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Pitavastatine

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https://www.readbyqxmd.com/read/29782986/antiglycation-study-of-hmg-r-inhibitors-and-tocotrienol-against-glycated-bsa-and-ldl-a-comparative-study
#1
Rabia Nabi, Sahir Sultan Alvi, Rizwan Khan, Shafeeque Ahmad, Saheem Ahmad, M Salman Khan
Non-enzymatic glycation mediated advanced glycation end products (AGEs) generation results in the pathogenesis of diabetic complications and atherosclerotic cardiovascular disease (ASCVD) which is greatly influenced by 3-hydroxy-3-methyl-glutaryl Co-A reductase (HMG-R) activity. HMG-R inhibitors, statins, are well known for reducing mortality and morbidity of ASCVD in patients with diabetes due to their pleiotropic effects independent of cholesterol lowering. Due to distinct chemical structures, various statins may play important role in the inhibition of AGEs mediated pathologies...
May 18, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29772482/baseline-serum-sitosterol-level-as-predictor-of-adverse-clinical-events-in-acute-coronary-syndrome-patients-with-dyslipidaemia-a-sub-analysis-of-hij-proper
#2
Junichi Yamaguchi, Erisa Kawada-Watanabe, Ryo Koyanagi, Hiroyuki Arashi, Haruki Sekiguchi, Koichi Nakao, Tetsuya Tobaru, Hiroyuki Tanaka, Toshiaki Oka, Yasuhiro Endo, Katsumi Saito, Tatsuro Uchida, Kunihiko Matsui, Hiroshi Ogawa, Nobuhisa Hagiwara
BACKGROUND AND AIMS: We aimed to examine the effect of serum sitosterol, a cholesterol absorption marker, on clinical outcomes in acute coronary syndrome patients with dyslipidaemia. METHODS: This is a sub-analysis of the HIJ-PROPER trial that assesses the effect of aggressive low-density lipoprotein cholesterol (LDL-C) lowering treatment with pitavastatin + ezetimibe in 1734 acute coronary syndrome (ACS) patients with dyslipidaemia. Patients were divided into two groups based on sitosterol level at enrolment (cut-off value was 2...
May 5, 2018: Atherosclerosis
https://www.readbyqxmd.com/read/29771125/palladium-catalyzed-stereoselective-cyclization-of-in-situ-formed-allenyl-hemiacetals-synthesis-of-rosuvastatin-and-pitavastatin
#3
Pierre A Spreider, Bernhard Breit
A diastereoselective palladium-catalyzed cyclization of allenyl hemiacetals is described. It permits the selective synthesis of 1,3-dioxane derivatives, precursors for syn-configured 1,3-diols which make an appearance in all of the statin representatives. The reaction allows the total synthesis of Rosuvastatin and Pitavastatin in a straightforward fashion.
May 17, 2018: Organic Letters
https://www.readbyqxmd.com/read/29768081/unremarkable-impact-of-oatp-inhibition-on-the-liver-concentration-of-fluvastatin-lovastatin-and-pitavastatin-in-wild-type-and-oatp1a-1b-knockout-mouse
#4
Jae H Chang, Xiaolin Zhang, Kirsten Messick, Yi-Chen Chen, Eugene Chen, Jonathan Cheong, Justin Ly
1. OATP inhibitors have been shown to significantly increase the plasma exposure of statins. However, understanding alterations of liver concentration is also important. While modeling has simulated liver concentration changes, availability of experimental data is limited, especially when concerning drug-drug interactions (DDI). The objective of this work was to determine blood and liver concentrations of fluvastatin, lovastatin and pitavastatin, when blocking uptake transporters. 2. In wild-type mouse, rifampin pre-treatment decreased the unbound liver-to-plasma ratio (Kp,uu ) of fluvastatin by 4...
May 16, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29748935/comparative-study-of-the-dose-dependence-of-oatp1b-inhibition-by-rifampicin-using-probe-drugs-and-endogenous-substrates-in-healthy-volunteers
#5
Issey Takehara, Takashi Yoshikado, Keiko Ishigame, Daiki Mori, Ken-Ichi Furihata, Nobuaki Watanabe, Osamu Ando, Kazuya Maeda, Yuichi Sugiyama, Hiroyuki Kusuhara
PURPOSE: To evaluate association of the dose-dependent effect of rifampicin, an OATP1B inhibitor, on the plasma concentration-time profiles among OATP1B substrates drugs and endogenous substrates. METHODS: Eight healthy volunteers received atorvastatin (1 mg), pitavastatin (0.2 mg), rosuvastatin (0.5 mg), and fluvastatin (2 mg) alone or with rifampicin (300 or 600 mg) in a crossover fashion. The plasma concentrations of these OATP1B probe drugs, total and direct bilirubin, glycochenodeoxycholate-3-sulfate (GCDCA-S), and coproporphyrin I, were determined...
