Overview of extended release tacrolimus in solid organ transplantation
Overview of extended release tacrolimus in solid organ transplantation作者机构：Department of Pharmacy Loyola Medical Center
出 版 物：《World Journal of Transplantation》 (世界移植杂志)
年 卷 期：2016年第6卷第1期
页 面：144-154页
学科分类：10[医学]
主 题：Tacrolimus Extended release tacrolimus Pharmacokinetics Pharmacoeconomics Solid-organ transplant
摘 要：Tacrolimus(Prograf?, Astellas Pharma Europe Ltd, Staines, United Kingdom; referred to as tacrolimusBID) is an immunosuppressive agent to prevent and treat allograft rejection in kidney transplant recipients in combination with mycophenolate mofetil, corticosteroids,with or without basiliximab induction. The drug has also been studied in liver, heart and lung transplant; however, these are currently off-label indications. An extended release tacrolimus formulation(Advagraf?, Astagraf XL?) allows for once-daily dosing, with the potential to improve adherence. Extended release tacrolimus has similar absorption, distribution, metabolism and excretion to tacrolimus-BID. Phase Ⅰ pharmacokinetic trials comparing extended release tacrolimus and tacrolimus-BID have demonstrated a decreased maximum concentration(C max) and delayed time to maximum concentration(t max) with the extended release formulation; however, AUC0-24 was comparable between formulations. Overall extended release tacrolimus has a very similar safety and efficacy profile to tacrolimus-BID. It is not recommended in the use of liver transplant patient s due to the increased risk of mortality in female recipients. There has been minimal data regarding the use of extended release tacrolimus in heart and lung transplant recipients. With the current data available for all organ groups the extended release tacrolimus should be dosed in a 1:1 fashion, the exception may be the cystic fibrosis population where their initial dose may need to be higher.
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