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Tacrolimus pharmacokinetics

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https://www.readbyqxmd.com/read/29135993/bioequivalence-between-innovator-and-generic-tacrolimus-in-liver-and-kidney-transplant-recipients-a-randomized-crossover-clinical-trial
#1
Rita R Alloway, Alexander A Vinks, Tsuyoshi Fukuda, Tomoyuki Mizuno, Eileen C King, Yuanshu Zou, Wenlei Jiang, E Steve Woodle, Simon Tremblay, Jelena Klawitter, Jost Klawitter, Uwe Christians
BACKGROUND: Although the generic drug approval process has a long-term successful track record, concerns remain for approval of narrow therapeutic index generic immunosuppressants, such as tacrolimus, in transplant recipients. Several professional transplant societies and publications have generated skepticism of the generic approval process. Three major areas of concern are that the pharmacokinetic properties of generic products and the innovator (that is, "brand") product in healthy volunteers may not reflect those in transplant recipients, bioequivalence between generic and innovator may not ensure bioequivalence between generics, and high-risk patients may have specific bioequivalence concerns...
November 2017: PLoS Medicine
https://www.readbyqxmd.com/read/29123208/differential-t-cell-signaling-pathway-activation-by-tacrolimus-and-belatacept-after-kidney-transplantation-post-hoc-analysis-of-a-randomised-controlled-trial
#2
Nynke M Kannegieter, Dennis A Hesselink, Marjolein Dieterich, Gretchen N de Graav, Rens Kraaijeveld, Carla C Baan
Pharmacokinetic immunosuppressive drug monitoring poorly correlates with clinical outcomes after solid organ transplantation. A promising method for pharmacodynamic monitoring of tacrolimus (TAC) in T cell subsets of transplant recipients might be the measurement of (phosphorylated) p38MAPK, ERK1/2 and Akt (activated downstream of the T cell receptor) by phospho-specific flow cytometry. Here, blood samples from n = 40 kidney transplant recipients (treated with either TAC-based or belatacept (BELA)-based immunosuppressive drug therapy) were monitored before and throughout the first year after transplantation...
November 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29110351/posaconazole-liquid-vs-tablet-formulation-in-lung-transplant-recipients
#3
D Telzer, A Weber, F Ihle, S Matthes, F Ceelen, G Zimmermann, N Kneidinger, R Schramm, H Winter, M Zoller, M Vogeser, J Behr, C Neurohr
BACKGROUND: Posaconazole is an extended-spectrum triazole antifungal used in the treatment and prophylaxis of Aspergillus infections. It is available as oral suspension (POS-Liq) and delayed-release tablets (POS-Tab). OBJECTIVES: The aim of this longitudinal, retrospective study was to compare the clinical effectiveness, toxicity, and pharmacokinetics of POS-Liq vs. POS-Tab in lung transplant recipients (LTx-recipients), who were treated with both formulations subsequently...
November 6, 2017: Mycoses
https://www.readbyqxmd.com/read/29095105/genotype-based-tacrolimus-dosing-guidelines-with-or-without-cyp3a4-22
#4
Laure Elens, Vincent Haufroid
AIM: To test the relevance of revisiting the genotype classification based on CYP3A5*3 solely by incorporating CYP3A4*22 information. METHODS: Discriminant analysis of principal component was performed to evaluate the relevance of either the CYP3A (CYP3A5 + CYP3A4 genotypes) or CYP3A5*3 classification variables. This analysis was based on a linear combination of noncompartmental pharmacokinetics parameters. RESULTS: Discriminant analysis of principal component gave better results with CYP3A compared with CYP3A5*3 clustering...
November 2, 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/29050276/a-new-donors-cyp3a5-and-recipients-cyp3a4-cluster-predicting-tacrolimus-disposition-and-new-onset-hypertension-in-chinese-liver-transplant-patients
#5
Yuan Liu, Tao Zhang, Xiaoqing Zhang, Ling Ye, Haitao Gu, Lin Zhong, Hongcheng Sun, Chenlong Song, Zhihai Peng, Junwei Fan
AIM: The purpose of the current study was to investigate individualized therapy of tacrolimus (Tac), as well as complications after liver transplantation (LT) with the known genetic determinants and clinical factors. METHODS: In this retrospective study, two cohorts (n=170) from the China Liver Transplant Registry (CLTR) database from July 2007 to March 2015 were included. RESULTS: Both donors' CYP3A5*3 and recipients' CYP3A4*1G had a correlation with Tac pharmacokinetics at four weeks (all P<0...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29045960/pharmacokinetics-of-once-daily-prolonged-release-formulation-of-tacrolimus-in-children-with-primary-nephrotic-syndrome
#6
Y Han, S Q DU, H J Xiao, Y Zhou, J Ding, J J Ding, Y M Cui
OBJECTIVE: Tacrolimus prolonged-release(PR) formulation is a new once-daily formulation of the calcineurin inhibitor tacrolimus, which is currently used in adult liver or kidney transplant patients,and is also gradually widely used in children with nephrotic syndrome.The present study was undertaken to preliminarily investigate the pharmacokinetic characteristics of tacrolimus PR in pediatric nephrotic syndrome recipients. METHODS: This single-center open-label prospective study was performed in pediatric nephrotic syndrome recipients...
