to investigate the effects of atorvastatin (10 mg, therapeutic dose) and grapefruit juice (GFJ), inhibitors of OATP2B1, on the pharmacokinetics of substrates for OATP2B1 and BCRP under oral small-dosing conditions (300 μg sulfasalazine, 250 μg rosuvastatin, 300 μg glibenclamide, 1200 μg celiprolol, and 600 μg sumatriptan), and (2) to evaluate the contribution of SLCO2B1*3 and ABCG2 c.421C>A polymorphisms to the pharmacokinetics of the five test drugs in 23 healthy volunteers...
March 17, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28321019/myocardial-infarction-in-a-young-man-with-nephrotic-syndrome
#3
Zhenliang Chu, Hang Zhu, Bin Zhang, Liqin Jiang
A 26-year-old man diagnosed with nephrotic syndrome (NS) 2 years previously presented with chest pain. An electrocardiogram (ECG) performed at a local hospital showed ST-elevation in chest leads. Cardiac troponin-I was significantly positive. Echocardiography revealed mild regional wall-motion abnormalities in the heart apex. Seven days later, angiography (CAG) revealed a thrombus in the left anterior descending branch (LAD). Tirofiban was injected into the LAD for thromboclasis. ECG after CAG showed the ST-segment was much lower than before...
March 17, 2017: International Heart Journal
https://www.readbyqxmd.com/read/28319303/synthesis-of-indoles-and-pyrroles-utilizing-iridium-carbenes-generated-from-sulfoxonium-ylides
#4
Janakiram Vaitla, Annette Bayer, Kathrin H Hopmann
Metal carbenes can undergo a myriad of synthetic transformations. Sulfur ylides are potential safe precursors of metal carbenes. Herein, we report cascade reactions that involve carbenoids derived from sulfoxonium ylides for the efficient and regioselective synthesis of indoles and pyrroles. The tandem action of iridium and Brønsted acid catalysts enables rapid assembly of the heterocycles from unmodified anilines or readily accessible enamines under microwave irradiation. The key mechanistic steps are the catalytic transformation of the sulfoxonium ylide into an iridium-carbene complex, followed by N-H or C-H functionalization of an aniline or enamine, respectively, and a final acid-catalyzed cyclization...
March 20, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28318833/bibliometric-analysis-of-the-scientific-production-as-regards-statin-use-for-ophthalmological-symptoms-of-myasthenia-gravis
#5
S M Salado-Font, F López-Muñoz, F J Povedano-Montero, F Labella Quesada
INTRODUCTION: The first symptoms of myasthenia gravis (MG) usually involve weakness of the ocular muscles, making it relevant that ophthalmologists have updated information on studies as regards its relationship with the consumption of drugs, such as statins. MATERIALS AND METHODS: A bibliometric analysis was performed using the Scopus database and by a search strategy in the selection of documents containing descriptors related to statins in the «Title» («TI») field and the descriptors «ophthalm *', «myast *', «visual *' in other fields of the document (period 1986-2015)...
March 16, 2017: Archivos de la Sociedad Española de Oftalmología
https://www.readbyqxmd.com/read/28318515/effect-of-dose-and-timing-of-preoperative-statins-on-mortality-after-coronary-artery-bypass-surgery
#6
Michael Curtis, Yi Deng, Vei-Vei Lee, MacArthur A Elayda, Joseph S Coselli, Charles D Collard, Wei Pan
BACKGROUND: Preoperative statin administration is associated with reduced mortality risk after a coronary artery bypass graft operation. However, the optimal dose and timing are unknown. METHODS: We retrospectively reviewed data from 3,025 primary isolated coronary artery bypass graft surgery patients at our institution. Patients were divided into three groups, according to timing of their preoperative statin: 24 hours or less (n = 1,788), 24 to 72 hours (n = 452), or more than 72 hours before operation or no dose (n = 781)...
