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 …

Measuring intracellular concentrations of calcineurin inhibitors: expert consensus from the international association of therapeutic drug monitoring and clinical …

F Lemaitre, NT Vethe, A d'Avolio, C Tron… - Therapeutic drug …, 2020 - journals.lww.com
Background: Therapeutic drug monitoring (TDM) of the 2 calcineurin inhibitors (CNIs),
tacrolimus (TAC) and cyclosporin A, has resulted in improvements in the management of …

Calcineurin inhibitors: pharmacologic mechanisms impacting both insulin resistance and insulin secretion leading to glucose dysregulation and diabetes mellitus

HA Chakkera, Y Kudva, B Kaplan - Clinical Pharmacology & …, 2017 - Wiley Online Library
Calcineurin inhibitors (CNIs), including tacrolimus and cyclosporine, are immune‐
modulating agents used in autoimmune disorders, glomerulonephritides, and after …

THE TEMPORAL PROFILE OF CALCINEURIN INHIBITION BY CYCLOSPORINE IN VIVO1

PF Halloran, LMH Helms, L Kung, J Noujaim - Transplantation, 1999 - journals.lww.com
Background. Cyclosporine (CsA) acts by inhibiting the phosphatase calcineurin (CN), but
the time course and extent of inhibition in vivo are unknown. We examined the effect of …

Whole-blood calcineurin activity is not predicted by cyclosporine blood concentration in renal transplant recipients

R Caruso, N Perico, D Cattaneo, G Piccinini… - Clinical …, 2001 - academic.oup.com
Background: In transplant patients, current cyclosporine (CsA) dose monitoring with classic
pharmacokinetics has demonstrated limitations. Evaluation of the activity of calcineurin (CN) …

Neurotoxicity of calcineurin inhibitors: impact and clinical management

WO Bechstein - Transplant International, 2000 - Wiley Online Library
Abstract Between 10%–28% of patients who receive the immuno‐suppressant cyclosporine
(CsA) experience some form of neurotoxic adverse event. Both sensorial motoric functions …

Are circulating metabolites important in drug–drug interactions?: quantitative analysis of risk prediction and inhibitory potency

CK Yeung, Y Fujioka, H Hachad… - Clinical …, 2011 - Wiley Online Library
The potential of metabolites to contribute to drug–drug interactions (DDIs) is not well
defined. The aim of this study was to determine the quantitative role of circulating …

Tacrolimus nephrotoxicity: beware of the association of diarrhea, drug interaction and pharmacogenetics

S Leroy, A Isapof, S Fargue, M Fakhoury… - Pediatric …, 2010 - Springer
Tacrolimus is known to potentially lead to adverse events in recipients with diarrhoea and/or
calcium channel blocker (CCB) co-administration. We report a renal transplant recipient who …

Urine metabolites reflect time-dependent effects of cyclosporine and sirolimus on rat kidney function

J Klawitter, J Bendrick-Peart, B Rudolph… - Chemical Research …, 2009 - ACS Publications
The clinical use of the immunosuppressant calcineurin inhibitor cyclosporine is limited by its
nephrotoxicity. This is enhanced when combined with the immunosuppressive mTOR …

Distinct inhibitory effects of tacrolimus and cyclosporin A on calcineurin phosphatase activity

M Fukudo, I Yano, S Masuda, M Okuda, K Inui - Journal of Pharmacology …, 2005 - ASPET
We have compared the pharmacodynamic properties of calcineurin inhibitors tacrolimus and
cyclosporin A in rats to clarify the different therapeutic drug monitoring strategy of both drugs …