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Pharmacokinetic

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https://www.readbyqxmd.com/read/29220876/pharmacokinetics-clot-strength-and-safety-of-a-new-fibrinogen-concentrate-randomized-comparison-with-active-control-in-congenital-fibrinogen-deficiency
#1
C Ross, S Rangarajan, M Karimi, G H Toogeh, S Apte, T Lissitchkov, S Acharya, M J Manco-Johnson, A Srivastava, B Brand, B Schwartz, S Knaub, F Peyvandi
BACKGROUND: Human fibrinogen concentrate (HFC) corrects fibrinogen deficiency in congenital a-/hypofibrinogenaemia. OBJECTIVES: To assess pharmacokinetics (PK), effects on thromboelastometry maximum clot firmness (MCF), and safety of a new double virus-inactivated/eliminated, highly purified HFC vs. active control. PATIENTS/METHODS: In this multinational, randomized, phase II, open-label, crossover study in 22 congenital afibrinogenaemia patients ≥12 years, 70 mg kg-1 of new HFC (FIBRYGA, Octapharma AG) or control (Haemocomplettan® P/RiaSTAP™ , CSL Behring GmbH) were administered, followed by crossover to the other concentrate...
December 8, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/29220724/pharmacokinetics-of-a-novel-triazine-ethanamizuril-in-rats-and-broiler-chickens
#2
Peipei Cheng, Chunmei Wang, Xi Lin, Lifang Zhang, Chenzhong Fei, Keyu Zhang, Juan Zhao, Na Lei, Lili Liu, Shuhua Mu, Xiaoyang Wang, Mi Wang, Wenli Zheng, Yingchun Liu, Chunna Guo, Feiqun Xue
Ethanamizuril is a new triazine compound that displays potent anticoccidial activity against chicken coccidiosis caused by Eimeria tenella. We studied the pharmacokinetics of ethanamizuril in rats and chickens after single oral doses of one, two and three times the minimum effective dose Ethanamizuril was readily absorbed at all three doses and the plasma concentration reached was maximal within 5h and progressively declined over time. The mean peak plasma concentrations (Cmax) and the area under the concentration-time curve (AUC) were both dose-dependent...
November 10, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/29218581/fabrication-of-tip-dissolving-microneedles-for-transdermal-drug-delivery-of-meloxicam
#3
Jianmin Chen, Weiyue Huang, Ziyao Huang, Shiqi Liu, Yaling Ye, Qinglian Li, Meiping Huang
Dissolving microneedles (MNs) offered a simple, minimally invasive method for meloxicam (MX) delivery to the skin. However, the fabrication of dissolving MNs still faced some challenges, such as significant time consumption, loss of drug activity, and difficulty in regulating MN drug loading. To address these issues, we developed the tip-dissolving (TD) MNs. Several kinds of drugs were encapsulated successfully, and the quantity of MX ranged from 37.23 ± 8.40 to 332.53 ± 13.37 μg was precisely controlled...
December 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29218501/evaluating-safety-reporting-in-paediatric-antibiotic-trials-2000-2016-a-systematic-review-and-meta-analysis
#4
REVIEW
Paola Pansa, Yingfen Hsia, Julia Bielicki, Irja Lutsar, A Sarah Walker, Mike Sharland, Laura Folgori
BACKGROUND: There are very few options to treat multidrug-resistant bacterial infections in children. A major barrier is the duration and complexity of regulatory trials of new antibiotics. Extrapolation of safety data from adult trials could facilitate drug development for children. OBJECTIVE: We performed a systematic review on the safety of antibiotic clinical trials (CTs) in children (0-18 years) to evaluate the overall quality of safety trials conducted in children and to determine if age-specific adverse events (AEs) could be identified for specific antibiotic classes...
December 7, 2017: Drugs
https://www.readbyqxmd.com/read/29217763/improved-tumor-penetration-and-single-cell-targeting-of-antibody-drug-conjugates-increases-anticancer-efficacy-and-host-survival
#5
Cornelius Cilliers, Bruna Menezes, Ian Nessler, Jennifer Linderman, Greg Thurber
Current antibody-drug conjugates (ADC) have made advances in engineering the antibody, linker, conjugation site, small molecule payload and drug-to-antibody ratio (DAR). However, the relationship between heterogeneous intratumoral distribution and efficacy of ADC is poorly understood. Here we compared trastuzumab and ado-trastuzumab emtansine (T-DM1) to study the impact of ADC tumor distribution on efficacy. In a mouse xenograft model insensitive to trastuzumab, co-administration of trastuzumab with a fixed dose of T-DM1 at 3:1 and 8:1 ratios dramatically improved ADC tumor penetration and resulted in twice the improvement in median survival compared to T-DM1 alone...
