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Pitavastatin

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https://www.readbyqxmd.com/read/28089347/virtual-screening-and-experimental-validation-identify-novel-modulators-of-nuclear-receptor-rxr%C3%AE-from-drugbank-database
#1
Dan Xu, Lijun Cai, Shangjie Guo, Lei Xie, Meimei Yin, Ziwen Chen, Hu Zhou, Ying Su, Zhiping Zeng, Xiaokun Zhang
Retinoid X receptor alpha (RXRα), an important ligand-dependent transcription factor, plays a critical role in the development of various cancers and metabolic and neurodegenerative diseases. Therefore, RXRα represents one of the most important targets in modern drug discovery. In this study, Drugbank 2.0 with 1280 old drugs were virtually screened by Glide according to the crystal structure of ligand-binding domain (LBP) of RXRα. 15 compounds selected were tested for their binding and transcriptional activity toward RXRα by Biacore and reporter gene assay, respectively...
December 26, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28029012/efficacy-of-moderate-intensity-statins-in-the-treatment-of-dyslipidemia-in-korean-patients-with-type-2-diabetes-mellitus
#2
Sung Hye Kong, Bo Kyung Koo, Min Kyong Moon
BACKGROUND: There has been evidences of ethnic differences in the low density lipoprotein cholesterol (LDL-C) lowering effect of statin. We aimed to evaluate the efficacy of moderate-intensity statins in the treatment of dyslipidemia among Korean patients with type 2 diabetes mellitus (T2DM). METHODS: We analyzed a retrospective cohort that consisted of Korean patients with T2DM aged 40 to 75 years who had been prescribed any of the moderate-intensity statins (atorvastatin 10 or 20 mg, rosuvastatin 5 or 10 mg, pitavastatin 2 mg, or pravastatin 40 mg)...
December 16, 2016: Diabetes & Metabolism Journal
https://www.readbyqxmd.com/read/27997722/pitavastatin-suppresses-hyperglycemia-induced-podocyte-injury-via-bone-morphogenetic-protein-7-preservation
#3
Makoto Ohigashi, Miyuki Kobara, Tamotsu Takahashi, Hiroe Toba, Takehiko Wada, Tetsuo Nakata
BACKGROUND: Podocytes form the essential components of the glomerular filtration barrier and play a critical role in diabetic nephropathy. Recent evidence suggests that HMG-CoA reductase inhibitors (statins) exert renoprotective effects. We investigated whether pitavastatin directly suppresses hyperglycemia-induced podocyte injury using cultured podocytes and, if so, the mechanism of the beneficial effects. METHODS AND RESULTS: Cultured podocytes were exposed to media containing normal (NG; 5 mmol/L) or high (HG; 25 mmol/L) glucose for one week...
December 20, 2016: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/27943276/validation-of-a-microdose-probe-drug-cocktail-for-clinical-drug-interaction-assessments-for-drug-transporters-and-cyp3a
#4
T Prueksaritanont, D A Tatosian, X Chu, R Railkar, R Evers, C Chavez-Eng, R Lutz, W Zeng, J Yabut, G H Chan, X Cai, A H Latham, J Hehman, D Stypinski, J Brejda, C Zhou, B Thornton, K P Bateman, I Fraser, S A Stoch
A microdose cocktail containing midazolam, dabigatran etexilate, pitavastatin, rosuvastatin, and atorvastatin has been established to allow simultaneous assessment of a perpetrator impact on the most common drug metabolizing enzyme, cytochrome P450 (CYP)3A, and the major transporters organic anion-transporting polypeptides (OATP)1B, breast cancer resistance protein (BCRP), and MDR1 P-glycoprotein (P-gp). The clinical utility of these microdose cocktail probe substrates was qualified by conducting clinical drug interaction studies with three inhibitors with different in vitro inhibitory profiles (rifampin, itraconazole, and clarithromycin)...
December 10, 2016: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27899849/statin-therapy-review-of-safety-and-potential-side-effects
#5
REVIEW
Satish Ramkumar, Ajay Raghunath, Sudhakshini Raghunath
BACKGROUND: Hydroxymethyl glutaryl coenzyme A reductase inhibitors, commonly called statins, are some of the most commonly prescribed medications worldwide. Evidence suggests that statin therapy has significant mortality and morbidity benefit for both primary and secondary prevention from cardiovascular disease. Nonetheless, concern has been expressed regarding the adverse effects of long term statin use. The purpose of this article was to review the current medical literature regarding the safety of statins...