March 15, 2017: Annals of Thoracic Surgery
https://www.readbyqxmd.com/read/28315329/atorvastatin-prevents-angiotensin-ii-induced-myocardial-hypertrophy-in%C3%A2-vitro-via-ccaat-enhancer-binding-protein-%C3%AE
#7
Yintao Chen, Shasha Yu, Naijin Zhang, Yuan Li, Shuang Chen, Ye Chang, Guozhe Sun, Yingxian Sun
Previous evidences suggested that atorvastatin not only reduced blood lipids but also reduced myocardial hypertrophy and remodeling. And it was reported that C/EBPβ (CCAAT/enhancer-binding protein β) played a pivotal role both in the physiologic and pathological cardiac hypertrophy. However, it has not been reported before whether this signaling pathway of C/EBPβ participates in protective effect of atorvastatin for hypertrophy cardiomyocytes. In present study, We found that overexpression of C/EBPβ significantly abrogated the effect of atorvastatin on increasing Bcl-2/Bax and PGC-1α while the early and late apoptosis rate increased and mitochondrial membrane potential (MMP) was reduced...
March 15, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28314859/effects-of-cetp-inhibition-with-anacetrapib-on-metabolism-of-vldl-tg-and-plasma-apolipoproteins-c-ii-c-iii-and-e
#8
John S Millar, Michael E Lassman, Tiffany Thomas, Rajasekhar Ramakrishnan, Patricia Jumes, Richard L Dunbar, Emile M deGoma, Amanda L Baer, Wahida Karmally, Daniel S Donovan, Hashmi Rafeek, John A Wagner, Stephen Holleran, Joseph Obunike, Yang Liu, Soumia Aoujil, Taylor Standiford, David E Gutstein, Henry N Ginsberg, Daniel J Rader, Gissette Reyes-Soffer
Cholesteryl ester transfer protein (CETP) mediates the transfer of HDL cholesteryl esters(CE) for TG in VLDL/LDL. CETP inhibition, with anacetrapib, increases HDL-cholesterol(C), reduces LDL-C and lowers TG levels. This study describes the mechanisms responsible for TG lowering by examining the kinetics of VLDL-TG and apolipoproteins (apo) C-II, C-III, and E. Hypercholesterolemic subjects were randomized to either placebo(N=10) or atorvastatin 20 mg/qd(N=29) for 4 weeks(period 1) followed by 8-weeks of anacetrapib, 100 mg/qd(period 2)...
March 17, 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/28314732/correction-to-intracellular-unbound-atorvastatin-concentrations-in-the-presence-of-metabolism-and-transport
#9
(no author information available yet)
No abstract text is available yet for this article.
April 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28302660/rhabdomyolysis-induced-compartment-syndrome-secondary-to-atorvastatin-and-strenuous-exercise
#10
Louise Dunphy, Rossel Morhij, Sarah Tucker
A 50-year-old male UK resident with a history of hypertension and hypercholesterolaemia presented to the emergency department with a 48-hour history of sudden onset bilateral thigh swelling and pain unrelieved by regular analgesia. 3 days prior to presentation, he performed a vigorous workout in the gym. His medications included ramipril 5 mg once daily and atorvastatin 20 mg at night time. He was a non-smoker and did not consume alcohol. He reported no known drug allergies. Physical examination confirmed bilateral swollen thighs, with no overlying skin changes, clinically suggestive of compartment syndrome...
March 16, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28301729/atorvastatin-can-ameliorate-left-atrial-stunning-induced-by-radiofrequency-ablation-for-atrial-fibrillation
#11
Ruiqin Xie, Yingtao Yang, Wei Cui, Hongning Yin, Hongmei Zheng, Jidong Zhang, Ling You
The objective of this study was to study the functional changes of left atrium after radiofrequency ablation treatment for atrial fibrillation and the therapeutic effect of Atorvastatin. 58 patients undergoing radiofrequency ablation for atrial fibrillation were randomly divided into non-Atorvastatin group and Atorvastatin group. Patients in Atorvastatin group were treated with Atorvastatin 20mg po per night in addition to the conventional treatment of atrial fibrillation; patients in non-Atorvastatin group received conventional treatment of atrial fibrillation only...
March 16, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28300827/simvastatin-and-atorvastatin-inhibit-dna-replication-licensing-factor-mcm7-and-effectively-suppress-rb-deficient-tumors-growth
#12
Juan Li, Jie Liu, Zheyong Liang, Fang He, Lu Yang, Pingping Li, Yina Jiang, Bo Wang, Can Zhou, Yaochun Wang, Yu Ren, Jin Yang, Jianmin Zhang, Zhijun Luo, Cyrus Vaziri, Peijun Liu
Loss or dysfunction of tumor suppressor retinoblastoma (RB) is a common feature in various tumors, and contributes to cancer cell stemness and drug resistance to cancer therapy. However, the strategy to suppress or eliminate Rb-deficient tumor cells remains unclear. In the present study, we accidentally found that reduction of DNA replication licensing factor MCM7 induced more apoptosis in RB-deficient tumor cells than in control tumor cells. Moreover, after a drug screening and further studies, we demonstrated that statin drug Simvastatin and Atorvastatin were able to inhibit MCM7 and RB expressions...