December 7, 2017: Cancer Research
https://www.readbyqxmd.com/read/29217733/sex-as-a-biological-variable-in-preclinical-imaging-research-initial-observations-with-18f-fluorothymidine
#6
Szeman Ruby Chan, Kelley Salem, Justin Jeffery, Ginny L Powers, Yongjun Yan, Kooresh I Shoghi, Aparna M Mahajan, Amy M Fowler
The study objective was to investigate whether sex influences 3'-deoxy-3'-[18F]fluorothymidine (18F-FLT) uptake and tissue distribution in mouse models of cancer. Methods:18F-FLT biodistribution was measured in three strains of male and female mice (129S6/SvEv, athymic nude, and BALB/c). 18F-Fluoro-2-deoxy-2-D-glucose (18F-FDG) biodistribution was performed for comparison. 18F-FLT uptake was also measured in female 129S6/SvEv mice bearing estrogen-dependent SSM3 mouse mammary tumors, male athymic nude mice bearing androgen-dependent CWR22 prostate cancer xenografts, and male and female athymic nude mice bearing estrogen-independent MDA-MB-231 human breast cancer xenografts...
December 7, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29217526/first-in-human-phase-i-study-of-single-agent-vanucizumab-a-first-in-class-bi-specific-anti-ang-2-anti-vegf-antibody-in-adult-patients-with-advanced-solid-tumors
#7
Manuel Hidalgo, Maria Martinez-Garcia, Christophe Le Tourneau, Christophe Massard, Elena Garralda, Valentina Boni, Alvaro Taus, Joan Albanell, Marie-Paule Sablin, Marie Alt, Rastilav Bahleda, Andreea Varga, Christophe Boetsch, Izolda Franjkovic, Florian Heil, Angelika Lahr, Katharina Lechner, Anthony Morel, Tapan K Nayak, Simona Rossomanno, Kevin Smart, Kay-Gunnar Stubenrauch, Oliver Krieter
PURPOSE: Vanucizumab is an investigational anti-angiogenic, first-in-class, bi-specific monoclonal antibody targeting VEGF-A and angiopoietin-2 (Ang-2). This first-in-human study evaluated the safety, pharmacokinetics, pharmacodynamics, and antitumor activity of vanucizumab in adults with advanced solid tumors refractory to standard therapies. EXPERIMENTAL DESIGN: Patients received escalating bi-weekly (q2w; 3-30 mg/kg) or weekly (qw; 10-30 mg/kg) intravenous doses guided by a Bayesian logistic regression model with overdose control...
December 7, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29217384/biocompatible-sulfenamide-and-sulfonamide-derivatives-of-metformin-can-exert-beneficial-effects-on-plasma-haemostasis
#8
Magdalena Markowicz-Piasecka, Kristiina M Huttunen, Elżbieta Mikiciuk-Olasik, Joanna Sikora
As the pharmacokinetic properties of metformin are unfavourable, several analogues and prodrugs have been synthesised to improve its bioavailability. The aim of this study was to assess the plasma stability of sulfenamide and sulfonamide derivatives of metformin and establish their effects on plasma haemostasis and integrity of red blood cells (RBCs). The overall haemostasis potential was evaluated spectrophotometrically by clot formation and lysis test (CL-test). PT (Prothrombin Time) and APTT (Activated Partial Tromboplastin Time) were used to evaluate the effects if the compounds on the extrinsic and intrinsic coagulation pathway...
December 4, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29217300/dynamic-magnetic-resonance-imaging-of-the-breast-comparison-of-gadobutrol-vs-gd-dtpa
#9
F Escribano, M Sentís, J C Oliva, L Tortajada, M Villajos, A Martín, S Ganau
OBJECTIVE: To compare the pharmacokinetic profile of gadobutrol versus Gd-DTPA in dynamic contrast-enhanced MRI (DCE-MRI) in patients with breast cancer. Secondary objectives included comparing the safety profiles and diagnostic efficacy of the two contrast agents for detecting additional malignant lesions. MATERIAL AND METHODS: This retrospective observational study included 400 patients with histologically confirmed breast cancer; 200 underwent DCE-MRI with Gd-DTPA (Magnevist®) and 200 underwent DCE-MRI with gadobutrol (Gadovist®)...
December 4, 2017: Radiología
https://www.readbyqxmd.com/read/29217237/pharmacokinetics-of-magnesium-in-cardiac-surgery-implications-for-prophylaxis-against-atrial-fibrillation
#10
EDITORIAL
Vladimir V Lomivorotov, Sergey M Efremov, Alexander M Karaskov
No abstract text is available yet for this article.
