[HTML][HTML] Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation

UM Zanger, M Schwab - Pharmacology & therapeutics, 2013 - Elsevier
Cytochromes P450 (CYP) are a major source of variability in drug pharmacokinetics and
response. Of 57 putatively functional human CYPs only about a dozen enzymes, belonging …

Impact of Genetic Polymorphisms of ABCB1 (MDR1, P-Glycoprotein) on Drug Disposition and Potential Clinical Implications: Update of the Literature

S Wolking, E Schaeffeler, H Lerche, M Schwab… - Clinical …, 2015 - Springer
ATP-binding cassette transporter B1 (ABCB1; P-glycoprotein; multidrug resistance protein 1)
is an adenosine triphosphate (ATP)-dependent efflux transporter located in the plasma …

PharmGKB summary: cyclosporine and tacrolimus pathways

JM Barbarino, CE Staatz… - Pharmacogenetics …, 2013 - journals.lww.com
Tacrolimus (FK506) and cyclosporine (cyclosporin A, CsA) are cornerstone
immunosuppressive agents administered to solid organ transplant recipients to prevent and …

Pharmacokinetics, pharmacodynamics and pharmacogenetics of tacrolimus in kidney transplantation

M Yu, M Liu, W Zhang, Y Ming - Current drug metabolism, 2018 - ingentaconnect.com
Background: Tacrolimus (Tac, or FK506), a calcineurin inhibitor (CNI), is the first-line
immunosuppressant which consists of the footstone as immunosuppressive regimens in …

The role of pharmacogenetics in the disposition of and response to tacrolimus in solid organ transplantation

DA Hesselink, R Bouamar, L Elens… - Clinical …, 2014 - Springer
The calcineurin inhibitor tacrolimus is the backbone of immunosuppressive drug therapy
after solid organ transplantation. Tacrolimus is effective in preventing acute rejection but has …

Intra-patient variability in tacrolimus exposure: causes, consequences for clinical management

N Shuker, T van Gelder, DA Hesselink - Transplantation reviews, 2015 - Elsevier
Tacrolimus (Tac) is widely used for the prevention of rejection after solid organ
transplantation. Finding the optimal balance between effective Tac concentrations and …

CYP3A4*22: Promising Newly Identified CYP3A4 Variant Allele for Personalizing Pharmacotherapy

L Elens, T Van Gelder, DA Hesselink… - …, 2013 - Taylor & Francis
Many studies have attempted to explain the interindividual variability observed in drug
metabolism by assessing the impact of SNPs in genes implicated in drug absorption …

A New Functional CYP3A4 Intron 6 Polymorphism Significantly Affects Tacrolimus Pharmacokinetics in Kidney Transplant Recipients

L Elens, R Bouamar, DA Hesselink, V Haufroid… - Clinical …, 2011 - academic.oup.com
BACKGROUND Tacrolimus (Tac) is a potent immunosuppressant with considerable toxicity.
Tac pharmacokinetics varies between individuals and thus complicates its use in preventing …

[HTML][HTML] Pharmacokinetics and toxicity of tacrolimus early after heart and lung transplantation

MA Sikma, EM Van Maarseveen… - American Journal of …, 2015 - Elsevier
Annually, about 8000 heart and lung transplantations are successfully performed worldwide.
However, morbidity and mortality still pose a major concern. Renal failure in heart and lung …

Clinical determinants of calcineurin inhibitor disposition: a mechanistic review

T Vanhove, P Annaert, DRJ Kuypers - Drug metabolism reviews, 2016 - Taylor & Francis
The calcineurin inhibitors (CNIs) tacrolimus and cyclosporine are widely used
immunosuppressive drugs characterized by high pharmacokinetic and pharmacodynamic …