Department of Pharmaceutical Services, Ronald Reagan UCLA Medical Center, Los Angeles, CA.
Division of Nephrology, Department of Medicine, David Geffen School of Medicine at UCLA, Los Angeles, CA, USA.
Expert Opin Drug Metab Toxicol. 2021 Oct;17(10):1175-1186. doi: 10.1080/17425255.2021.1974399. Epub 2021 Sep 22.
One of the most commonly used immunosuppressants in organ transplant, tacrolimus exhibits wide interpatient and intrapatient variability and narrow therapeutic index that necessitates routine concentration monitoring and dosage adjustments. Availability of modified -release tacrolimus products offer once-daily dosing options. The objective of this review is to highlight and compare available pharmacokinetic (PK) data of extended-release tacrolimus tablets (LCP-TAC) to immediate-release tacrolimus (IR-TAC) in kidney transplant recipients.
A review of the literature was performed using PubMed and Embase search to identify relevant articles evaluating PK data for LCP-TAC compared to IR-TAC in kidney transplant patients including special populations.
LCP-TAC's unique PK profile may be more favorable than IR-TAC. While the clinical impact of these PK differences have not been established, several outcomes are being evaluated in ongoing studies. Results of these studies will add information incrementally to care for kidney transplant patients. Larger prospective studies evaluating kidney and patient survival differences are needed but it is unlikely that they will be conducted. Given that the patent exclusivity of LCP-TAC for the next several years and imminent loss of exclusivity of PR-TAC, our opinion is the use of LCP-TAC will be increasing, especially in Europe.
他克莫司是器官移植中最常用的免疫抑制剂之一，具有广泛的个体间和个体内变异性以及狭窄的治疗指数，这需要常规进行浓度监测和剂量调整。改良释放他克莫司产品的可用性提供了每日一次的给药选择。本综述的目的是强调并比较在肾移植受者中，延长释放他克莫司片（LCP-TAC）与即时释放他克莫司（IR-TAC）的现有药代动力学（PK）数据。
使用 PubMed 和 Embase 搜索进行文献复习，以确定评估 LCP-TAC 与肾移植患者中 IR-TAC 的 PK 数据的相关文章，包括特殊人群。
LCP-TAC 的独特 PK 特征可能比 IR-TAC 更有利。虽然这些 PK 差异的临床影响尚未确定，但正在进行的研究正在评估几个结局。这些研究的结果将逐步为肾移植患者的护理提供信息。需要进行更大规模的前瞻性研究来评估肾和患者生存差异，但不太可能进行这些研究。鉴于 LCP-TAC 在未来几年的专利独占性以及 PR-TAC 的独占性即将丧失，我们的观点是，LCP-TAC 的使用将会增加，特别是在欧洲。
