Renal function, efficacy and safety postconversion from twice- to once-daily tacrolimus in stable liver recipients: an open-label multicenter study

Sańko-Resmer, Joanna; Boillot, Olivier; Wolf, Philippe; Thorburn, Douglas

doi:10.1111/j.1432-2277.2011.01412.x

Cited by 42 publications

(45 citation statements)

References 19 publications

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“…Three studies reported that within-subject variability [percentage coefficient of variation (% CV)] in AUC 0-24 or C min decreased significantly following conversion from Prograf Ò to Advagraf Ò [28,35,43], while two studies could find no significant difference [31,45]. Conversion from Prograf Ò to Advagraf Ò resulted in a significant reduction in within-subject variability in tacrolimus AUC 0-24 from 14.1 to 10.9 % (but no reduction in C min ) in a study involving 40 stable kidney transplant recipients, assessed using five AUC values for each dosing regimen [28], and a reduction in tacrolimus C min from 14.0 to 8.5 % in a study involving 129 stable kidney transplant recipients [35].…”

Section: Xrmentioning

confidence: 97%

Clinical Pharmacokinetics of Once-Daily Tacrolimus in Solid-Organ Transplant Patients

Staatz

Tett

2015

Clin Pharmacokinet

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Tacrolimus is a pivotal immunosuppressant agent used in solid-organ transplantation. It was originally formulated for oral administration as Prograf(®), a twice-daily immediate-release capsule. In an attempt to improve patient adherence, retain manufacturer market share and/or reduce health care costs, newer once-daily prolonged-release formulations of tacrolimus (Advagraf(®) and Envarsus(®) XR) and various generic versions of Prograf(®) are becoming available. Tacrolimus has a narrow therapeutic index. Small variations in drug exposure due to formulation differences can have a significant impact on patient outcomes. The aim of this review is to critically analyse the published data on the clinical pharmacokinetics of once-daily tacrolimus in solid-organ transplant patients. Forty-three traditional (non-compartmental) and five population pharmacokinetic studies were identified and evaluated. On the basis of the stricter criteria for narrow-therapeutic-index drugs, Prograf(®), Advagraf(®) and Envarsus(®) XR are not bioequivalent [in terms of the area under the concentration-time curve from 0 to 24 h (AUC0-24) or the minimum concentration (C min)]. Patients may require a daily dosage increase if converted from Prograf(®) to Advagraf(®), while a daily dosage reduction appears necessary for conversion from Prograf(®) to Envarsus(®) XR. Prograf(®) itself, or generic immediate-release tacrolimus, can be administered in a once-daily regimen with a lower than double daily dose being reported to give 24-h exposure equivalent to that of a twice-daily regimen. Intense clinical and concentration monitoring is prudent in the first few months after any conversion to once-daily tacrolimus dosing; however, there is no guarantee that therapeutic drug monitoring strategies applicable to one formulation (or twice-daily dosing) will be equally applicable to another. The correlation between the tacrolimus AUC0-24 and C min is variable and not strong for all three formulations, indicating that trough measurements may not always give a good indication of overall drug exposure. Further investigation is required into whether the prolonged-release formulations have reduced within-subject pharmacokinetic variability, which would be a distinct advantage. Whether the effects of factors that influence tacrolimus absorption and pre-systemic metabolism (patient genotype status; gastrointestinal disease and disorders) and drug interactions differ across the formulations needs to be further elucidated. Most pharmacokinetic comparison studies to date have involved relatively stable patients, and many have been sponsored by the pharmaceutical companies manufacturing the new formulations. Larger randomized, controlled trials are needed in different transplant populations to determine whether there are differences in efficacy and toxicity across the formulations and whether formulation conversion is worthwhile in the longer term. While it has been suggested that once-daily administration of tacrolimus may improve patient compliance, further studies a...

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Section: Xrmentioning

confidence: 97%

Clinical Pharmacokinetics of Once-Daily Tacrolimus in Solid-Organ Transplant Patients

Staatz

Tett

2015

Clin Pharmacokinet

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“…The lower peak levels and reduced interpatient and intrapatient variability is observed with extended release tacrolimus after conversion from regular release tacrolimus in stable liver transplant recipients [10,11]. However, there still exists a significant intrapatient and interpatient variability in peak levels and area under curve (AUC) in de-novo transplant patients necessitating the need for frequent blood drug level monitoring [12].…”

Section: Pharmakokineticsmentioning

confidence: 99%

Extended release once a day tacrolimus

Singh

Visger

Zachariah

2015

Current Opinion in Organ Transplantation

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“…[2][3][4][5] These studies demonstrated that pharmacokinetics of twicedaily tacrolimus and the 2 formulations of once-daily tacrolimus are significantly different. Because no such data are available to date, the aim of the present study was to analyze the impact of conversion in daily practice from PR-Tac to ER-Tac among a large cohort of stable LT recipients, especially with regard to pharmacokinetics, safety, and cost.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Altieri¹,

Delaval²,

Kimmoun³

et al. 2018

Exp Clin Transplant

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Objectives: After organ transplant, strategies to simplify the therapeutic regimen may improve adherence and prevent rejection and/or graft loss. The aim of the present study was to evaluate the safety of conversion from once-daily prolonged-release tacrolimus (Advagraf; Astellas Pharma Europe Limited, Middlesex, UK) to once-daily extended-release tacrolimus (Envarsus; Chiesi SAS, Nanterre, France) in stable adult liver transplant recipients. Materials and Methods: This observational study included 44 liver transplant patients (median age of 59 y; 63.6% men; median delay after transplant of 72.5 mo). Conversion was based on a 1:0.70 proportion. Results: Mean dose of tacrolimus was 2.65 ± 1.24 mg/day before conversion and 2.09 ± 1.68 mg/day after conversion (P < .05), with ratio of 1:0.79. Mean serum tacrolimus trough level increased after conversion (4.92 ± 1.65 vs 5.60 ± 2.89 ng/mL; P < .05), with ratio of 1:1.14. Six months after conversion, mean dose of tacrolimus was 1.65 ± 0.93 mg/day (ratio of 1:0.62) and mean serum tacrolimus trough level was 4.82 ± 1.85 ng/mL, similar to the initial level before conversion. At the end of follow-up, 2 patients had returned to once-daily prolonged-release tacrolimus because of adverse effects (allergy, digestive trouble), which resolved thereafter. The mean cost of tacrolimus therapy was 5.54 ± 2.29 Euros/patient/day before conversion and 4.11 ± 2.32 Euros/patient/day after conversion (P < .05). Conclusions:Conversion from prolonged-release to extended-release tacrolimus in stable liver transplant patients is safe and cost-effective; however, initially, dose adaptations and careful monitoring are required.

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Renal function, efficacy and safety postconversion from twice- to once-daily tacrolimus in stable liver recipients: an open-label multicenter study

Cited by 42 publications

References 19 publications

Clinical Pharmacokinetics of Once-Daily Tacrolimus in Solid-Organ Transplant Patients

Clinical Pharmacokinetics of Once-Daily Tacrolimus in Solid-Organ Transplant Patients

Extended release once a day tacrolimus

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