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https://www.readbyqxmd.com/read/29454264/development-and-validation-of-uplc-ms-ms-assay-for-quantification-of-cladrin-absolute-bioavailability-and-dose-proportionality-study-in-rats
#1
Mamunur Rashid, Sandeep K Singh, Mohd Yaseen Malik, Sadaf Jahan, Swati Chaturvedi, Isha Taneja, Kanumuri Sivarama Raju, Zaiba Naseem, J R Gayen, Muhammad Wahajuddin
Cladrin, an isoflavone is a major bioactive constituent found in stem bark of Butea monosperma with remarkable osteogenic activity. A speedy and sensitive UPLC coupled tandem mass spectrometry (UPLC-MS/MS) method was developed, validated and successfully applied to bioavailability, blood partitioning, plasma protein binding, intravenous and multiple-dose oral pharmacokinetics of cladrin in rats. Separation was done on C18 column (5.0 μm, 4.6 × 50 mm) using mobile phase containing acetonitrile and 0.10% formic acid in the ratio of 65:35 (v/v) with 0...
January 31, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29454237/liposomes-of-dimeric-artesunate-phospholipid-a-combination-of-dimerization-and-self-assembly-to-combat-malaria
#2
Muhammad Ismail, Longbing Ling, Yawei Du, Chen Yao, Xinsong Li
Artemisinin and its derivatives are highly effective drugs in the treatment of P. falciparum malaria. However, their clinical applications face challenges because of short half-life, poor bioavailability and growing drug resistance. In this article, novel dimeric artesunate phospholipid (Di-ART-GPC) based liposomes were developed by combination of dimerization and self-assembly to address these shortcomings. Firstly, Di-ART-GPC conjugate was synthesized by a facile esterification of artesunate (ART) and glycerophosphorylcholine (GPC) and confirmed by MS, 1 H NMR and 13 C NMR...
February 10, 2018: Biomaterials
https://www.readbyqxmd.com/read/29454114/mitochondria-targeting-mitochondrial-reactive-oxygen-species-with-mitochondriotropic-polyphenolic-based-antioxidants
#3
José Teixeira, Cláudia M Deus, Fernanda Borges, Paulo J Oliveira
Mitochondrial function and regulation of redox balance is fundamental in controlling cellular life and death pathways. Antioxidants have been used to counteract disruption of redox networks, normally associated with progressive loss of cell homeostasis and disease pathophysiology, although therapeutic success is limited mainly due to pharmacokinetic drawbacks. Attempts to improve mitochondrial function in a range of diseases spurred active drug discovery efforts. Currently, the most effective strategy to deliver drugs to mitochondria is the covalent link of lipophilic cations to the bioactive compound...
February 14, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29454062/laser-assisted-delivery-of-synergistic-combination-chemotherapy-in-in-vivo-skin
#4
Emily Wenande, Joshua Tam, Brijesh Bhayana, Steven Kyle Schlosser, Emily Ishak, William A Farinelli, Agata Chlopik, Mai P Hoang, Omar R Pinkhasov, Peter Caravan, R Rox Anderson, Merete Haedersdal
The effectiveness of topical drugs for treatment of non-melanoma skin cancer is greatly reduced by insufficient penetration to deep skin layers. Ablative fractional lasers (AFLs) are known to enhance topical drug uptake by generating narrow microchannels through the skin, but information on AFL-drug delivery in in vivo conditions is limited. In this study, we examined pharmacokinetics, biodistribution and toxicity of two synergistic chemotherapy agents, cisplatin and 5-fluorouracil (5-FU), following AFL-assisted delivery alone or in combination in in vivo porcine skin...
