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Background <p>Everolimus (EVR) is widely used in kidney transplantation; however, the optimal sampling time point for therapeutic drug monitoring and the relationship between EVR exposure and adverse events under tacrolimus-based regimens remain unclear.</p> Methods <p>We retrospectively analyzed EVR pharmacokinetics in kidney transplant recipients receiving tacrolimus-based immunosuppressive therapy. EVR whole-blood concentrations at multiple post-dose time points were compared with the area under the concentration–time curve from 0 to 4 hours (AUC₀–₄). Associations between EVR exposure and adverse events, including proteinuria and de novo hyperlipidemia (HL), were explored using statistical models accounting for repeated pharmacokinetic measurements.</p> Results <p>EVR concentration at 2 hours post-dose (C2) showed the strongest correlation with AUC₀–₄ and was superior to trough concentration (C0) as a surrogate marker of short-term systemic exposure. Short-term EVR systemic exposure (AUC₀–₄) was not independently associated with de novo HL, whereas longer treatment duration was strongly associated with lipid abnormalities. No significant association was observed between EVR exposure and proteinuria.</p> Conclusions <p>C2 represents a practical surrogate marker for short-term EVR exposure in kidney transplant recipients receiving tacrolimus-based therapy. While EVR exposure itself was not independently associated with de novo HL, treatment duration appears to be an important factor, underscoring the need to consider long-term metabolic effects during EVR therapy.</p>

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Evaluation of everolimus pharmacokinetic monitoring based on trough concentration and area under the blood concentration time curve in kidney transplantation

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年1月19日

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  • Shota Fukae,
  • Yoichi Kakuta,
  • Soichi Matsumura,
  • Ryo Tanaka,
  • Masataka Kawamura,
  • Shigeaki Nakazawa,
  • Norio Nonomura

摘要

Background

Everolimus (EVR) is widely used in kidney transplantation; however, the optimal sampling time point for therapeutic drug monitoring and the relationship between EVR exposure and adverse events under tacrolimus-based regimens remain unclear.

Methods

We retrospectively analyzed EVR pharmacokinetics in kidney transplant recipients receiving tacrolimus-based immunosuppressive therapy. EVR whole-blood concentrations at multiple post-dose time points were compared with the area under the concentration–time curve from 0 to 4 hours (AUC₀–₄). Associations between EVR exposure and adverse events, including proteinuria and de novo hyperlipidemia (HL), were explored using statistical models accounting for repeated pharmacokinetic measurements.

Results

EVR concentration at 2 hours post-dose (C2) showed the strongest correlation with AUC₀–₄ and was superior to trough concentration (C0) as a surrogate marker of short-term systemic exposure. Short-term EVR systemic exposure (AUC₀–₄) was not independently associated with de novo HL, whereas longer treatment duration was strongly associated with lipid abnormalities. No significant association was observed between EVR exposure and proteinuria.

Conclusions

C2 represents a practical surrogate marker for short-term EVR exposure in kidney transplant recipients receiving tacrolimus-based therapy. While EVR exposure itself was not independently associated with de novo HL, treatment duration appears to be an important factor, underscoring the need to consider long-term metabolic effects during EVR therapy.