October 18, 2017: Beijing da Xue Xue Bao. Yi Xue Ban, Journal of Peking University. Health Sciences
https://www.readbyqxmd.com/read/29033547/new-tablet-formulation-of-tacrolimus-with-smaller-interindividual-variability-may-become-a-better-treatment-option-than-the-conventional-capsule-formulation-in-organ-transplant-patients
#7
Yu Kyong Kim, Anhye Kim, Shin Jung Park, Howard Lee
To evaluate the pharmacokinetic (PK) and tolerability profiles of a new tablet formulation of tacrolimus and its interindividual variability (IIV) in the systemic exposure, and to compare them with those of the conventional capsule formulation, a randomized, open-label, two-treatment, two-period, two-sequence, crossover study was performed in 47 healthy males. The capsule or tablet formulation of tacrolimus was orally administered, and serial blood samples were collected up to 96 hours after dosing. Whole-blood tacrolimus concentration was determined using liquid chromatography-tandem mass spectrometry...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28976570/renal-transplant-acute-rejection-with-lower-mycophenolate-mofetil-dosing-and-proton-pump-inhibitors-or-histamine-2-receptor-antagonists
#8
Kajal S Patel, Brian R Stephany, Julie F Barnes, Seth R Bauer, Michael L Spinner
BACKGROUND: Pharmacokinetic data show reduced mycophenolic acid levels in renal transplant recipients taking mycophenolate mofetil (MMF) and proton pump inhibitors (PPIs) concomitantly. This reduced exposure could increase rejection risk. The typical initial MMF dose post-renal transplant is 2 g daily, which often requires dose reduction secondary to side effects. Existing studies have not shown significant acute rejection differences for patients taking MMF-PPI versus MMF-ranitidine...
October 4, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28967706/pharmacokinetics-and-safety-of-letermovir-coadministered-with-cyclosporine-a-or-tacrolimus-in-healthy-subjects
#9
Dirk Kropeit, Oliver von Richter, Hans-Peter Stobernack, Helga Rübsamen-Schaeff, Holger Zimmermann
Letermovir is being developed for human cytomegalovirus infection treatment and prophylaxis. In patients receiving transplants, antivirals are coadministered with cyclosporine A (CsA) or tacrolimus (TAC) immunosuppressants. Therefore, we investigated the potential for letermovir-immunosuppressant interactions. In 2 phase 1 clinical trials either CsA 50 mg or TAC 5 mg was administered to healthy males. Following washout, letermovir 80 mg was dosed twice daily for 7 and 11 days in the CsA and TAC trials, respectively, with a second dose of immunosuppressant coadministered with letermovir at steady state...
October 2, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28947731/pharmacokinetic-interaction-between-tacrolimus-and-fentanyl-in-patients-receiving-allogeneic-hematopoietic-stem-cell-transplantation
#10
Fumiaki Kitazawa, Shin-Ichi Fuchida, Yoko Kado, Kumi Ueda, Takatoshi Kokufu, Akira Okano, Mayumi Hatsuse, Satoshi Murakami, Yuko Nakayama, Kohji Takara, Chihiro Shimazaki
BACKGROUND Tacrolimus and fentanyl are well-known cytochrome P450 (CYP) 3A4 substrates with a narrow therapeutic range. However, the pharmacokinetic interaction between tacrolimus and fentanyl is unclear. The aim of this study was to determine whether drug interaction exists between tacrolimus and fentanyl. MATERIAL AND METHODS A retrospective study was performed in 6 patients who had received allogeneic hematopoietic stem cell transplantation between April 2010 and March 2015. The patients received continuous intravenous infusion of fentanyl with concomitant use of tacrolimus, and the blood concentrations of tacrolimus were evaluated using fluorescence polarization immunoassay...