February 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29453787/a-phase-ii-trial-of-riluzole-an-antagonist-of-metabotropic-glutamate-receptor-1-grm1-signaling-in-patients-with-advanced-melanoma
#5
Janice M Mehnert, Ann W Silk, Yu Wen, J H Lee, Liesel Dudek, Byeong-Seon Jeong, Jiadong Li, Jason M Schenkel, Evita Sadimin, Michael Kane, Hongxia Lin, Weichung J Shih, Andrew Zloza, Suzie Chen, James S Goydos
Studies demonstrate that GRM, expressed by >60% of human melanomas, may be a therapeutic target. We performed a phase II trial of 100 mg po bid of riluzole, an inhibitor of GRM1 signaling, in patients with advanced melanoma with the primary endpoint of response rate. Thirteen patients with GRM1-positive tumors were enrolled. No objective responses were observed and accrual was stopped. Stable disease was noted in 6 (46%) patients, with 1 patient on study for 42 weeks. Riluzole was well-tolerated, with fatigue (62%) as the most common adverse event...
February 17, 2018: Pigment Cell & Melanoma Research
https://www.readbyqxmd.com/read/29453777/intramuscular-allopregnanolone-and-ganaxolone-in-a-mouse-model-of-treatment-resistant-status-epilepticus
#6
Dorota Zolkowska, Chun-Yi Wu, Michael A Rogawski
Allopregnanolone (5α-pregnan-3α-ol-20-one) and its synthetic 3β-methyl analog, ganaxolone, are positive allosteric modulators of synaptic and extrasynaptic γ-aminobutyric acid (GABA) A receptors that exhibit antiseizure activity in diverse animal seizure models, including models of status epilepticus (SE). The 2 neuroactive steroids are being investigated as treatments for SE, including as a treatment for SE induced by chemical threat agents. Intramuscular injection is the preferred route of administration in the prehospital treatment of SE...
February 17, 2018: Epilepsia
https://www.readbyqxmd.com/read/29453687/impact-of-boosted-antiretroviral-therapy-on-the-pharmacokinetics-and-efficacy-of-clopidogrel-and-prasugrel-active-metabolites
#7
Niloufar Marsousi, Youssef Daali, Pierre Fontana, Jean-Luc Reny, Virginie Ancrenaz-Sirot, Alexandra Calmy, Serge Rudaz, Jules Alexandre Desmeules, Caroline Flora Samer
BACKGROUND AND OBJECTIVES: Prasugrel and clopidogrel are inhibitors of the ADP-P 2 Y 12 platelet receptor used in acute coronary syndrome patients. They require bioactivation via isoenzymes such as cytochrome P450 (CYP) 3A4, CYP2C19 and CYP2B6. Ritonavir and cobicistat are potent CYP3A inhibitors, prescribed as pharmacokinetic (PK) enhancers in the treatment of human immunodeficiency virus (HIV) infection. METHODS: In this study, the impact of boosted antiretroviral therapies (ARTs) on the PK of clopidogrel and prasugrel active metabolites (AMs), and on the efficacy of prasugrel and clopidogrel, were evaluated in a randomized crossover clinical trial...
February 16, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29453681/-18-f-fpybf-2-a-new-f-18-labelled-amyloid-imaging-pet-tracer-biodistribution-and-radiation-dosimetry-assessment-of-first-in-man-18-f-fpybf-2-pet-imaging
#8
Ryuichi Nishii, Tatsuya Higashi, Shinya Kagawa, Chio Okuyama, Yoshihiko Kishibe, Masaaki Takahashi, Tomoko Okina, Norio Suzuki, Hiroshi Hasegawa, Yasuhiro Nagahama, Koichi Ishizu, Naoya Oishi, Hiroyuki Kimura, Hiroyuki Watanabe, Masahiro Ono, Hideo Saji, Hiroshi Yamauchi
OBJECTIVE: Recently, a benzofuran derivative for the imaging of β-amyloid plaques, 5-(5-(2-(2-(2- 18 F-fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)- N-methylpyridin-2-amine ( 18 F-FPYBF-2) has been validated as a tracer for amyloid imaging and it was found that 18 F-FPYBF-2 PET/CT is a useful and reliable diagnostic tool for the evaluation of AD (Higashi et al. Ann Nucl Med, https://doi.org/10.1007/s12149-018-1236-1 , 2018). The aim of this study was to assess the biodistribution and radiation dosimetry of diagnostic dosages of 18 F-FPYBF-2 in normal healthy volunteers as a first-in-man study...