November 2016: Acta Cardiologica Sinica
https://www.readbyqxmd.com/read/27865182/early-initiation-of-eicosapentaenoic-acid-and-statin-treatment-is-associated-with-better-clinical-outcomes-than-statin-alone-in-patients-with-acute-coronary-syndromes-1-year-outcomes-of-a-randomized-controlled-study
#6
Kazumasa Nosaka, Toru Miyoshi, Mutsumi Iwamoto, Masahito Kajiya, Keisuke Okawa, Saori Tsukuda, Fumi Yokohama, Masahiro Sogo, Tomoyuki Nishibe, Naoaki Matsuo, Satoshi Hirohata, Hiroshi Ito, Masayuki Doi
BACKGROUND: Early initiation of EPA treatment in combination with a statin within 24h after percutaneous coronary intervention (PCI) in patients with acute myocardial infarction (MI) reduces inflammation and ventricular arrhythmia compared with statin monotherapy; however, the impact of early initiation of EPA treatment on cardiovascular events is unclear. We determined whether early eicosapentaenoic acid (EPA) treatment in patients with acute coronary syndrome (ACS) reduces adverse cardiovascular events...
February 1, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/27861386/statins-and-risk-for-new-onset-diabetes-mellitus-a-real-world-cohort-study-using-a-clinical-research-database
#7
Dukyong Yoon, Seung Soo Sheen, Sukhyang Lee, Yong Jun Choi, Rae Woong Park, Hong-Seok Lim
Although concern regarding the increased risk for new-onset diabetes mellitus (NODM) after statin treatment has been raised, there has been a lack of evidence in real-world clinical practice, particularly in East Asians. We investigated whether statin use is associated with risk for NODM in Koreans. We conducted a retrospective cohort study using the clinical research database from electronic health records. The study cohort consisted of 8265 statin-exposed and 33,060 matched nonexposed patients between January 1996 and August 2013...
November 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27858342/physiologically-based-pharmacokinetic-pbpk-modeling-of-pitavastatin-and-atorvastatin-to-predict-drug-drug-interactions-ddis
#8
Peng Duan, Ping Zhao, Lei Zhang
BACKGROUND: The disposition of statins varies and involves both metabolizing enzymes and transporters, making predictions of statin drug-drug interactions (DDIs) challenging. Physiologically based pharmacokinetic (PBPK) models have, however, demonstrated ability to predict complex DDIs. OBJECTIVE: In this study, PBPK models of two statins (pitavastatin and atorvastatin) were developed and applied to predict pitavastatin and atorvastatin associated DDIs. METHOD: Pitavastatin and atorvastatin PBPK models were developed using in vitro and human pharmacokinetic data in a population-based PBPK software (SimCYP(®)) by considering the contribution of both metabolizing enzymes and transporters to their overall pharmacokinetics...
November 17, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27837448/consensus-on-the-statin-of-choice-in-patients-with-impaired-glucose-metabolism-results-of-the-diana-study
#9
Jesús Millán Núñez-Cortés, Aleix Cases Amenós, Juan Francisco Ascaso Gimilio, Vivencio Barrios Alonso, Vicente Pascual Fuster, Juan Carles Pedro-Botet Montoya, Xavier Pintó Sala, Adalberto Serrano Cumplido
INTRODUCTION AND OBJECTIVES: Despite the recognized clinical benefit of statins on cardiovascular prevention, providing correct management of hypercholesterolaemia, possible adverse effects of their use cannot be disregarded. Previously published data shows that there is a risk of developing diabetes mellitus or experiencing changes in glucose metabolism in statin-treated patients. The possible determining factors are the drug characteristics (potency, dose), patient characteristics (kidney function, age, cardiovascular risk and polypharmacy because of multiple disorders) and the pre-diabetic state...
November 11, 2016: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/27764723/efficacy-and-safety-of-long-term-treatment-with-statins-for-coronary-heart-disease-a-bayesian-network-meta-analysis
#10
Yongbin Lu, Zhiyuan Cheng, Yaxue Zhao, Xiaoyu Chang, Cynthia Chan, Yana Bai, Ning Cheng
BACKGROUND AND AIMS: Our study aims to evaluate the efficacy and safety of long-term treatment of statins for coronary heart disease (CHD). METHODS: Efficacy outcomes included changes in blood lipids, risk of CHD mortality and all-cause mortality. Safety outcomes were evaluated by the risk of adverse events (AE). Bayesian network meta-analysis was used to compare the direct and indirect effects between different statins. RESULTS: The systematic review showed that levels of blood lipids decreased during statin treatment...
