Results 1 to 10 of about 11,833 (101)

Personalized tacrolimus therapy in allogeneic hematopoietic stem cell transplantation: from pharmacokinetic variability to novel control strategies [PDF]

Journal of Pharmaceutical Health Care and Sciences
Background Allogeneic hematopoietic stem cell transplantation is an established curative therapy for many hematological diseases, but graft-versus-host disease remains a major cause of morbidity and mortality.
Naoki Yoshikawa
doaj   +2 more sources

Everolimus and sirolimus antagonize tacrolimus based calcineurin inhibition via competition for FK-binding protein 12 [PDF]

Biochemical Pharmacology, 2009
The calcineurin inhibitors cyclosporin A and tacrolimus and the inhibitors of the mTOR, sirolimus and everolimus bind immunophilins that are required for their immunosuppressive action. In contrast to cyclosporin A, tacrolimus and the mTOR inhibitors (MTIs) share common immunophilins, the FK506-binding proteins (FKBPs).
Fred P H T M Romijn, Johan W de Fijter, Johannes Van Pelt   +2 more
exaly   +4 more sources

Effect of Tacrolimus on Activity and Expression of P-Glycoprotein and ATP-Binding Cassette Transporter A5 (ABCA5) Proteins in Hematoencephalic Barrier Cells

Biological and Pharmaceutical Bulletin, 2008
Tacrolimus is an agent used in clinical immunosuppressive drug therapies. A wide spectrum of adverse effects has been reported in association with this immunosuppressor, including neurotoxic effect. The upper limit of therapeutic blood concentrations of tacrolimus has been described as 30 ng/ml in immunosuppressed patients.
Juan CARLOS Slebe, Juan G Carcamo
exaly   +4 more sources

Tacrolimus ameliorates podocyte injury by restoring FK506 binding protein 12 (FKBP12) at actin cytoskeleton [PDF]

The FASEB Journal, 2021
Abstract FKBP12 was identified as a binding protein of tacrolimus (Tac). Tac binds to FKBP12 and exhibits immunosuppressive effects in T cells. Although it is reported that Tac treatment directly ameliorates the dysfunction of the podocyte in nephrotic syndrome, the precise pharmacological mechanism of Tac is not well understood yet ...
Hidenori, Yasuda, Yoshiyasu, Fukusumi, Veniamin, Ivanov, Ying, Zhang, Hiroshi, Kawachi   +4 more
openaire   +2 more sources

Total and Free Blood and Plasma Concentration Changes in Pregnancy for Medicines Highly Bound to Plasma Proteins: Application of Physiologically Based Pharmacokinetic Modelling to Understand the Impact on Efficacy

Pharmaceutics, 2023
Free drug concentrations are generally considered the pharmacologically active moiety and are important for cellular diffusion and distribution. Pregnancy-related changes in plasma protein binding and blood partitioning are due to decreases in plasma ...
Paola Coppola, Andrew Butler, Susan Cole, Essam Kerwash   +3 more
doaj   +1 more source

A multi-omics investigation of tacrolimus off-target effects on a proximal tubule cell-line

Pharmacological Research, 2023
Introduction: Tacrolimus, an immunosuppressive drug prescribed to a majority of organ transplant recipients is nephrotoxic, through still unclear mechanisms.
Hassan Aouad, Quentin Faucher, François-Ludovic Sauvage, Emilie Pinault, Claire-Cécile Barrot, Hélène Arnion, Marie Essig, Pierre Marquet   +7 more
doaj   +1 more source

Assessing Trans-Inhibition of OATP1B1 and OATP1B3 by Calcineurin and/or PPIase Inhibitors and Global Identification of OATP1B1/3-Associated Proteins

Pharmaceutics, 2023
Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 are key determinants of drug–drug interactions (DDIs). Various drugs including the calcineurin inhibitor (CNI) cyclosporine A (CsA) exert preincubation-induced trans-inhibitory effects upon ...
John T. Powell, Ruhul Kayesh, Alexandra Ballesteros-Perez, Khondoker Alam, Pascaline Niyonshuti, Erik J. Soderblom, Kai Ding, Chao Xu, Wei Yue   +8 more
doaj   +1 more source

ABCB1 1199G>A genetic polymorphism (Rs2229109) influences the intracellular accumulation of tacrolimus in HEK293 and K562 recombinant cell lines. [PDF]

PLoS ONE, 2014
ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A.
Géraldine Dessilly, Laure Elens, Nadtha Panin, Arnaud Capron, Anabelle Decottignies, Jean-Baptiste Demoulin, Vincent Haufroid   +6 more
doaj   +1 more source

Renal Deletion of 12 kDa FK506-Binding Protein Attenuates Tacrolimus-Induced Hypertension [PDF]

Journal of the American Society of Nephrology, 2015
Tacrolimus is a widely used immunosuppressive drug that inhibits the phosphatase calcineurin when bound to the 12 kDa FK506-binding protein (FKBP12). When this binding occurs in T cells, it leads to immunosuppression. Tacrolimus also causes side effects, however, such as hypertension and hyperkalemia.
Rebecca A, Lazelle, Belinda H, McCully, Andrew S, Terker, Nina, Himmerkus, Katharina I, Blankenstein, Kerim, Mutig, Markus, Bleich, Sebastian, Bachmann, Chao-Ling, Yang, David H, Ellison   +9 more
openaire   +2 more sources

Characterization of the FKBP12-Encoding Genes in Aspergillus fumigatus. [PDF]

PLoS ONE, 2015
Invasive aspergillosis, largely caused by Aspergillus fumigatus, is responsible for a growing number of deaths among immunosuppressed patients. Immunosuppressants such as FK506 (tacrolimus) that target calcineurin have shown promise for antifungal drug ...
Katie Falloon, Praveen R Juvvadi, Amber D Richards, José M Vargas-Muñiz, Hilary Renshaw, William J Steinbach   +5 more
doaj   +1 more source