May 10, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29747299/-the-clinical-application-of-pitavastatin-evidence-of-efficacy-and-safety-in-east-asian-population
#6
S P Zhao
No abstract text is available yet for this article.
May 1, 2018: Zhonghua Nei Ke za Zhi [Chinese Journal of Internal Medicine]
https://www.readbyqxmd.com/read/29746136/relative-activity-factor-raf-based-scaling-of-uptake-clearance-mediated-by-organic-anion-transporting-polypeptide-oatp-1b1-and-oatp1b3-in-human-hepatocytes
#7
Saki Izumi, Yoshitane Nozaki, Hiroyuki Kusuhara, Koichiro Hotta, Toshiki Mochizuki, Takafumi Komori, Kazuya Maeda, Yuichi Sugiyama
In vitro-in vivo extrapolation based on uptake clearance determined in human hepatocytes has been used to predict in vivo hepatic clearance of organic anion transporting polypeptide (OATP) substrates. This study evaluated the relative activity factor (RAF) approach to extrapolate active uptake clearance in transporter-transfected cell systems (CLuptake ) to that in human hepatocyte suspensions (PSinf,act ). RAF values for OATP1B1 and OATP1B3 were determined in two batches of cryopreserved human hepatocytes using estrone-3-sulfate and cholecystokinin octapeptide as reference substrates, respectively...
May 10, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29738341/effect-of-pitavastatin-and-atorvastatin-on-regression-of-atherosclerosis-assessed-using-intravascular-ultrasound-a-meta-analysis
#8
Hui Liu, Mingjun Zhang, Delong Li, Jingjing Tian, Xuyang Wang, Jinyu Pan, Dian Liu, Xiaowei Li, Fengshuang An
BACKGROUND: The aim of this study is to compare the efficacy and safety of pitavastatin and atorvastatin using data from randomized-controlled trial pooled together by means of a meta-analysis and decide which is better. METHODS: PubMed, CENTRAL, Web of Knowledge, and ClinicalTrials.gov website were searched for randomized-controlled trials published until October 2016. Eligible studies comparing pitavastatin with atorvastatin head to head and reporting the outcome of low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), glycated hemoglobin, and intravascular ultrasound evaluation were enrolled...
May 5, 2018: Coronary Artery Disease
https://www.readbyqxmd.com/read/29735587/high-dose-versus-low-dose-pitavastatin-in-japanese-patients-with-stable-coronary-artery-disease-real-cad-a-randomized-superiority-trial
#9
Isao Taguchi, Satoshi Iimuro, Hiroshi Iwata, Hiroaki Takashima, Mitsuru Abe, Eisuke Amiya, Takanori Ogawa, Yukio Ozaki, Ichiro Sakuma, Yoshihisa Nakagawa, Kiyoshi Hibi, Takafumi Hiro, Yoshihiro Fukumoto, Seiji Hokimoto, Katsumi Miyauchi, Tsutomu Yamazaki, Hiroshi Ito, Yutaka Otsuji, Kazuo Kimura, Jun Takahashi, Atsushi Hirayama, Hiroyoshi Yokoi, Kazuo Kitagawa, Takao Urabe, Yasushi Okada, Yasuo Terayama, Kazunori Toyoda, Takehiko Nagao, Masayasu Matsumoto, Yasuo Ohashi, Tetsuji Kaneko, Retsu Fujita, Hiroshi Ohtsu, Hisao Ogawa, Hiroyuki Daida, Hiroaki Shimokawa, Yasushi Saito, Takeshi Kimura, Teruo Inoue, Masunori Matsuzaki, Ryozo Nagai
BACKGROUND: Current guidelines call for high-intensity statin therapy in patients with cardiovascular disease on the basis of several previous "more versus less statins" trials. However, no clear evidence for more versus less statins has been established in an Asian population. METHODS: In this prospective, multicenter, randomized, open-label, blinded end point study, 13 054 Japanese patients with stable coronary artery disease who achieved low-density lipoprotein cholesterol (LDL-C) <120 mg/dL during a run-in period (pitavastatin 1 mg/d) were randomized in a 1-to-1 fashion to high-dose (pitavastatin 4 mg/d; n=6526) or low-dose (pitavastatin 1 mg/d; n=6528) statin therapy...