February 16, 2018: Annals of Nuclear Medicine
https://www.readbyqxmd.com/read/29453671/comparative-evaluation-of-pharmacokinetics-and-pharmacodynamics-of-insulin-glargine-glaritus-%C3%A2-and-lantus-%C3%A2-in-healthy-subjects-a-double-blind-randomized-clamp-study
#9
Ashima Bhatia, Shraddha Tawade, Mushtaque Mastim, Eliford Ngaimisi Kitabi, Mathangi Gopalakrishnan, Manish Shah, Sridhar Yeshamaina, Joga Gobburu, Maharaj Sahib, Dipak Thakur, K M Prasanna Kumar
AIMS: The objective of the study was to compare the pharmacokinetic (PK) and pharmacodynamic (PD) properties of an insulin glargine formulation, Glaritus ® (test) with the innovator's formulation Lantus ® (reference) using the euglycemic clamp technique in a single-dose, double-blind, randomized, two sequences, four-period replicate crossover study in healthy volunteers (n = 40). METHODS: Subjects received subcutaneous administration of the insulin glargine (0...
February 16, 2018: Acta Diabetologica
https://www.readbyqxmd.com/read/29453635/monitoring-of-erlotinib-in-pancreatic-cancer-patients-during-long-time-administration-and-comparison-to-a-physiologically-based-pharmacokinetic-model
#10
Andrea Gruber, Martin Czejka, Philipp Buchner, Marie Kitzmueller, Nairi Kirchbaumer Baroian, Christian Dittrich, Azra Sahmanovic Hrgovcic
PURPOSE: In this study, a therapeutic drug monitoring (TDM) of erlotinib in pancreatic cancer patients was performed over 50 weeks to reveal possible alterations in erlotinib plasma concentrations. Additionally, a physiologically based pharmacokinetic (PBPK) model was created to assess such variations in silico. METHODS: Patients with advanced pancreatic cancer received a chemotherapeutic combination of 100 mg erlotinib q.d., 500-900 mg capecitabine b.d. and 5 mg/kg bevacizumab q...
February 16, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29453628/safety-tolerability-and-preliminary-activity-of-imgn529-a-cd37-targeted-antibody-drug-conjugate-in-patients-with-relapsed-or-refractory-b-cell-non-hodgkin-lymphoma-a-dose-escalation-phase-i-study
#11
Anastasios Stathis, Ian W Flinn, Sumit Madan, Kami Maddocks, Arnold Freedman, Steven Weitman, Emanuele Zucca, Mihaela C Munteanu, M Lia Palomba
Background CD37 is expressed on B-cell lymphoid malignancies, thus making it an attractive candidate for targeted therapy in non-Hodgkin lymphoma (NHL). IMGN529 is an antibody-drug conjugate comprising a CD37-binding antibody linked to the maytansinoid DM1, a potent anti-mitotic agent. Methods This first-in-human, phase 1 trial recruited adult patients with relapsed or refractory B-cell NHL. The primary objective was to determine the maximum tolerated dose (MTD) and recommended phase 2 dose. Secondary objectives were to evaluate safety, pharmacokinetics, and preliminary clinical activity...
February 17, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29453627/a-phase-i-and-pharmacokinetic-study-of-taladegib-a-smoothened-inhibitor-in-japanese-patients-with-advanced-solid-tumors
#12
Hideki Ueno, Shunsuke Kondo, Shusuke Yoshikawa, Koichi Inoue, Valérie Andre, Masaomi Tajimi, Haruyasu Murakami
Background This phase I dose-escalation study investigated the safety of the Smoothened inhibitor taladegib in Japanese patients with advanced solid tumors. Methods Patients received taladegib orally once daily for 28-day cycles, using a 3 + 3 dose-escalation method. The primary objective was the safety and tolerability of taladegib at doses up to the global recommended dose (400 mg). Secondary objectives included pharmacokinetics, changes in skin glioma-associated oncogene homolog 1 (Gli1) transcript levels, and antitumor activity...
