Lehmkuhl H, Ross H, Eisen H, Valantine H
Deutsches Herzzentrum Berlin, Berlin, Germany.
Transplant Proc. 2005 Dec;37(10):4145-9. doi: 10.1016/j.transproceed.2005.10.005.
The proliferation signal inhibitor everolimus is efficacious for reducing the incidence of acute rejection and cardiac allograft vasculopathy (CAV) in heart transplantation; and it has the potential to facilitate cyclosporine (CsA) minimization in this setting. Reducing CsA dose in heart transplantation is dependent on everolimus trough blood levels of 3 to 8 ng/mL being achieved. Physicians experienced in the use of everolimus aim for CsA trough blood levels of 175 to 200 ng/mL in everolimus-treated patients during the initial 3 months following heart transplantation. Modeling data from the heart pivotal study suggest that CsA trough blood levels of 100 ng/mL at 6 months posttransplant could be targeted without loss of efficacy, and antibody induction therapy may assist with this approach. Target CsA trough blood levels for maintenance patients could possibly be reduced from the current 80 to 100 ng/mL to 50 to 80 ng/mL. Maintenance patients with renal dysfunction or CAV may benefit from conversion to everolimus and subsequent reduction in CsA trough blood levels (eg, by 50%). Initial experience of everolimus with reduced CsA trough blood levels in heart transplantation is favorable, but there is scope for further study.
增殖信号抑制剂依维莫司在心脏移植中对于降低急性排斥反应的发生率及心脏移植血管病变（CAV）有效；并且在这种情况下它有促进环孢素（CsA）减量的潜力。在心脏移植中降低CsA剂量取决于依维莫司血药谷浓度达到3至8 ng/mL。有依维莫司使用经验的医生在心脏移植后的最初3个月内，对于接受依维莫司治疗的患者，目标是使CsA血药谷浓度达到175至200 ng/mL。来自心脏关键研究的建模数据表明，移植后6个月时CsA血药谷浓度为100 ng/mL可作为目标且不损失疗效，抗体诱导治疗可能有助于这种方法。维持治疗患者的目标CsA血药谷浓度可能从目前的80至100 ng/mL降至50至80 ng/mL。肾功能不全或患有CAV的维持治疗患者可能会从转换为依维莫司并随后降低CsA血药谷浓度（如降低50%）中获益。依维莫司在心脏移植中降低CsA血药谷浓度的初步经验是良好的，但仍有进一步研究的空间。
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