May 8, 2018: Circulation
https://www.readbyqxmd.com/read/29733433/statin-therapy-on-glycemic-control-in-type-2-diabetic-patients-a-network-meta-analysis
#10
J Y Cui, R R Zhou, S Han, T S Wang, L Q Wang, X H Xie
WHAT IS KNOWN AND OBJECTIVE: Statins are the cornerstone of primary and secondary prevention of cardiovascular diseases (CVDs) and are effective for the prevention of vascular events in diabetic patients. Diabetes mellitus is an important risk factor for CVDs .The majority of patients with diabetes mellitus benefits from statin therapy. According to the recent clinical guidelines of the American College of Cardiology and the American Heart Association, moderate-intensity or high-intensity statin therapy should be used as the primary prevention for individuals with diabetes mellitus, aged between 40 and 75 years and with low-density lipoprotein cholesterol (LDL-C) from 70 to 189 mg/dL...
May 7, 2018: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/29724614/total-hepatocellular-disposition-profiling-of-rosuvastatin-and-pitavastatin-in-sandwich-cultured-human-hepatocytes
#11
Katsuhiro Kanda, Ryosuke Takahashi, Takashi Yoshikado, Yuichi Sugiyama
This study describes the total disposition profiling of rosuvastatin (RSV) and pitavastatin (PTV) using a single systematic procedure called D-PREX (Disposition Profile Exploration) in sandwich-cultured human hepatocytes (SCHH). The biliary excretion fractions of both statins were clearly observed, which were significantly decreased dependent on the concentration of Ko143, an inhibitor for breast cancer resistance protein (BCRP). Ko143 also decreased the basolateral efflux fraction of RSV, whereas that of PTV was not significantly affected...
April 9, 2018: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29723430/relationships-of-changes-in-pharmacokinetic-parameters-of-substrate-drugs-in-drug-drug-interactions-on-metabolizing-enzymes-and-transporters
#12
Shinji Yamazaki
A general objective of drug-drug interaction (DDI) studies is to determine whether potential interactions of new molecular entities with concomitantly administered other drugs exist and, if DDIs occur, whether dosage adjustments are required. A typical end point for DDI evaluations is the ratio of area under the plasma concentration-time curve (AUC) of substrate drugs (AUCR), whereas the ratios of maximal plasma concentration (Cmax ) and terminal half-life (t1/2 ) are also important to understand DDI mechanisms (Cmax R and t1/2 R, respectively)...
May 3, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29720472/predicting-human-clearance-of-oatp-substrates-using-cynomolgus-monkey-in-vitro-in-vivo-scaling-of-hepatic-uptake-clearance
#13
Tom de Bruyn, Ayse Ufuk, Carina Cantrill, Rachel E Kosa, Yi-An Bi, Mark Niosi, Sweta Modi, A David Rodrigues, Larry M Tremaine, Manthena Vs Varma, Aleksandra Galetin, J Brian Houston
This work explores the utility of the cynomolgus monkey as a preclinical model to predict hepatic uptake clearance mediated by organic anion transporting polypeptide (OATP) transporters. Nine OATP substrates (rosuvastatin, pravastatin, repaglinide, fexofenadine, cerivastatin, telmisartan, pitavastatin, bosentan and valsartan) were investigated in plated cynomolgus monkey and human hepatocytes. Total uptake clearance and passive diffusion were measured in vitro from initial rates in the absence and presence of the OATP inhibitor rifamycin SV, respectively...
May 2, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29666154/prediction-and-quantification-of-hepatic-transporter-mediated-uptake-of-pitavastatin-utilizing-a-combination-of-the-relative-activity-factor-approach-and-mechanistic-modeling
#14
Pallabi Mitra, Samantha Weinheimer, Meeghan Michalewicz, Mitchell E Taub
Quantification of the fraction transported (ft) by a particular transporter will facilitate more robust estimations of transporter interactions. Using pitavastatin as a model uptake transporter substrate, we investigated the utility of the relative activity factor (RAF) approach and mechanistic modeling, to estimate ft in hepatocytes. Transporters evaluated were OATP1B1, OATP1B3, and NTCP. Transporter expressing HEK293 cells and human hepatocytes were used for determining RAF values, which were then incorporated into the mechanistic model to simulate hepatocyte uptake of pitavastatin over time...
April 17, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29663259/clinical-investigation-of-coproporphyrins-as-sensitive-biomarkers-to-predict-mild-to-strong-oatp1b-mediated-drug-drug-interactions
#15
Annett Kunze, Emmanuel Njumbe Ediage, Lieve Dillen, Mario Monshouwer, Jan Snoeys
INTRODUCTION: Coproporphyrin (CP) I and III have recently been proposed as endogenous clinical biomarkers to predict organic anion-transporting polypeptide 1B (OATP1B)-mediated drug-drug interactions (DDIs). In the present study, we first investigated the in vitro selectivity of CPI and CPIII towards drug uptake and efflux transporters. We then assessed the in vivo biomarker sensitivity towards OATP1B inhibition. METHODS: To assess transporter selectivity, incubations with CPI and CPIII were performed in vitro, using single transporter-expressing and control systems...