February 17, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29453492/application-of-physiologically-based-pharmacokinetic-modeling-to-the-prediction-of-drug-drug-and-drug-disease-interactions-for-rivaroxaban
#13
Ruijuan Xu, Weihong Ge, Qing Jiang
PURPOSE: Rivaroxaban is a direct oral anticoagulant with a large inter-individual variability. The present study is to develop a physiologically based pharmacokinetic (PBPK) model to predict several scenarios in clinical practice. METHODS: A whole-body PBPK model for rivaroxaban, which is metabolized by the cytochrome P450 (CYP) 3A4/5, 2J2 pathways and excreted via kidneys, was developed to predict the pharmacokinetics at different doses in healthy subjects and patients with hepatic or renal dysfunction...
February 17, 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29453199/simultaneous-assessment-of-clearance-metabolism-induction-and-drug-drug-interaction-potential-using-a-long-term-in-vitro-liver-model-for-a-novel-hepatitis-b-virus-inhibitor
#14
Nicole A Kratochwil, Miriam Triyatni, Martina B Mueller, Florian Klammers, Brian Leonard, Dan Turley, Josephine Schmaler, Aynur Ekiciler, Birgit Molitor, Isabelle Walter, Pierre-Alexis Gonsard, Charles A Tournillac, Alexandre Durrwell, Michaela Marschmann, Russell Jones, Mohammed Ullah, Franziska Boess, Giorgio Ottaviani, Yuyan Yin, Neil J Parrott, Stephen Fowler
Long-term in vitro liver models are now widely explored for human hepatic metabolic clearance prediction, enzyme phenotyping, cross species metabolism, comparison of low clearance drugs as well as induction studies. Here, we present studies using a long-term liver model which show how metabolism and active transport, drug-drug interactions and enzyme induction in healthy and diseased states, e.g. hepatitis B virus (HBV) infection, may be assessed in a single test system to enable effective data integration for PBPK modeling...
February 16, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29453094/a-multidisciplinary-study-of-3-%C3%AE-d-glucopyranosyl-5-substituted-1-2-4-triazole-derivatives-as-glycogen-phosphorylase-inhibitors-computation-synthesis-crystallography-and-kinetics-reveal-new-potent-inhibitors
#15
Sándor Kun, Jaida Begum, Efthimios Kyriakis, Evgenia C V Stamati, Thomas A Barkas, Eszter Szennyes, Éva Bokor, Katalin E Szabó, George A Stravodimos, Ádám Sipos, Tibor Docsa, Pál Gergely, Colin Moffatt, Myrto S Patraskaki, Maria C Kokolaki, Alkistis Gkerdi, Vassiliki T Skamnaki, Demetres D Leonidas, László Somsák, Joseph M Hayes
3-(β-d-Glucopyranosyl)-5-substituted-1,2,4-triazoles have been revealed as an effective scaffold for the development of potent glycogen phosphorylase (GP) inhibitors but with the potency very sensitive to the nature of the alkyl/aryl 5-substituent (Kun et al., Eur. J. Med. Chem. 2014, 76, 567). For a training set of these ligands, quantum mechanics-polarized ligand docking (QM-PLD) demonstrated good potential to identify larger differences in potencies (predictive index PI = 0.82) and potent inhibitors with K i 's < 10 μM (AU-ROC = 0...
February 2, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29453084/solid-lipid-nanoparticles-as-an-efficient-drug-delivery-system-of-olmesartan-medoxomil-for-the-treatment-of-hypertension
#16
Nilima T Pandya, Parva Jani, Jigar Vanza, Hemal Tandel
The aim of the current investigation was to develop solid lipid nanoparticles of olmesartan medoxomil using hot homogenization method to improve its oral bioavailability. Central composite design was applied to optimize the formulation variables; lipid X1 (Glyceryl monostearate) and surfactant X2 (Poloxamer: Tween 80). The particle sizes were in the nanometer range and spherical shaped for all prepared solid lipid nanoparticles formulations and the zeta potential absolute values were high, predicting good long-term stability...
