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Pitavastatin

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https://www.readbyqxmd.com/read/29439129/simultaneous-assessment-in-vitro-of-transporter-and-metabolic-processes-in-hepatic-drug-clearance-use-of-a-media-loss-approach
#1
James Harrison, Tom De Bruyn, Adam S Darwich, J Brian Houston
Hepatocyte drug depletion-time assays are well established for the determination of metabolic clearance in vitro. The present study focuses on the refinement and evaluation of a "media loss" assay, an adaptation of the conventional depletion assay involving centrifugation of hepatocytes prior to sampling, allowing estimation of uptake in addition to metabolism. Using experimental procedures consistent with a high throughput, a selection of 12 compounds with a range of uptake and metabolism characteristics (atorvastatin, cerivastatin, clarithromycin, erythromycin, indinavir, pitavastatin, repaglinide, rosuvastatin, saquinavir and valsartan, together with two control compounds - midazolam and tolbutamide) were investigated in the presence and absence of the cytochrome P450 inhibitor 1-aminobenzotriazole and organic anion transporter protein inhibitor rifamycin SV...
February 8, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29434898/abt-737-and-pictilisib-synergistically-enhance-pitavastatin-induced-apoptosis-in-ovarian-cancer-cells
#2
Elizabeth De Wolf, Christopher De Wolf, Alan Richardson
There is considerable interest in redeploying drugs for use in combination with other oncology therapeutics. The single-agent activity of statins in ovarian cancer has been widely reported, however the drug concentration required to cause cell death is considerably higher than that achieved in patients receiving statin treatment for hypercholesterolemia. Unfortunately, statins can cause myopathy when administered in high doses. One solution to this is to identify drugs that could be used in combination with statins to reduce the dose required and those that may potentially reduce the incidence of adverse side effects...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29427912/adjunctive-therapy-with-statins-in-schizophrenia-patients-a-meta-analysis-and-implications
#3
Hong Shen, Rui Li, Rong Yan, Xia Zhou, Xia Feng, Mengjie Zhao, Hong Xiao
There are some conflicting results regarding the benefit of adjunctive therapy with statins for severity of negative symptoms in schizophrenia. This study aimed to verify whether statins use for adjunctive therapy was indeed beneficial to improve psychiatric symptoms in schizophrenia. The data were from CENTRAL, PubMed, Embase and MEDLINE. The Boolean search term used for the electronic database search was (statin OR simvastatin OR atorvastatin OR fluvastatin OR lovastatin OR mevastatin OR pitavastatin OR pravastatin OR rosuvastatin OR cerivastatin) and (schizophrenia OR schizoaffective disorder OR psychosis)...
February 5, 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29425980/dose-dependent-effects-of-statins-for-patients-with-aneurysmal-subarachnoid-hemorrhage-meta-regression-analysis
#4
REVIEW
Minh-Son To, Shivesh Prakash, Santosh I Poonnoose, Shailesh Bihari
OBJECTIVE: The study utilizes meta-regression analysis to quantify the dose-dependent effects of statin pharmacotherapy on vasospasm, delayed ischemic neurologic deficits (DINDs) and mortality in aneurysmal subarachnoid hemorrhage (aSAH). METHODS: Prospective, retrospective observational studies and randomized controlled trials (RCTs) were retrieved by a systematic database search. Summary estimates were expressed as absolute risk (AR) for a given statin dose or control (placebo)...
February 6, 2018: World Neurosurgery
https://www.readbyqxmd.com/read/29404047/electrochemical-determination-of-an-anti-hyperlipidimic-drug-pitavastatin-at-electrochemical-sensor-based-on-electrochemically-pre-treated-polymer-film-modified-gce
#5
Umar J Pandit, Gowhar A Naikoo, Mehraj Ud Din Sheikh, Gulzar A Khan, K K Raj, S N Limaye
An electrochemically pretreated silver macroporous (Ag MP) multiwalled carbon nanotube modified glassy carbon electrode (PAN-Ag MP-MWCNT-GCE) was fabricated for the selective determination of an anti-hyperlipidimic drug, pitavastatin (PST). The fabricated electrochemical sensor was characterized by cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS). The fabricated electrode was employed in quantifying and determining PST through differential pulse adsorptive stripping voltammetry (DPAdSV) and CV...