March 16, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28299634/prevalence-and-determinants-of-the-use-of-lipid-lowering-agents-in-a-population-of-older-hospitalized-patients-the-findings-from-the-reposi-registro-politerapie-societ%C3%A3-italiana-di-medicina-interna-study
#13
Marco Bertolotti, Carlotta Franchi, Marco B L Rocchi, Andrea Miceli, M Vittoria Libbra, Alessandro Nobili, Giulia Lancellotti, Lucia Carulli, Chiara Mussi
BACKGROUND: Older patients are prone to multimorbidity and polypharmacy, with an inherent risk of adverse events and drug interactions. To the best of our knowledge, available information on the appropriateness of lipid-lowering treatment is extremely limited. AIM: The aim of the present study was to quantify and characterize lipid-lowering drug use in a population of complex in-hospital older patients. METHODS: We analyzed data from 87 units of internal medicine or geriatric medicine in the REPOSI (Registro Politerapie della Società Italiana di Medicina Interna) study, with reference to the 2010 and 2012 patient cohorts...
April 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28296588/a-healthy-balance-of-plasma-cholesterol-by-a-novel-annurca-apple-based-nutraceutical-formulation-results-of-a-randomized-trial
#14
Gian Carlo Tenore, Domenico Caruso, Giuseppe Buonomo, Maria D'Avino, Pietro Campiglia, Luciana Marinelli, Ettore Novellino
Cardiovascular diseases are nowadays preferential targets of preventive medicine through a straightforward therapy on lipid profile. However, statins, the first-line lipid-lowering drug therapy, specifically act on low-density lipoprotein cholesterol (LDL-C), having a modest effect on plasma high-density lipoprotein cholesterol (HDL-C) concentrations. Today, a number of novel HDL-targeted therapies are emerging, along with unexpected side effects. Thus, novel and possibly safe substances, able to correct impaired lipid profile in humans, are still in great demand...
March 2017: Journal of Medicinal Food
https://www.readbyqxmd.com/read/28295458/improvement-in-erectile-function-in-a-rat-model-of-high-cholesterol-diet-induced-atherosclerosis-by-atorvastatin-in-a-manner-that-is-independent-of-its-lipid-lowering-property
#15
Z Zhang, L Tang, W Yu, Y Chen, Y-T Dai
The purpose of the present study is to explore the effects of a lipid-lowering drug atorvastatin, a three-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, in the treatment of erectile dysfunction (ED) in a rat model of atherosclerosis (AS) and the possible mechanisms underneath. A high-cholesterol diet was administrated to Sprague-Dawley rats in an attempt to induce an ASED model, which was later confirmed by abdominal aorta histopathology and erectile function evaluation. ASED rats were further assigned to non-treatment group, atorvastatin low-dose treatment group (5 mg kg(-1)  day(-1) ), high-dose group (10 mg kg(-1)  day(-1) ) and sildenafil (1...
March 10, 2017: Andrologia
https://www.readbyqxmd.com/read/28294872/-pleotropic-effects-of-atorvastatin-in-patients-with-chronic-ischemic-heart-disease
#16
V P Mikhin, Yu A Zhilyaeva, N I Gromnaky
Examined 52 patients with a diagnosis Ischemic heart disease: stable angina II-III FC CHF I-IIA stage, in combination with hypercholesterolemia aged 53-65 years (58,2+/-6,5), receiving together with traditional antianginal therapy generic atorvastatin Torvakard in the dose of 10 mg/day (20 people) with the level of total cholesterol from 5.0 to 6.50 mmol/l, patients with cholesterol levels from is 6.51 to 8.0 mmol/l was taking Torvakard 20 mg/day (32 person). As a result of 3 months therapy with low doses of Torvakarda decreased level of CRP, endothelin-1, IMT, improving the parameters of endothelium-dependent vasodilation, which shows the positive impact of the drug on morphological and functional parameters of the vascular wall...