September 26, 2017: Annals of Transplantation: Quarterly of the Polish Transplantation Society
https://www.readbyqxmd.com/read/28945481/long-term-influence-of-cyp3a5-cyp3a4-abcb1-and-nr1i2-polymorphisms-on-tacrolimus-concentration-in-chinese-renal-transplant-recipients
#11
Fei Liu, Yang-Meng Ou, Ai-Rong Yu, Lei Xiong, Hua-Wen Xin
BACKGROUND: The highly pharmacokinetic variability of tacrolimus makes it difficult to adjust the dose. In the current study, we investigated the influence of gene polymorphisms and other clinical factors on long-term tacrolimus dosing in Chinese renal transplant recipients. METHODS: A total of 276 renal transplant recipients were enrolled. The tacrolimus trough concentration and other clinical variables were recorded for 5 years following transplantation. Eight single nucleotide polymorphisms in four genes (CYP3A5, CYP3A4, ABCB1, and NR1I2) were genotyped using polymerase chain reaction-restriction fragment length polymorphism analysis and sequencing...
September 25, 2017: Genetic Testing and Molecular Biomarkers
https://www.readbyqxmd.com/read/28945011/prediction-of-drug-drug-interaction-between-tacrolimus-and-principal-ingredients-of-wuzhi-capsule-in-chinese-healthy-volunteers-using-physiologically-based-pharmacokinetic-modelling
#12
Hongyan Zhang, Fengjiao Bu, Lei Li, Zheng Jiao, Guo Ma, Weimin Cai, Xiaomei Zhuang, Hai-Shu Lin, Jae-Gook Shin, Xiaoqiang Xiang
Schisantherin A and schisandrin A, the most abundant active ingredients of Wuzhi capsule, are known to inhibit tacrolimus metabolism by inhibiting CYP3A4/5. We aimed to predict the contribution of schisantherin A and schisandrin A to drug-drug interaction (DDI) between Wuzhi capsule and tacrolimus using physiologically-based pharmacokinetic (PBPK) modelling. Firstly, the inhibition mechanism of schisantherin A and schisandrin A on CYP3A4/5 were investigated. Thereafter, PBPK models of schisantherin A, schisandrin A and tacrolimus were established...
September 25, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28856745/using-known-drug-interactions-to-manage-supratherapeutic-calcineurin-inhibitor-concentrations
#13
REVIEW
Nicholas W Lange, David M Salerno, Karen Berger, Demetra S Tsapepas
OBJECTIVES: To summarize the available body of evidence guiding the management of supratherapeutic concentrations of calcineurin inhibitors (CNI) using cytochrome P450 (CYP450) enzyme inducers. METHODS: A nondate restricted literature search within MEDLINE, Embase, and Scopus was performed using the terms "cyclosporine," "tacrolimus," "calcineurin inhibitor," "toxicity," "pharmacokinetics," "carbamazepine," "rifampin," "phenytoin," and "phenobarbital." Additional references were identified from a review of all included citations...
August 30, 2017: Clinical Transplantation
https://www.readbyqxmd.com/read/28833329/population-pharmacokinetics-and-bayesian-estimation-of-tacrolimus-exposure-in-chinese-liver-transplant-patients
#14
B Chen, H-Q Shi, X-X Liu, W-X Zhang, J-Q Lu, B-M Xu, H Chen
WHAT IS KNOWN AND OBJECTIVES: Tacrolimus (TAC) is widely used as part of immunosuppressive regimens. There is great interindividual variation on the disposition of TAC. The aim of this study was to develop a population pharmacokinetic (PPK) model for Chinese liver transplant patients and evaluate genetic polymorphism and other possible factors on the PK parameters. The exposure of TAC is to be estimated through Bayesian modelling. METHODS: A total of 47 sets of rich-time PK and 1234 conventional therapeutic drug monitoring (TDM) data were collected from 125 Chinese liver transplant patients...
August 17, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28782485/a-low-concentration-of-tacrolimus-semifluorinated-alkane-sfa-eyedrop-suppresses-intraocular-inflammation-in-experimental-models-of-uveitis
#15
S De Majumdar, M Subinya, J Korward, A Pettigrew, D Scherer, H Xu
PURPOSE: Corticosteroids remain the mainstay therapy for uveitis, a major cause of blindness in the working age population. However, a substantial number of patients cannot benefit from the therapy due to steroids resistance or intolerance. Tacrolimus has been used to treat refractory uveitis through systemic administration. The aim of this study was to evaluate the therapeutic potential of 0.03% tacrolimus eyedrop in mouse models of uveitis. METHODS: 0.03% tacrolimus in perfluorobutylpentane (F4H5) (0...