August 2017: Journal of Pharmaceutical Analysis
https://www.readbyqxmd.com/read/29403315/high-potency-statins-but-not-all-statins-decrease-the-risk-of-new-onset-osteoporotic-fractures-a-nationwide-population-based-longitudinal-cohort-study
#6
Tsung-Kun Lin, Yi-Sheng Liou, Ching-Heng Lin, Pesus Chou, Gwo-Ping Jong
Background: Statins have been linked to new-onset osteoporotic fractures (NOFs), and different statins may alter the risk for the development of NOFs. Aim: In this study, we investigated the association between different statins and the development of NOFs. Patients and methods: This was a longitudinal cohort study performed using data from claim forms submitted to the Taiwan Bureau of National Health Insurance, including case patients with NOFs from January 2004 to December 2013 and non-NOF subjects...
2018: Clinical Epidemiology
https://www.readbyqxmd.com/read/29361282/a-rapid-quantitative-assay-for-juvenile-hormones-and-intermediates-in-the-biosynthetic-pathway-using-gas-chromatography-tandem-mass-spectrometry
#7
Zhen-Peng Kai, Yue Yin, Zhi-Ruo Zhang, Juan Huang, Stephen S Tobe, Shan-Shan Chen
A method for rapid quantitation of insect juvenile hormones (JH) and intermediates in the biosynthetic pathway, both in vitro and in vivo (hemolymph and whole body), has been developed using GC-MS/MS. This method is as simple as the radiochemical assay (RCA), the most commonly used method for measurement of JH biosynthesis in vitro, without need for further purification and derivatization, or radioactive precursors or ligands. It shows high sensitivity, accuracy and reproducibility. Linear responses were obtained the range of 1-800 ng/mL (approximately 4-3000 nM)...
January 17, 2018: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29344241/combined-pitavastatin-and-dacarbazine-treatment-activates-apoptosis-and-autophagy-resulting-in-synergistic-cytotoxicity-in-melanoma-cells
#8
Abeer Al-Qatati, Saeb Aliwaini
Melanoma is an aggressive skin cancer and its incidence is increasing faster than any other type of cancer. Whilst dacarbazine (DTIC) is the standard chemotherapy for metastatic melanoma, it has limited success. Statins, including pitavastatin, have been demonstrated to have a range of anti-cancer effects in a number of human cancer cell lines. The present study therefore explored the anti-cancer activity of combined DTIC and pitavastatin in A375 and WM115 human melanoma cells. Cell survival assays demonstrated that combined DTIC and pitavastatin treatment resulted in synergistic cell death...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29334477/improvement-of-endothelial-function-by-pitavastatin-a-meta-analysis
#9
Niki Katsiki, Željko Reiner, Eugenia Tedeschi Reiner, Khalid Al-Rasadi, Matteo Pirro, Dimitri P Mikhailidis, Amirhossein Sahebkar
OBJECTIVE: Dyslipidemia is commonly associated with endothelial dysfunction and increased cardiovascular risk. Pitavastatin has been shown to reduce total and low-density lipoprotein cholesterol, to increase high-density lipoprotein (HDL)-cholesterol and improve HDL function. Furthermore, several trials explored its effects on flow-mediated dilation (FMD), as an index of endothelial function. The authors evaluated the effect of pitavastatin therapy on FMD. METHODS: The authors performed a systematic review and meta-analysis of all clinical trials exploring the impact of pitavastatin on FMD...
January 15, 2018: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29298773/the-phenomenon-of-albumin-mediated-hepatic-uptake-of-organic-anion-transport-polypeptide-substrates-prediction-of-the-in-vivo-uptake-clearance-from-the-in-vitro-uptake-by-isolated-hepatocytes-using-a-facilitated-dissociation-model
#10
Seiji Miyauchi, Masayuki Masuda, Soo-Jin Kim, Yuudai Tanaka, Kyeong Ryoon Lee, Shouko Iwakado, Momoko Nemoto, Shotaro Sasaki, Kazumi Shimono, Yoshio Tanaka, Yuichi Sugiyama
The effects of bovine serum albumin (BSA) and human serum albumin (HSA) on the unbound hepatic uptake clearance (PSu,inf) of the organic anion transporting polypeptide (Oatp/OATP) substrates 1-anilino-8-naphthalene sulfonate (ANS) and pitavastatin (PTV) were determined using primary cultured hepatocytes of rat and isolated hepatocytes of human, respectively. The PSu,inf value of hepatocytes was estimated by dividing the initial uptake rate of these anions by their unbound concentrations. The PSu,inf values for ANS and PTV were enhanced in the presence of albumin, thereby demonstrating the phenomenon of "albumin-mediated" hepatic uptake...
