Department of Laboratory Medicine, University of Washington, Seattle, WA, 98195-7110, USA.
Am J Clin Pathol. 2010 Mar;133(3):454-7. doi: 10.1309/AJCPR23YAOYFSZTX.
Leflunomide (Arava), a drug with immunosuppressive and antiviral effects, is being used in renal transplant recipients, primarily for its action against BK polyomavirus (BKV), which affects 1% to 10% of renal transplant recipients and often causes failure of grafted kidneys. Leflunomide effects are solely due to an active metabolite, teriflunomide (formerly A77 1726). Trough blood concentrations of teriflunomide exceeding 40 microg/mL (148 micromol/L) are associated with progressive clearance of BKV. Toxic effects become increasingly apparent at higher concentrations. We have developed a rapid, simple, and robust high-performance liquid chromatography (HPLC) method for therapeutic monitoring of teriflunomide in renal transplant recipients. Sample preparation is rapid, and each HPLC separation takes about 7 minutes. Intraday and interday coefficients of variation were 1.5% or less and 5.6% or less, respectively. The method was linear to 200 microg/mL (740 micromol/L), which is well above teriflunomide concentrations that are likely to be observed.
来氟米特（Arava）是一种具有免疫抑制和抗病毒作用的药物，正在肾移植受者中使用，主要是因为其对 BK 多瘤病毒（BKV）的作用，BKV 影响 1%至 10%的肾移植受者，并且经常导致移植肾脏衰竭。来氟米特的作用完全归因于其活性代谢物特立氟胺（以前称为 A771726）。特立氟胺的血药浓度谷值超过 40μg/mL（148μmol/L）与 BKV 的逐渐清除有关。在更高的浓度下，毒性作用变得越来越明显。我们已经开发出一种快速、简单和强大的高效液相色谱（HPLC）方法，用于肾移植受者特立氟胺的治疗监测。样品制备快速，每个 HPLC 分离大约需要 7 分钟。日内和日间变异系数分别为 1.5%或更低和 5.6%或更低。该方法的线性范围为 200μg/mL（740μmol/L），远高于可能观察到的特立氟胺浓度。
