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Pharmacokinetic

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https://www.readbyqxmd.com/read/28651249/administration-of-the-mitochondrial-permeability-transition-pore-inhibitor-tro40303-prior-to-primary-percutaneous-coronary-intervention-does-not-affect-the-levels-of-pro-inflammatory-cytokines-or-acute-phase-proteins
#1
Noreen Butt, Lena K Bache-Mathiesen, Jan Erik Nordrehaug, Vegard Tuseth, Peter Scott Munk, Vernon Bonarjee, Trygve Sundby Hall, Svend Eggert Jensen, Sigrun Halvorsen, Huseyin Firat, Dan Atar, Alf Inge Larsen
OBJECTIVES: In the MITOCARE study, reperfusion injury was not prevented after administration of the mitochondrial permeability transition pore (mPTP) opening inhibitor, TRO40303, in patients with ST-segment elevation myocardial infarction (STEMI) treated with primary percutaneous coronary intervention (pPCI). The effects of TRO40303 on pro-inflammatory cytokines and acute-phase proteins were assessed. METHODS: STEMI patients (n = 163, mean age 62 years) with chest pain within 6 h before admission for pPCI were randomized to intravenous bolus of TRO40303 (n = 83) or placebo (n = 80) prior to reperfusion...
June 27, 2017: Cardiology
https://www.readbyqxmd.com/read/28651154/new-comprehensive-studies-of-a-gold-iii-dithiocarbamate-complex-with-proven-anticancer-properties-aqueous-dissolution-with-cyclodextrins-pharmacokinetics-and-upstream-inhibition-of-the-ubiquitin-proteasome-pathway
#2
Marianna F Tomasello, Chiara Nardon, Valeria Lanza, Giuseppe Di Natale, Nicolò Pettenuzzo, Stefano Salmaso, Danilo Milardi, Paolo Caliceti, Giuseppe Pappalardo, Dolores Fregona
The gold(III)-dithiocarbamate complex AuL12 (dibromo [ethyl-N-(dithiocarboxy-kS,kS')-N-methylglycinate] gold(III)), is endowed with promising in vitro/in vivo antitumor activity and toxicological profile. Here, we report our recent strategies to improve its water solubility and stability under physiological conditions along with our efforts for unravelling its tangled mechanism of action. We used three types of α-cyclodextrins (CDs), namely β-CD, Me-β-CD and HP-β-CD to prepare aqueous solutions of AuL12...
June 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28651055/pharmacokinetic-characterization-of-18-f-ucb-h-pet-radiopharmaceutical-in-the-rat-brain
#3
Guillaume Becker, Corentin Warnier, Maria Elisa Serrano, Mohamed Ali Bahri, Joël Mercier, Christian Lemaire, Eric Salmon, André Luxen, Alain Plenevaux
The synaptic vesicle glycoprotein 2A (SV2A), a protein essential to the proper nervous system function, is found in presynaptic vesicles. Thus, SV2A targeting, using dedicated radiotracers combined with positron emission tomography (PET), allows the assessment of synaptic density in the living brain. The first-in-class fluorinated SV2A specific radioligand, [(18)F]UCB-H, is now available at high-activity through an efficient radiosynthesis compliant with the current good manufacturing practices (cGMP). We report here a non-invasive method to quantify [(18)F]UCB-H binding in rat brain with microPET...
June 26, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28650720/nonclinical-development-of-env905-difluprednate-ophthalmic-implant-for-the-treatment-of-inflammation-and-pain-associated-with-ocular-surgery
#4
Rozemarijn S Verhoeven, Andres Garcia, RiLee Robeson, Brian C Gilger, David Culp, Craig Struble, Lee Hamm, Tomas Navratil, Benjamin Yerxa
PURPOSE: Topical corticosteroids are widely used in the treatment of inflammation and pain after ocular surgery, but they possess several shortcomings, including frequent dosing and low patient adherence. We evaluated the efficacy and pharmacokinetics of ENV905 (difluprednate or DFBA) Ophthalmic Implant, a single-dose drug delivery system, compared with 0.05% Durezol. METHODS: PRINT(®) technology was used to fabricate ENV905 implants for either intracameral (IC) or subconjunctival (SCJ) delivery of extended-release DFBA...