January 3, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29273744/pitavastatin-nanoparticle-engineered-endothelial-progenitor-cells-repair-injured-vessels
#11
Huanyun Liu, Pang Bao, Lufeng Li, Yuqing Wang, Chunxin Xu, Mengyang Deng, Jihang Zhang, Xiaohui Zhao
Endothelial progenitor cells (EPC) participate in vessel recovery and maintenance of normal endothelial function. Therefore, pitavastatin-nanoparticles (NPs)-engineered EPC may be effective in repairing injured vasculature. Pitavastatin-loaded poly(lactic-co-glycolic) acid (PLGA) NPs were obtained via ultrasonic emulsion solvent evaporation with PLGA as the carrier encapsulating pitavastatin. The effects and mechanism of pitavastatin-NPs on EPC proliferation in vitro were evaluated. Then, EPC that internalized pitavastatin-NPs were transplanted into rats after carotid artery injury...
December 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29212965/effects-of-ezetimibe-statin-combination-therapy-on-coronary-atherosclerosis-in-acute-coronary-syndrome
#12
Kiyoshi Hibi, Shinjo Sonoda, Masanori Kawasaki, Yutaka Otsuji, Toyoaki Murohara, Hideki Ishii, Katsuhiko Sato, Ryoji Koshida, Yukio Ozaki, Masataka Sata, Yoshihiro Morino, Tadashi Miyamoto, Tetsuya Amano, Satoshi Morita, Ken Kozuma, Kazuo Kimura, Hisayoshi Fujiwara
BACKGROUND: The results of previous clinical trials on the effects of ezetimibe-statin combination therapy on atherosclerosis are inconsistent, and the anti-atherosclerotic effect of ezetimibe remains controversial.Methods and Results:We conducted a prospective, randomized open-label study at 10 centers. One hundred and twenty-eight statin-naïve patients with acute coronary syndrome (ACS) undergoing intravascular ultrasound (IVUS)-guided percutaneous coronary intervention were randomized to receive either 2 mg/day pitavastatin plus 10 mg/day ezetimibe, or 2 mg/day pitavastatin...
December 7, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/29187694/efficacy-and-safety-of-pitavastatin-in-children-and-adolescents-with-familial-hypercholesterolemia-in-japan-and-europe
#13
Mariko Harada-Shiba, John J P Kastelein, G Kees Hovingh, Kausik K Ray, Akira Ohtake, Osamu Arisaka, Takao Ohta, Tomoo Okada, Hideki Suganami, Albert Wiegman
AIM: Children with Familial Hypercholesterolemia (FH) are widely prescribed statins, and it has been suggested that the effects of statins differ among ethnicities. We compared the efficacy and safety of pitavastatin in children and adolescents with FH in clinical trials conducted in Japan and Europe. METHODS: Low-density lipoprotein cholesterol (LDL-C) reductions, adjusted for confounding factors, and safety were compared between the studies in Japan and Europe...
November 29, 2017: Journal of Atherosclerosis and Thrombosis
https://www.readbyqxmd.com/read/29180851/differences-of-statin-activity-in-2d-and-3d-pancreatic-cancer-cell-cultures
#14
Miglė Paškevičiūtė, Vilma Petrikaitė
Purpose: To evaluate the anticancer activity of lovastatin (LOVA), mevastatin (MEVA), pitavastatin (PITA), and simvastatin (SIMVA) in 2D and 3D models of three human pancreatic cancer cell lines (BxPC-3, MIA PaCa-2, and PANC-1). Methods: The effect of statins on cell viability was estimated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test. The activity of statins in 3D pancreatic cancer cell cultures was examined by measuring the size change of spheroids...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29107984/treatment-with-proteasome-inhibitor-bortezomib-decreases-organic-anion-transporting-polypeptide-oatp-1b3-mediated-transport-in-a-substrate-dependent-manner
#15
Khondoker Alam, Taleah Farasyn, Alexandra Crowe, Kai Ding, Wei Yue
OATP1B1 and OATP1B3 mediate hepatic uptake of many drugs (e.g., statins) and can mediate transporter-mediated drug-drug-interactions (DDIs). Bortezomib is the first-in-class proteasome inhibitor drug approved by the U. S. Food and Drug Administration for the treatment of multiple myeloma. The potential of bortezomib to cause OATP-mediated DDIs has not been assessed. The current study investigated the involvement of the ubiquitin-proteasome system (UPS) in OATP1B1 and OATP1B3 degradation and determined the effects of proteasome inhibitors on OATP1B1- and OATP1B3-mediated transport...
