减少移植受者服用药物的频次能够提高这些患者对于复杂免疫抑制药物方案的顺应性。他克莫司一天一次服药的缓释（XL）剂型发明后能够和一天两次的他克莫司（TAC）行1：1的转换，与谷浓度相关性的暴露良好。一项开放标签多中心的研究将69名平稳的肝移植患者一天两次的TAC转换为每天早晨一次的XL，维持至少2年，并采用和实用TAC时相同的治疗监测和患者看护技术。转换后2年，活检证实的急性排斥反应发生率为5.8％（69名患者中4名），患者和移植物存活率为98.6％（69名中有68名）。XL的安全性和先前报道的TAC保持一致。肝移植受者从一天两次的TAC转换为一天一次的XL并维持至少两年后没有特别的效果也不存在安全性问题。

Compliance with complex immunosuppressant drug therapies in transplant recipients might be improved with regimens that require less frequent dosing. A once-daily extended release (XL) formulation of tacrolimus has been developed that allows a 1:1 conversion from the twice-a-day tacrolimus (TAC) formulation and has a good exposure to trough concentration correlation. In an open-label, multicenter study, stable liver transplant recipients (n=69) were converted from twice-a-day TAC to XL once-daily in the morning, and were maintained for at least 2 years postconversion using the same therapeutic monitoring and patient care techniques employed with TAC. Two years after conversion, the incidence of biopsy-confirmed acute rejection was 5.8% (4 of 69); patient and graft survival was 98.6% (68 of 69). The safety profile of XL was consistent with that previously reported for TAC. Liver transplant recipients can be converted from twice-a-day TAC to once-daily XL and maintained for at least 2 years postconversion with neither unique efficacy nor safety concerns.

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