June 26, 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28650650/prodrugs-of-pyrazolo-3-4-d-pyrimidines-from-library-synthesis-to-evaluation-as-potential-anticancer-agents-in-an-orthotopic-glioblastoma-model
#5
Giulia Vignaroli, Giulia Iovenitti, Claudio Zamperini, Federica Coniglio, Pierpaolo Calandro, Alessio Molinari, Anna Lucia Fallacara, Andrea Sartucci, Alessia Calgani, David Colecchia, Andrea Mancini, Claudio Festuccia, Elena Dreassi, Massimo Valoti, Francesca Musumeci, Mario Chiariello, Adriano Angelucci, Maurizio Botta, Silvia Schenone
Pyrazolo[3,4-d]pyrimidines are potent protein kinase inhibitors with promising antitumor activity but suboptimal aqueous solubility, consequently worth to be further optimized. Herein, we present the one-pot two-step procedure for the synthesis of a set of pyrazolo[3,4-d]pyrimidine prodrugs (1a-9a,e) with higher aqueous solubility and enhanced pharmacokinetic and therapeutic properties. ADME studies demonstrated for the most promising prodrugs a better aqueous solubility, a favorable hydrolysis in human and murine serum and an increased ability to cross cell membranes with respect to the parental drugs, explaining their better 24h in vitro cytotoxicity against human glioblastoma U87 cell line...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28650526/a-dual-administration-microtracer-technique-to-characterize-the-absorption-distribution-metabolism-and-excretion-of-14-c-seletalisib-ucb5857-in-healthy-subjects
#6
Eric Helmer, Jean-Marie Nicolas, Jeff Long, Ad F Roffel, Emma Jones, Hugues Chanteux, Nieves Diaz, Holly Garratt, Tjerk Bosje
Phosphoinositide 3 kinases are targets for development of small-molecule inhibitors to disrupt progression of immune-inflammatory diseases. This phase 1 open-label study (Eudract 2014-005353-39) evaluated the safety and relative bioavailability of 2 new seletalisib (UCB5857) formulations (A and B) compared with a reference formulation. Absolute bioavailability (period 1a, n = 6) and disposition and metabolism (period 1b, n = 6) of the reference formulation were evaluated: healthy subjects received 30 mg orally plus ∼20 μg of a (14) C-labeled microtracer (intravenously in 1a, orally in 1b)...
June 26, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28650363/population-pharmacokinetics-and-pharmacodynamic-target-attainment-of-vancomycin-in-neonates-on-extracorporeal-life-support
#7
Jeffrey J Cies, Wayne S Moore, Kristen Nichols, Chad A Knoderer, Dominick M Carella, Arun Chopra
OBJECTIVES: To evaluate the population pharmacokinetics and pharmacodynamic target attainment of vancomycin in neonates with a contemporary ¼-inch extracorporeal life support circuit with a Quadrox-iD Pediatric oxygenator (Maquet Cardiovascular, LLC, Wayne, NJ). DESIGN: Retrospective medical record review. SETTING: Two free-standing tertiary/quaternary pediatric children's hospitals. PATIENTS: Neonates receiving either veno-arterial or veno-venous extracorporeal life support and vancomycin for empiric or definitive therapy with resulting serum concentrations...
June 22, 2017: Pediatric Critical Care Medicine
https://www.readbyqxmd.com/read/28650232/pharmacokinetics-of-cyclophosphamide-and-4-hydroxycyclophosphamide-in-cats-after-oral-intravenous-and-intraperitoneal-administration-of-cyclophosphamide
#8
Katherine A Stroda, Jacqueline D Murphy, Ryan J Hansen, Lisa Brownlee, Elizabeth A Atencio, Daniel L Gustafson, Susan E Lana
OBJECTIVE To characterize pharmacokinetics of cyclophosphamide and 4-hydoxycyclophosphamide (4-OHCP) in the plasma of healthy cats after oral, IV, and IP administration of cyclophosphamide. ANIMALS 6 healthy adult cats. PROCEDURES Cats were randomly assigned to receive cyclophosphamide (200 mg/m(2)) via each of 3 routes of administration (oral, IV, and IP); there was a 30-day washout period between successive treatments. Plasma samples were obtained at various time points for up to 8 hours after administration...
July 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28650231/pharmacokinetics-and-safety-of-ceftiofur-crystalline-free-acid-in-new-zealand-white-rabbits-oryctolagus-cuniculus
#9
Sara Gardhouse, David Sanchez-Migallon Guzman, Sherry Cox, Philip H Kass, Tracy L Drazenovich, Barbara A Byrne, Michelle G Hawkins
OBJECTIVE To determine the pharmacokinetics and adverse effects following SC administration of ceftiofur crystalline free acid (CCFA) in New Zealand White rabbits. ANIMALS 6 adult sexually intact female New Zealand White rabbits. PROCEDURES Each rabbit was administered 40 mg of CCFA/kg SC. A blood sample was obtained immediately before (0 minutes), at 5 and 30 minutes after, and at 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 95, 120, 144, and 168 hours after administration, and plasma concentrations of ceftiofur free acid equivalents (CFAE) were measured...