2017: PloS One
https://www.readbyqxmd.com/read/29089470/pitavastatin-attenuates-ages-induced-mitophagy-via-inhibition-of-ros-generation-in-the-mitochondria-of-cardiomyocytes
#16
Zhimin Zha, Junhong Wang, Shiling Li, Yan Guo
This study aimed to investigate whether pitavastatin protected against injury induced by advanced glycation end products products (AGEs) in neonatal rat cardiomyocytes, and to examine the underlying mechanisms. Cardiomyocytes of neonatal rats were incubated for 48 hours with AGEs (100mg/mL), receptor for advanced glycation end products (RAGE), antibody (1 mg/mL) and pitavastatin (600 ng/mL). The levels of p62 and beclin1 were determined by Western blotting. Mitochondrial membrane potential (DYm) and the generation of reactive oxygen species (ROS) were measured through the JC-1 and DCFH-DA...
November 1, 2017: Journal of Biomedical Research
https://www.readbyqxmd.com/read/29078817/long-term-effects-of-high-dose-pitavastatin-on-diabetogenicity-in-comparison-with-atorvastatin-in-patients-with-metabolic-syndrome-less-dm-study-protocol-for-a-randomized-controlled-trial
#17
Jun-Bean Park, Ji-Hyun Jung, Yeonyee E Yoon, Hack-Lyong Kim, Seung-Pyo Lee, Hyung-Kwan Kim, Yong-Jin Kim, Goo-Yeong Cho, Dae-Won Sohn
BACKGROUND: The diabetogenic action of statins remains a concern, particularly in patients at high risk for diabetes receiving intensive statin therapy. Despite the risk of diabetes with statin use being considered a potential class effect, recent studies have suggested that pitavastatin exerts neutral or favorable effects on diabetogenicity. However, no randomized trial has compared the long-term effects of pitavastatin with those of other statins on glycemic control in populations at high risk for diabetes...
October 27, 2017: Trials
https://www.readbyqxmd.com/read/29067253/evidence-based-review-of-statin-use-in-patients-with-hiv-on-antiretroviral-therapy
#18
REVIEW
Daniel B Chastain, Kayla R Stover, Daniel M Riche
INTRODUCTION: As a result of improved safe and effective therapeutic options for human immunodeficiency virus (HIV), life expectancy of those living with HIV is increasing leading to new challenges (e.g., management of chronic diseases). Some chronic diseases (e.g., cardiovascular disease [CVD]), are up to two times more prevalent in patients with HIV. Statins are a mainstay of therapy for prevention of CVD; but, clinicians should be aware that not all statins are appropriate for use in the HIV population, especially those receiving antiretroviral therapy (ART)...
June 2017: Journal of Clinical & Translational Endocrinology
https://www.readbyqxmd.com/read/29066168/patterns-and-predictors-of-physician-adoption-of-new-cardiovascular-drugs
#19
Timothy S Anderson, Wei-Hsuan Lo-Ciganic, Walid F Gellad, Rouxin Zhang, Haiden A Huskamp, Niteesh K Choudhry, Chung-Chou H Chang, Seth Richards-Shubik, Hasan Guclu, Bobby Jones, Julie M Donohue
BACKGROUND: Little is known about physicians' approaches to adopting new cardiovascular drugs and how adoption varies between drugs of differing novelty. METHODS: Using data on dispensed prescriptions from IMS Health's Xponent™ database, we created a cohort of all primary care physicians (PCPs) and cardiologists in Pennsylvania who regularly prescribed anticoagulants, antihypertensives and statins from 2007 to 2011. We examined prescribing of three new cardiovascular drugs of differing novelty: dabigatran, aliskiren and pitavastatin...
October 21, 2017: Healthcare
https://www.readbyqxmd.com/read/29030460/hmg-coa-reductase-inhibition-delays-dna-repair-and-promotes-senescence-after-tumor-irradiation
#20
Elena V Efimova, Natalia Ricco, Edwardine Labay, Helena J Mauceri, Amy C Flor, Aishwarya Ramamurthy, Harold G Sutton, Ralph R Weichselbaum, Stephen J Kron
Despite significant advances in combinations of radiotherapy and chemotherapy, altered fractionation schedules and image-guided radiotherapy, many cancer patients fail to benefit from radiation. A prevailing hypothesis is that targeting repair of DNA double strand breaks (DSBs) can enhance radiation effects in the tumor and overcome therapeutic resistance without incurring off-target toxicities. Unrepaired DSBs can block cancer cell proliferation, promote cancer cell death and induce cellular senescence. Given the slow progress to date translating novel DSB repair inhibitors as radiosensitizers, we have explored drug repurposing, a proven route to improving speed, costs and success rates of drug development...
October 13, 2017: Molecular Cancer Therapeutics
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