April 16, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29643253/in-vitro-in-vivo-extrapolation-of-oatp1b-mediated-drug-drug-interactions-in-cynomolgus-monkey
#16
Ayse Ufuk, Rachel E Kosa, Hongying Gao, Yi-An Bi, Sweta Modi, Dana Gates, A David Rodrigues, Larry M Tremaine, Manthena V S Varma, J Brian Houston, Aleksandra Galetin
Hepatic organic anion transporting polypeptides (OATP) 1B1 and 1B3 are clinically relevant transporters associated with significant drug-drug interactions (DDIs) and safety concerns. Given that OATP1Bs in cynomolgus monkey share >90% degree of gene and amino acid sequence identity with human orthologs, we evaluated the in vitro-in vivo translation of OATP1B-mediated DDI risk using this preclinical model. In vitro studies using cynomolgus monkey hepatocytes showed active uptake Km values of 2.0 and 3.9 µM for OATP1B probe substrates, pitavastatin and rosuvastatin, respectively...
April 11, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29626287/suppressive-effect-of-pitavastatin-on-aortic-arch-dilatation-in-acute-stanford-type-b-aortic-dissection-analysis-of-stanp-trial
#17
Naoki Masaki, Kiichiro Kumagai, Konosuke Sasaki, Satoshi Matsuo, Naotaka Motoyoshi, Osamu Adachi, Masatoshi Akiyama, Shunsuke Kawamoto, Koichi Tabayashi, Yoshikatsu Saiki
OBJECTIVES: Medical therapy for patients with uncomplicated acute type B aortic dissection (ABAD) is essentially accepted for its excellent early outcome; however, long-term outcomes have not been satisfactory due to aorta-related complications. This trial was performed to investigate the efficacy of a statin as an additive that may enhance the effectiveness of conventional medical treatment in patients with ABAD. METHODS: This was a multi-center, prospective, and randomized comparative investigation of patients with uncomplicated ABAD...
April 6, 2018: General Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/29574070/duality-of-statin-action-on-lipoprotein-subpopulations-in-the-mixed-dyslipidemia-of-metabolic-syndrome-quantity-vs-quality-over-time-and-implication-of-cetp
#18
M John Chapman, Alexina Orsoni, Paul Robillard, Patrice Therond, Philippe Giral
BACKGROUND: Statins impact the metabolism, concentrations, composition, and function of circulating lipoproteins. OBJECTIVE: We evaluated time course relationships between statin-mediated reduction in atherogenic apolipoprotein B (ApoB)-containing particles and dynamic intravascular remodeling of ApoAI-containing lipoprotein subpopulations in the mixed dyslipidemia of metabolic syndrome. METHODS: Insulin-resistant, hypertriglyceridemic, hypercholesterolemic, obese males (n = 12) were treated with pitavastatin (4 mg/d) and response evaluated at 6, 42, and 180 days...
February 9, 2018: Journal of Clinical Lipidology
https://www.readbyqxmd.com/read/29569046/in-vitro-antibacterial-effects-of-statins-against-bacterial-pathogens-causing-skin-infections
#19
Humphrey H T Ko, Ricky R Lareu, Brett R Dix, Jeffery D Hughes
With financial considerations impeding research and development of new antibiotics, drug repurposing (finding new indications for old drugs) emerges as a feasible alternative. Statins are extensively prescribed around the world to lower cholesterol, but they also possess inherent antimicrobial properties. This study identifies statins with the greatest potential to be repurposed as topical antibiotics and postulates a mechanism of action for statins' antibacterial activity. Using broth microdilution, the direct antibacterial effects of all seven parent statins currently registered for human use and three selected statin metabolites were tested against bacterial skin pathogens Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Serratia marcescens...
March 22, 2018: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/29567347/extrapolation-of-the-hepatic-clearance-of-drugs-in-the-absence-of-albumin-in-vitro-to-that-in-the-presence-of-albumin-in-vivo-comparative-assessement-of-two-extrapolation-models-based-on-the-albumin-mediated-hepatic-uptake-theory-and-limitations-and-mechanistic
#20
Patrick Poulin, Sami Haddad
The extrapolation of hepatic clearance (CL) from data determined in an in vitro assay in the absence of albumin (ALB) to that in the presence of ALB in liver in vivo were often inaccurate using traditional in vitro-to-in vivo extrapolation (IVIVE) methods for drugs binding to the ALB. It is recognized that considering an ALB-facilitated hepatic uptake phenomenon in the IVIVE can improve the extrapolation. Therefore, the present study provides a comparison of two existing models that account for the ALB-facilitated hepatic uptake phenomenon in the IVIVE of CL...
March 19, 2018: Journal of Pharmaceutical Sciences
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