September 20, 2017: Journal of Cardiothoracic and Vascular Anesthesia
https://www.readbyqxmd.com/read/29216752/an-acryl-resin-based-swellable-microneedles-for-controlled-release-intradermal-delivery-of-granisetron
#11
Guozhong Yang, Meilin He, Suohui Zhang, Man Wu, Yunhua Gao
Swellable microneedles (SMNs) are made of hydrogels and can deliver drug with controlled delivery rate by the cross-link density of the hydrogel. In this study, an acryl resin-based SMNs was developed for poorly water-soluble drugs. The making process of the SMNs is very simple and only need 60 min. The SMNs has high mechanical strength and is not easily broken. In-vitro release of SMNs-loaded model drug, granisetron base (GRB), was investigated. The results showed that 7 days controlled release of GRB was obtained when SMNs contained pore-foaming agents (1...
December 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29216583/hplc-ms-ms-analysis-of-mesupron-and-its-application-to-a-pharmacokinetic-study-in-rats
#12
Changmin Park, Joong Gyu Ha, Seungmok Choi, Eunyoung Kim, Keumhan Noh, Beom Soo Shin, Wonku Kang
Mesupron, the first-in-class inhibitor of urokinase-type plasminogen activator (uPA) is known to regulate cell proliferation and migration, and is under investigation for the treatment of metastatic breast cancer. In this study, a quantification method was developed for the determination of mesupron in rat plasma using liquid chromatography with a tandem mass spectrometry (LC-MS/MS). After protein precipitation with acetonitrile including itraconazole (internal standard, IS), the analytes were chromatographed on a reversed phased column with a mobile phase of acetonitrile and water (7:3, v/v, including 0...
December 4, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29216562/substituted-carbamothioic-amine-1-carbothioic-thioanhydrides-as-novel-trichomonicidal-fungicides-design-synthesis-and-biology
#13
Dhanaraju Mandalapu, Bhavana Kushwaha, Sonal Gupta, Shagun Krishna, Nidhi Srivastava, Mahendra Shukla, Pratiksha Singh, Bhavana S Chauhan, Ravi Goyani, Jagdamba P Maikhuri, Koneni V Sashidhara, Brijesh Kumar, Renu Tripathi, Praveen K Shukla, Mohammad I Siddiqi, Jawahar Lal, Gopal Gupta, Vishnu L Sharma
Sexually transmitted diseases like trichomoniasis along with opportunistic fungal infections like candidiasis are major global health burden in female reproductive health. In this context a novel non-nitroimidazole class of substituted carbamothioic amine-1-carbothioic thioanhydride series was designed, synthesized, evaluated for trichomonacidal and fungicidal activities, and was found to be more active than the standard drug Metronidazole (MTZ). Compounds were trichomonicidal in the MIC ranges of 4.77-294...
November 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29216560/identification-of-an-oxime-containing-c-glucosylarene-as-a-potential-inhibitor-of-sodium-dependent-glucose-co-transporter-2
#14
Mao-Chia Yuan, Teng-Kuang Yeh, Chiung-Tong Chen, Jen-Shin Song, Yu-Chen Huang, Tsung-Chih Hsieh, Chung-Yu Huang, Yu-Ling Huang, Min-Hsien Wang, Szu-Huei Wu, Chun-Hsu Yao, Yu-Sheng Chao, Jinq-Chyi Lee
Treatment of hyperglycemia with drugs that block renal glucose reabsorption via inhibition of sodium-dependent glucose cotransporter 2 (SGLT2) is a novel approach to diabetes management. In this study, twenty-seven aryl C-glycosides bearing a C=N/C-N linkage at the glucosyl C6 position were designed, synthesized and evaluated for their inhibitory activity against human SGLT2 (hSGLT2). Compounds with good hSGLT2 inhibition were further investigated to determine their selectivity over hSGLT1. Of these, five representative aryl C-glycosides were chosen for pharmacokinetic analysis...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29216395/a-randomized-trial-of-the-prophylactic-activity-of-dsm265-against-pre-erythrocytic-plasmodium-falciparum-controlled-human-malaria-infection-by-mosquito-bites-and-direct-venous-inoculation
#15
Sean C Murphy, Elizabeth R Duke, Kelly J Shipman, Ryan L Jensen, Youyi Fong, Sue Ferguson, Holly E Janes, Kevin Gillespie, Annette M Seilie, Amelia E Hanron, Laurie Rinn, Matthew Fishbaugher, Tracie VonGoedert, Emma Fritzen, Stefan H Kappe, Ming Chang, Jason C Sousa, Sean R Marcsisin, Stephan Chalon, Stephan Duparc, Nicola Kerr, Jörg J Möhrle, Nicole Andenmatten, Thomas Rueckle, James G Kublin
Background: DSM265 is a selective inhibitor of Plasmodium dihydroorotate dehydrogenase that fully protected against controlled human malarial infection (CHMI) by direct venous inoculation of Plasmodium falciparum sporozoites when administered one day pre-challenge and provided partial protection when administered seven days pre-challenge. Methods: A double-blind, randomized, placebo-controlled trial was performed to assess safety, tolerability, pharmacokinetics and efficacy of one oral dose of 400 mg DSM265 pre-CHMI...