2017: Current Molecular Medicine
https://www.readbyqxmd.com/read/28777242/analysis-of-common-polymorphisms-within-nr1i2-and-nr1i3-genes-and-tacrolimus-dose-adjusted-concentration-in-stable-kidney-transplant-recipients
#16
Mateusz Kurzawski, Damian Malinowski, Krzysztof Dziewanowski, Marek Droździk
OBJECTIVES: Several genetic factors were identified to be responsible for interidividual variability in tacrolimus (TAC) pharmacokinetics, with the predominant role of CYP3A5 and CYP3A4 polymorphisms. In this study, genetic variants of NR1I2 and NR1I3 nuclear receptors (responsible for the regulation of drug-metabolizing enzymes and transporters at the transcriptional level) were evaluated for their potential association with altered TAC concentrations. MATERIALS AND METHODS: Two hundred and forty White kidney transplant patients were genotyped for five single-nucleotide polymorphisms (rs3814055, rs6785049, rs2276707, rs2307424, and rs2307418) in NR1I2 and NR1I3 genes...
October 2017: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28736028/association-between-tacrolimus-pharmacokinetics-and-cytochrome-p450-3a5-and-multidrug-resistance-protein-1-exon-21-polymorphisms
#17
M Soda, M Fujitani, R Michiuchi, A Shibayama, K Kanamori, S Yoshikuni, Y Ohno, T Tsuchiya, A Suzuki, K Horie, T Deguchi, Y Itoh, K Kitaichi
BACKGROUND: Individual differences in the pharmacokinetics (PK) of tacrolimus (TAC), an immunosuppressive drug, are reportedly associated with single-nucleotide polymorphisms (SNPs) of cytochrome P450 (CYP) 3A5 and multidrug resistance protein 1 (MDR1). We determined the effect of SNPs in CYP3A5 and MDR1 exons 21 and 26 on TAC PK parameters. METHODS: Thirty-eight Japanese patients who underwent renal transplantation were genotyped for CYP3A5 and exons 21 and 26 of MDR1 with the use of polymerase chain reaction-restriction fragment length polymorphism analysis...
July 2017: Transplantation Proceedings
https://www.readbyqxmd.com/read/28717926/clinical-evaluation-of-modified-release-and-immediate-release-tacrolimus-formulations
#18
Simon Tremblay, Rita R Alloway
The science of drug delivery has evolved considerably and has led to the development of multiple sustained release formulations. Each of these formulations can present particular challenges in terms of clinical evaluation and necessitate careful study to identify their optimal use in practice. Tacrolimus is an immunosuppressive agent that is widely used in organ transplant recipients. However, it is poorly soluble, has an unpredictable pharmacokinetic profile subject to important genetic polymorphisms and drug-drug interactions, and has a narrow therapeutic index...
July 17, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28704257/the-combination-of-cyp3a4-22-and-cyp3a5-3-single-nucleotide-polymorphisms-determines-tacrolimus-dose-requirement-after-kidney-transplantation
#19
Nuria Lloberas, Laure Elens, Ines Llaudó, Ariadna Padullés, Teun van Gelder, Dennis A Hesselink, Helena Colom, Franc Andreu, Joan Torras, Oriol Bestard, Josep M Cruzado, Salvador Gil-Vernet, Ron van Schaik, Josep M Grinyó
INTRODUCTION: Tacrolimus (Tac) has a narrow therapeutic window and shows large between-patient pharmacokinetic variability. As a result, over-immunosuppression and under-immunosuppression are frequently encountered in daily clinical practice. Unraveling the impact of genetic polymorphisms on Tac pharmacokinetics may help to refine therapy. In this study, the associations of single-nucleotide polymorphisms (SNPs) in drug-metabolizing enzymes (CYP3A) with Tac pharmacokinetics were investigated in renal transplant recipients...
September 2017: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28686294/nfat-regulated-cytokine-gene-expression-during-tacrolimus-therapy-early-after-renal-transplantation
#20
Sara Bremer, Nils T Vethe, Morten Skauby, Margrete Kasbo, Elisabet D Johansson, Karsten Midtvedt, Stein Bergan
AIMS: Despite pharmacokinetic monitoring of calcineurin inhibitors, the long-term outcome after transplantation (Tx) is still hampered by the side effects of these drugs. The aim of the present study was to characterize nuclear factor of activated T cells (NFAT)-regulated gene expression as a potential pharmacodynamic biomarker for further individualization of tacrolimus (Tac) therapy. METHODS: In 29 renal allograft recipients, samples were drawn once pre-Tx, and before and 1...
November 2017: British Journal of Clinical Pharmacology
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