July 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28650129/in-vitro-efficacy-and-in-silico-analysis-of-cefixime-ofloxacin-combination-for-salmonella-typhi-from-bloodstream-infection
#10
Yamuna Devi Bakthavatchalam, Thirumal Kumar D, Iftikhar Aslam Tayubi, Baby Abirami S, Priyanka Babu, Elakkiya Munusamy, Bhuvaneswari Thukkaram, Raji Ravi, George Priya Doss C, Balaji Veeraraghavan
AIMS: Recently, the cefixime-ofloxacin combination is approved by drug controller general of India (DCGI) to treat typhoid fever. We sought to evaluate the antimicrobial activity of cefixime-ofloxacin combination against S. Typhi. METHODS AND RESULTS: 283 non-duplicate S. Typhi isolates collected during 2012 to 2014 were included in this study. Minimum inhibitory concentration (MIC) of cefixime and ofloxacin was determined by using broth microdilution method. Combinational testing was performed by using checkerboard assay...
June 26, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28649898/a-review-of-body-composition-and-pharmacokinetics-in-oncology
#11
Jessica J Hopkins, Michael B Sawyer
Body surface area dosing of chemotherapeutic agents is based on limited scientific data, and often results in unpredictable plasma drug levels. Cross-sectional computed tomography (CT) imaging provides an accurate measurement of lean mass. This review summarizes emerging roles of lean mass in predicting pharmacokinetics and drug toxicities in cancer patients. Areas covered: A concise review of body composition measurement with CT cross-sectional imaging and its relationship to drug pharmacokinetics and toxicities...
June 26, 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/28649895/the-safety-and-efficacy-of-palbociclib-in-the-treatment-of-metastatic-breast-cancer
#12
Johannes Ettl, Nadia Harbeck
Palbociclib (Ibrance(®)) is the first-in-class CDK4/6 inhibitor which has been introduced into clinical practice for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer (MBC). It is an orally administered drug, which acts by selectively inhibiting cyclin-dependant kinases CDK4 and CDK6. Given together with anti-estrogens like letrozole and fulvestrant it enhances the antiproliferative effect of these drugs without compromising the favorable toxicity profile of endocrine therapy...
June 26, 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/28649788/pharmacokinetics-and-dynamics-of-mycophenolate-mofetil-after-single-dose-oral-administration-in-juvenile-dachshunds
#13
M Grobman, D M Boothe, H Rindt, B G Williamson, M L Katz, J R Coates, C R Reinero
Mycophenolate mofetil (MMF) is recommended as an alternative/complementary immunosuppressant. Pharmacokinetic and dynamic effects of MMF are unknown in young-aged dogs. We investigated the pharmacokinetics and pharmacodynamics of single oral dose MMF metabolite, mycophenolic acid (MPA), in healthy juvenile dogs purpose-bred for the tripeptidyl peptidase 1 gene (TPP1) mutation. The dogs were heterozygous for the mutation (nonaffected carriers). Six dogs received 13 mg/kg oral MMF and two placebo. Pharmacokinetic parameters derived from plasma MPA were evaluated...
June 25, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28649438/translational-learning-from-clinical-studies-predicts-drug-pharmacokinetics-across-patient-populations
#14
Markus Krauss, Ute Hofmann, Clemens Schafmayer, Svitlana Igel, Jan Schlender, Christian Mueller, Mario Brosch, Witigo von Schoenfels, Wiebke Erhart, Andreas Schuppert, Michael Block, Elke Schaeffeler, Gabriele Boehmer, Linus Goerlitz, Jan Hoecker, Joerg Lippert, Reinhold Kerb, Jochen Hampe, Lars Kuepfer, Matthias Schwab
Early indication of late-stage failure of novel candidate drugs could be facilitated by continuous integration, assessment, and transfer of knowledge acquired along pharmaceutical development programs. We here present a translational systems pharmacology workflow that combines drug cocktail probing in a specifically designed clinical study, physiologically based pharmacokinetic modeling, and Bayesian statistics to identify and transfer (patho-)physiological and drug-specific knowledge across distinct patient populations...
2017: NPJ Systems Biology and Applications
https://www.readbyqxmd.com/read/28649429/hd-physiology-project-japanese-efforts-to-promote-multilevel-integrative-systems-biology-and-physiome-research
#15
Kazuharu Furutani, Kunichika Tsumoto, Yoshihisa Kurachi
The HD Physiology Project is a Japanese research consortium that aimed to develop methods and a computational platform in which physiological and pathological information can be described in high-level definitions across multiple scales of time and size. During the 5 years of this project, an appropriate software platform for multilevel functional simulation was developed and a whole-heart model including pharmacokinetics for the assessment of the proarrhythmic risk of drugs was developed. In this article, we outline the description and scientific strategy of this project and present the achievements and influence on multilevel integrative systems biology and physiome research...