February 9, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29453076/development-of-novel-synthesized-phthalazinone-based-parp-1-inhibitors-with-apoptosis-inducing-mechanism-in-lung-cancer
#17
Hadia Almahli, Elie Hadchity, Maiy Y Jaballah, Racha Daher, Hazem A Ghabbour, Maha M Kabil, Nasser S Al-Shakliah, Wagdy M Eldehna
Herein we report the synthesis of two series of 4-phenylphthalazin-1-ones 11a-i and 4- benzylphthalazin-1-ones 16a-h as anti-lung adenocarcinoma agents with potential inhibitory activity against PARP-1. All the newly synthesized phthalazinones were evaluated for their anti-proliferative activity against A549 lung carcinoma cell line. Phthalazinones 11c-i and 16b, c showed significant cytotoxic activity against A549 cells at different concentrations (0.1, 1 and 10 μM) for two time intervals (24 h and 48 h)...
February 7, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29453075/pharmacokinetic-variability-of-valproate-during-pregnancy-implications-for-the-use-of-therapeutic-drug-monitoring
#18
Cecilie Johannessen Landmark, Anette Huuse Farmen, Margrete Larsen Burns, Arton Baftiu, Morten I Lossius, Svein I Johannessen, Torbjörn Tomson
BACKGROUND AND PURPOSE: Use of valproate (VPA) in women of childbearing age is restricted due to dose-dependent risk of teratogenicity. The purpose of this study was to characterise pharmacokinetic variability of VPA in pregnancy, and discuss use of therapeutic drug monitoring (TDM) as guidance to exposure in women. METHOD: Measurements of trough total and unbound VPA concentrations before, during and after pregnancy, at assumed steady-state were collected from the TDM-database (2006-2016) at the National Center for Epilepsy in Norway...
February 11, 2018: Epilepsy Research
https://www.readbyqxmd.com/read/29452834/pain-and-analgesic-drugs-in-chronic-venous-ulcers-with-topical-sevoflurane-use
#19
Adrian Imbernon-Moya, Francisco Javier Ortiz-de Frutos, Mónica Sanjuan-Alvarez, Isabel Portero-Sanchez, Raúl Merinero-Palomares, Victoria Alcazar
OBJECTIVE: Pain in chronic venous ulcers (CVUs) notably increases with the usual cleaning of the wound. Chronic pain is usually poorly controlled even with the multiple analgesic treatments available. Analgesics can have different serious adverse effects and medical interactions in old patients with several comorbidities. This study reports the efficacy and safety of topical sevoflurane for treatment of pain in CVUs. METHODS: We report a descriptive and retrospective study of 30 patients older than 65 years with painful CVUs refractory to conventional analgesic treatments...
February 13, 2018: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/29452720/evaluation-of-the-biological-activities-of-the-il-15-superagonist-complex-alt-803-following-intravenous-versus-subcutaneous-administration-in-murine-models
#20
Bai Liu, Monica Jones, Lin Kong, Terra Noel, Emily K Jeng, Sixiang Shi, Christopher G England, Sarah Alter, Jeffrey S Miller, Weibo Cai, Peter R Rhode, Hing C Wong
ALT-803 is a fusion protein complex consisting of an interleukin (IL)-15 superagonist and a dimeric IL-15 receptor alpha sushi domain IgG1 Fc fusion protein. When administered to mice, ALT-803 is capable of inducing natural killer (NK) and CD8 + T cell proliferation and activation, and effectively promoting potent anti-tumor responses. Currently, ALT-803 is in clinical trials for treatment of various solid tumors and hematological malignancies. In the initial phase of these clinical studies, intravenous (iv) injection was used according to the route used in pre-clinical efficacy studies...
February 13, 2018: Cytokine
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