May 2016: Kardiologiia
https://www.readbyqxmd.com/read/28285599/microbiome-and-metabolome-modifying-effects-of-several-cardiovascular-disease-interventions-in-apo-e-mice
#17
Paul M Ryan, Lis E E London, Trent C Bjorndahl, Rupasri Mandal, Kiera Murphy, Gerald F Fitzgerald, Fergus Shanahan, R Paul Ross, David S Wishart, Noel M Caplice, Catherine Stanton
BACKGROUND: There is strong evidence indicating that gut microbiota have the potential to modify, or be modified by the drugs and nutritional interventions that we rely upon. This study aims to characterize the compositional and functional effects of several nutritional, neutraceutical, and pharmaceutical cardiovascular disease interventions on the gut microbiome, through metagenomic and metabolomic approaches. Apolipoprotein-E-deficient mice were fed for 24 weeks either high-fat/cholesterol diet alone (control, HFC) or high-fat/cholesterol in conjunction with one of three dietary interventions, as follows: plant sterol ester (PSE), oat β-glucan (OBG) and bile salt hydrolase-active Lactobacillus reuteri APC 2587 (BSH), or the drug atorvastatin (STAT)...
March 13, 2017: Microbiome
https://www.readbyqxmd.com/read/28283885/anti-inflammatory-effects-of-atorvastatin-by-suppressing-traf3ip2-and-il-17ra-in-human-glioblastoma-spheroids-cultured-in-a-three-dimensional-model-possible-relevance-to-glioblastoma-treatment
#18
Neda Bayat, Somayeh Ebrahimi-Barough, Abbas Norouzi-Javidan, Hooshang Saberi, Mohammad Mehdi Mokhtari Ardakan, Arman Ai, Mostafa Soleimannejad, Jafar Ai
Glioblastoma multiform (GBM) is a primary malignant brain tumor with a few therapeutic targets available for it. The interaction between the immune system and glioma is an important factor that could lead to novel therapeutic approaches to fight glioma. In this study, we investigated in vitro anti-inflammatory and apoptotic activity of atorvastatin in different concentrations 1, 5, and 10 μM on glioma spheroid cells cultured in a three-dimensional model in fibrin gel that indicate the complex in vivo microenvironment better than a simple two-dimensional cell culture...
March 10, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28273631/protective-effects-of-n-acetylcystein-and-atorvastatin-against-renal-and-hepatic-injury-in-a-rat-model-of-intestinal-ischemia-reperfusion
#19
Dimitrios Alexandropoulos, Gerasimos V Bazigos, Ilias P Doulamis, Aspasia Tzani, Panagiotis Konstantopoulos, Nikolitsa Tragotsalou, Agathi Kondi-Pafiti, Thomas Kotsis, Nikolaos Arkadopoulos, Vasileios Smyrniotis, Despina N Perrea
AIM OF THE STUDY: We sought to examine whether the separate and combined effect of N-acetylcystein (NAC) and atorvastatin prevented hepatic and renal tissue injury induced by intestinal ischemia-reperfusion (I/R). MATERIAL AND METHODS: 40 male Wistar rats were allocated into 5 experimental groups; Control (n=8): sham, I/R (n=8): rats underwent occlusion of superior mesenteric artery for 45min, Atorvastatin (n=8): rats received 10mg/kg atorvastatin, NAC (n=8): rats received 160mg/kg NAC, NAC&Atorvastatin (n=8): rats received both aforementioned agents...
March 5, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28264197/simvastatin-and-atorvastatin-reduce-the-mechanical-properties-of-tendon-constructs-in-vitro-and-introduce-catabolic-changes-in-the-gene-expression-pattern
#20
Pernilla Eliasson, Rene B Svensson, Antonis Giannopoulos, Christian Eismark, Michael Kjær, Peter Schjerling, Katja M Heinemeier
Treatment with lipid-lowering drugs, statins, is common all over the world. Lately, the occurrence of spontaneous tendon ruptures or tendinosis have suggested a negative influence of statins upon tendon tissue. But how statins might influence tendons is not clear. In the present study, we investigated the effect of statin treatment on mechanical strength, cell proliferation, collagen content and gene expression pattern in a tendon-like tissue made from human tenocytes in vitro. Human tendon fibroblasts were grown in a 3D tissue culture model (tendon constructs), and treated with either simvastatin or atorvastatin, low or high dose, respectively, for up to seven days...
2017: PloS One
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