2017: NPJ Systems Biology and Applications
https://www.readbyqxmd.com/read/28649245/camelid-single-domain-antibodies-as-an-alternative-to-overcome-challenges-related-to-the-prevention-detection-and-control-of-neglected-tropical-diseases
#16
REVIEW
Carla F C Fernandes, Soraya Dos S Pereira, Marcos B Luiz, Juliana P Zuliani, Gilvan P Furtado, Rodrigo G Stabeli
Due mainly to properties such as high affinity and antigen specificity, antibodies have become important tools for biomedical research, diagnosis, and treatment of several human diseases. When the objective is to administer them for therapy, strategies are used to reduce the heterologous protein immunogenicity and to improve pharmacokinetic and pharmacodynamic characteristics. Size minimization contributes to ameliorate these characteristics, while preserving the antigen-antibody interaction site. Since the discovery that camelids produce functional antibodies devoid of light chains, studies have proposed the use of single domains for biosensors, monitoring and treatment of tumors, therapies for inflammatory and neurodegenerative diseases, drug delivery, or passive immunotherapy...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28649066/simultaneous-determination-and-pharmacokinetics-of-eight-ginsenosides-by-lc-ms-ms-after-intravenously-infusion-of-shenmai-injection-in-dogs
#17
Jian Yu, Li-Qiang Gu, Yan-Fei Xin, Hai-Yan Gao, Xiao-Zhen Xu, Sheng Zhang, Guo-Liang Zhou, Zhen-Qiang You, Li-Ru Huo, Yao-Xian Xuan
SHENMAI injection, a prescription comprised of Panax ginseng and Ophiopogon japonicas, is being extensively applied in the field of cardio-protection and immune-modulation in China. Ginsenosides are the main active components in SHENMAI injection. In order to capture and analyze the pharmacokinetic profile of major ginsenosides of SHENMAI injection in Beagle dogs, liquid chromatography equipped with electro-spray ionization and tandem mass spectrometry method was applied in simultaneous determination for protopanaxatriol type ginsenoside (Re, Rf, Rg1), protopanaxadiol type ginsenoside (Rb2, Rb1, Rd, Rc) and oleanolic acid type ginsenoside (Ro)...
March 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28648785/lc-ms-bioanalysis-of-trastuzumab-and-released-emtansine-using-nano-surface-and-molecular-orientation-limited-nsmol-proteolysis-and-liquid-liquid-partition-in-plasma-of-trastuzumab-emtansine-treated-breast-cancer-patients
#18
Noriko Iwamoto, Akihiko Shimomura, Kenji Tamura, Akinobu Hamada, Takashi Shimada
Antibody-drug conjugates (ADCs) consist of monoclonal antibody and cytotoxic drugs covalently attached via stable crosslinkers, and are prospective antibody drugs for cancer therapy. To cover the overall pharmacokinetic understanding of ADCs, both the antibody and the released drugs are necessary for practical clinical observation. The nano-surface and molecular-orientation limited (nSMOL) proteolysis is a universal approach for antibody bioanalysis that enable Fab-selective proteolysis, which maintains antibody sequence specificity while decreasing excess analyte peptides...
June 19, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28648684/hbk-15-protects-mice-from-stress-induced-behavioral-disturbances-and-changes-in-corticosterone-bdnf-and-ngf-levels
#19
Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Elżbieta Żmudzka, Magdalena Jakubczyk, Anna Waszkielewicz, Paulina Janiszewska, Maria Walczak
Unlike majority of current antidepressants, HBK-15-a 5-HT1A and 5-HT7 receptor antagonist - showed memory-enhancing properties. In this study, we aimed to further characterize pharmacological profile of HBK-15 and investigate its antidepressant- and anxiolytic-like activity in the mouse model of unpredictable chronic mild stress. We used sucrose consumption test, forced swim test and elevated plus maze and evaluated the influence on brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF) levels in the hippocampus and prefrontal cortex, as well as body weight, relative adrenal glands weight and plasma corticosterone level in the stressed mice...
June 22, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28648640/pulmonary-delivery-of-synergistic-combination-of-fluoroquinolone-antibiotic-complemented-with-proteolytic-enzyme-a-novel-antimicrobial-and-antibiofilm-strategy
#20
Purnima V Gupta, Abhijit M Nirwane, Tejashree Bellubi, Mangal S Nagarsenker
Bacterial resistance remains a major hindrance in treatment with antimicrobial agents. Therefore, we assessed the improved antimicrobial and antibiofilm activity of Levofloxacin (LFX) and Serratiopeptidase (SRP) combinations in in vitro microbiological studies. Further, pharmacodynamic and pharmacokinetic studies of liposomal LFX in combination with SRP (LFX liposome-SRP) were performed in S. aureus infected rats. LFX at sub-MIC with SRP eradicated >90% of the preformed biofilm. The entrapment efficiency of LFX in liposome was >80% and the co-spray dried product had MMAD <5μ...
June 22, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
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