November 2016: Atherosclerosis
https://www.readbyqxmd.com/read/27756037/effect-of-statins-on-atherogenic-serum-amyloid-a-and-%C3%AE-1-antitrypsin-low-density-lipoprotein-complexes
#11
Yusuke Miyazaki, Yasufumi Katanasaka, Yoichi Sunagawa, Sae Hirano-Sunagawa, Masafumi Funamoto, Eriko Morimoto, Maki Komiyama, Akira Shimatsu, Noriko Satoh-Asahara, Hajime Yamakage, Hiromichi Wada, Koji Hasegawa, Tatsuya Morimoto
PURPOSE: HMG-CoA reductase inhibitors, also termed statins, are used to reduce the risk of coronary artery disease. Two oxidatively modified low-density lipoprotein (LDL) complexes, serum amyloid A-LDL (SAA-LDL) and α1-antitrypsin-LDL (AT-LDL), serve as atherosclerotic, inflammatory, and cardiovascular risk markers. In this study, we examined the effects of hydrophilic rosuvastatin (RSV) and lipophilic pitavastatin (PTV) on these markers in patients with hypercholesterolemia. METHODS: The present study was a sub-analysis of our previous STAT-LVDF study...
October 3, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/27696476/radiosynthesis-of-novel-pitavastatin-derivative-18-f-ptv-f1-as-a-tracer-for-hepatic-oatp-using-a-one-pot-synthetic-procedure
#12
Hiroyuki Kimura, Yusuke Yagi, Kenji Arimitsu, Kazuya Maeda, Kazuaki Ikejiri, Jun-Ichi Takano, Hiroyuki Kusuhara, Shinya Kagawa, Masahiro Ono, Yuichi Sugiyama, Hideo Saji
Pitavastatin is an antihyperlipidemic agent, a potent inhibitor of 3-hydroxymethyl-glutaryl-CoA reductase, which is selectively taken up into the liver mainly via hepatic organic anion transporting polypeptide 1B1 (OATP1B1). OATP1B1 can accept a variety of organic anions, and previous reports indicated that it is responsible for the hepatic clearance of several clinically used anionic drugs. Therefore, the pharmacokinetics and the hepatic distribution of pitavastatin provide an insight into the function of OATP1B1 in humans...
November 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27643859/simultaneous-determination-of-telmisartan-and-pitavastatin-in-rat-plasma-by-uplc-ms-ms-application-to-pharmacokinetic-interaction-study
#13
Xi Chen, Bei Xu, Jian Yang, Juan Liu, Dailong Fang, Yongjun Gu, Zhifei Jian, Minghai Tang, Chunmei Fu, Zhi Zhang, Chunling Jiang, Xiangrong Song
To investigate the pharmacokinetic (PK) interaction between telmisartan (Tel) and pitavastatin (Pit), a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometric assay method had been successfully established and fully validated for the simultaneous quantification of Tel and Pit in rat plasma. A simple protein precipitation procedure was adopted for the sample preparation with satisfactory extraction recovery for both analytes and the internal standard. The samples were chromatographed on an Inertsil ODS-3 C18 column (100mm×2...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27621652/pitavastatin-suppressed-liver-cancer-cells-in-vitro-and-in-vivo
#14
He-Yi You, Wei-Jian Zhang, Xue-Meng Xie, Zhi-Hai Zheng, Heng-Liang Zhu, Fei-Zhao Jiang
Pitavastatin classically functions as a blood cholesterol-lowering drug. Previously, it was discovered with antiglioma stem cell properties through drug screening. However, whether it can be used for liver cancer cell therapy has never been reported. In this study, the cell viability and colony formation assay were utilized to analyze the cytotoxicity of pitavastatin on liver cancer cells. The cell cycle alteration was checked after pitavastatin treatment. Apoptosis-related protein expression and the effect of caspase inhibitor were also checked...
2016: OncoTargets and Therapy
https://www.readbyqxmd.com/read/27603665/a-translational-study-of-a-new-therapeutic-approach-for-acute-myocardial-infarction-nanoparticle-mediated-delivery-of-pitavastatin-into-reperfused-myocardium-reduces-ischemia-reperfusion-injury-in-a-preclinical-porcine-model
#15
Kenzo Ichimura, Tetsuya Matoba, Kaku Nakano, Masaki Tokutome, Katsuya Honda, Jun-Ichiro Koga, Kensuke Egashira
BACKGROUND: There is an unmet need to develop an innovative cardioprotective modality for acute myocardial infarction, for which interventional reperfusion therapy is hampered by ischemia-reperfusion (IR) injury. We recently reported that bioabsorbable poly(lactic acid/glycolic acid) (PLGA) nanoparticle-mediated treatment with pitavastatin (pitavastatin-NP) exerts a cardioprotective effect in a rat IR injury model by activating the PI3K-Akt pathway and inhibiting inflammation. To obtain preclinical proof-of-concept evidence, in this study, we examined the effect of pitavastatin-NP on myocardial IR injury in conscious and anesthetized pig models...