December 5, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/29216348/mic-based-dose-adjustment-facts-and-fables
#16
Johan W Mouton, Anouk E Muller, Rafael Canton, Christian G Giske, Gunnar Kahlmeter, John Turnidge
Over recent decades, several publications have described optimization procedures for antibiotic therapy in the individual patient based on antimicrobial MIC values. Most methods include therapeutic drug monitoring and use a single MIC determination plus the relevant pharmacokinetics/pharmacodynamics to adjust the dose to optimize antimicrobial drug exposure and antibacterial effects. However, the use of an MIC obtained by a single MIC determination is inappropriate. First, routine clinical laboratories cannot determine MICs with sufficient accuracy to guide dosage owing to the inherent assay variation in the MIC test...
December 5, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29216273/isoniazid-concentrations-in-hair-and-plasma-area-under-the-curve-exposure-among-children-with-tuberculosis
#17
Vidya Mave, Aarti Kinikar, Anju Kagal, Smita Nimkar, Hari Koli, Sultanat Khwaja, Renu Bharadwaj, Roy Gerona, Anita Wen, Geetha Ramachandran, Hemanth Kumar, Peter Bacchetti, Kelly E Dooley, Nikhil Gupte, Amita Gupta, Monica Gandhi
We measured hair and plasma concentrations of isoniazid among sixteen children with tuberculosis who underwent personal or video-assisted directly observed therapy and thus had 100% adherence. This study therefore defined typical isoniazid exposure parameters after two months of treatment among fully-adherent patients in both hair and plasma (plasma area under the concentration-time curve, AUC, estimated using pharmacokinetic data collected 0, 2, 4, and 6 hours after drug administration). We found that INH levels in hair among highly-adherent individuals did not correlate well with plasma AUC or trough concentrations, suggesting that each measure may provide incremental and complementary information regarding drug exposure in the context of TB treatment...
2017: PloS One
https://www.readbyqxmd.com/read/29215627/a-pharmacokinetic-rationale-for-proactive-therapeutic-drug-monitoring-of-anti-tnf-drugs
#18
Andrew R Reinink
No abstract text is available yet for this article.
December 2017: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/29215597/application-of-pharmacokinetics-modelling-to-predict-human-exposure-of-a-cationic-liposomal-subunit-antigen-vaccine-system
#19
Raj K S Badhan, Swapnil Khadke, Yvonne Perrie
The pharmacokinetics of a liposomal subunit antigen vaccine system composed of the cationic lipid dimethyldioctadecylammonium bromide (DDA) and the immunostimulatory agent trehalose 6,6-dibehenate (TDB) (8:1 molar ratio) combined with the Ag85B-ESAT-6 (H1) antigen were modelled using mouse in-vivo data. Compartment modelling and physiologically based pharmacokinetics (PBPK) were used to predict the administration site (muscle) and target site (lymph) temporal concentration profiles and factors governing these...
December 7, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29215048/high-dose-parenteral-ascorbate-inhibited-pancreatic-cancer-growth-and-metastasis-mechanisms-and-a-phase-i-iia-study
#20
Kishore Polireddy, Ruochen Dong, Gregory Reed, Jun Yu, Ping Chen, Stephen Williamson, Pierre-Christian Violet, Ziyan Pessetto, Andrew K Godwin, Fang Fan, Mark Levine, Jeanne A Drisko, Qi Chen
Pancreatic cancer is among the most lethal cancers with poorly tolerated treatments. There is increasing interest in using high-dose intravenous ascorbate (IVC) in treating this disease partially because of its low toxicity. IVC bypasses bioavailability barriers of oral ingestion, provides pharmacological concentrations in tissues, and exhibits selective cytotoxic effects in cancer cells through peroxide formation. Here, we further revealed its anti-pancreatic cancer mechanisms and conducted a phase I/IIa study to investigate pharmacokinetic interaction between IVC and gemcitabine...
December 7, 2017: Scientific Reports
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