2016: PloS One
https://www.readbyqxmd.com/read/27603548/pre-incubation-with-cyclosporine-a-potentiates-its-inhibitory-effects-on-pitavastatin-uptake-mediated-by-recombinantly-expressed-cynomolgus-monkey-hepatic-organic-anion-transporting-polypeptide
#16
Tsuyoshi Takahashi, Tatsuyuki Ohtsuka, Yasuhiro Uno, Masahiro Utoh, Hiroshi Yamazaki, Toshiyuki Kume
Cyclosporine A, an inhibitor of hepatic organic anion transporting polypeptides (OATPs), reportedly increased plasma concentrations of probe substrates, although its maximum unbound blood concentrations were lower than the experimental half-maximal inhibitory (IC50 ) concentrations. Pre-incubation with cyclosporine A in vitro before simultaneous incubation with probes has been reported to potentiate its inhibitory effects on recombinant human OATP-mediated probe uptake. In the present study, the effects of cyclosporine A and rifampicin on recombinant cynomolgus monkey OATP-mediated pitavastatin uptake were investigated in pre- and simultaneous incubation systems...
November 2016: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/27583130/statin-3-hydroxy-3-methylglutaryl-coenzyme-a-reductase-inhibitor-based-therapy-for-hepatitis-c-virus-hcv-infection-related-diseases-in-the-era-of-direct-acting-antiviral-agents
#17
Sara Kishta, Reem Ei-Shenawy, Sobhy Kishta
Recent improvements have been made in the treatment of hepatitis C virus (HCV) infection with the introduction of direct-acting antiviral agents (DAAs). However, despite successful viral clearance, many patients continue to have HCV-related disease progression. Therefore, new treatments must be developed to achieve viral clearance and prevent the risk of HCV-related diseases. In particular, the use of pitavastatin together with DAAs may improve the antiviral efficacy as well as decrease the progression of liver fibrosis and the incidence of HCV-related hepatocellular carcinoma...
2016: F1000Research
https://www.readbyqxmd.com/read/27581680/statin-action-enriches-hdl3-in-polyunsaturated-phospholipids-and-plasmalogens-and-reduces-ldl-derived-phospholipid-hydroperoxides-in-atherogenic-mixed-dyslipidemia
#18
Alexina Orsoni, Patrice Thérond, Ricardo Tan, Philippe Giral, Paul Robillard, Anatol Kontush, Peter J Meikle, M John Chapman
Atherogenic mixed dyslipidemia associates with oxidative stress and defective HDL antioxidative function in metabolic syndrome (MetS). The impact of statin treatment on the capacity of HDL to inactivate LDL-derived, redox-active phospholipid hydroperoxides (PCOOHs) in MetS is indeterminate. Insulin-resistant, hypertriglyceridemic, hypertensive, obese males were treated with pitavastatin (4 mg/day) for 180 days, resulting in marked reduction in plasma TGs (-41%) and LDL-cholesterol (-38%), with minor effects on HDL-cholesterol and apoAI...
November 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27534254/-japan-acs-japan-assessment-of-pitavastatin-and-atorvastatin-in-acute-coronary-syndrome
#19
COMPARATIVE STUDY
Tomotaka Dohi, Hiroyuki Daida
No abstract text is available yet for this article.
June 20, 2016: Nihon Rinsho. Japanese Journal of Clinical Medicine
https://www.readbyqxmd.com/read/27498397/impact-of-statin-therapy-on-plasma-adiponectin-concentrations-a-systematic-review-and-meta-analysis-of-43-randomized-controlled-trial-arms
#20
Piotr Chruściel, Amirhossein Sahebkar, Magdalena Rembek-Wieliczko, Maria-Corina Serban, Sorin Ursoniu, Dimitri P Mikhailidis, Steven R Jones, Svetlana Mosteoru, Michael J Blaha, Seth S Martin, Jacek Rysz, Peter P Toth, Gregory Y H Lip, Michael J Pencina, Kausik K Ray, Maciej Banach
BACKGROUND AND AIMS: The effect of statin therapy on plasma adiponectin levels has not been conclusively studied. Therefore, we aimed to evaluate this effect through a systematic review and meta-analysis of available randomized controlled trials (RCTs). METHODS: Quantitative data synthesis was performed using a random-effects model with weighted mean difference (WMD) and 95% confidence interval (CI) as summary statistics. RESULTS: In 30 studies (43 study arms) with 2953 participants, a significant increase in plasma adiponectin levels was observed after statin therapy (WMD: 0...
October 2016: Atherosclerosis
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