Radboud University Medical Center, Radboud Institute for Health Sciences, Department of Pharmacy, Nijmegen, the Netherlands; ZANOB Hospital Pharmacy, Jeroen Bosch Hospital, 's-Hertogenbosch, the Netherlands.
Department of Clinical Pharmacy and Toxicology, Maastricht University Medical Center, Maastricht, the Netherlands; CAPHRI-Care and Primary Health Research Institute, Maastricht University Medical Center, Maastricht, the Netherlands.
Lung Cancer. 2019 Apr;130:156-158. doi: 10.1016/j.lungcan.2019.01.018. Epub 2019 Feb 1.
Pemetrexed is indicated for non-small cell lung cancer and mesothelioma. Dosing is based on body surface are (BSA), while renal function is the only determinant for exposure and thus toxicity. BSA-based dosing introduces large variability in exposure and may lead to (hemato)toxicity in patients with impaired renal function. Therefore, pemetrexed is contraindicated in renal impairment. The presented cases provide proof-of-concept for pharmacokinetically-guided dosing of pemetrexed in a haemodialysis patient and a patient with mild renal impairment.
The pharmacokinetic target was an area under the concentration-time curve (AUC) of 123-205 mg·h/L. Using a previously developed population pharmacokinetic model, individual pharmacokinetics were estimated.
Both patients had an exposure above target after the initial dose, but a proportional dose reduction resulted in a therapeutic exposure in both patients (185 and 166 mg·h/L, respectively), that was well-tolerated. Interestingly, a threefold increase in systemic clearance of pemetrexed was observed during hemodialysis (from 1.00 L/h to 3.01 L/h), which approximates the population clearance of pemetrexed.
Altogether, we showed that pharmacokinetically-guided dosing of pemetrexed may be a feasible strategy for patients with lung cancer and renal impairment.
培美曲塞适用于非小细胞肺癌和间皮瘤。剂量基于体表面积 (BSA),而肾功能是决定暴露程度和因此产生毒性的唯一因素。BSA 为基础的剂量方案会导致暴露程度出现较大差异,可能导致肾功能受损的患者出现(血液)毒性。因此,培美曲塞禁用于肾功能损害患者。本案例提供了在血液透析患者和轻度肾功能损害患者中,基于药代动力学调整培美曲塞剂量的概念验证。
药代动力学目标是浓度-时间曲线下面积(AUC)为 123-205 mg·h/L。使用先前开发的群体药代动力学模型,估算个体药代动力学。
两名患者在初始剂量后均获得了高于目标的暴露量,但适当减少剂量后,两名患者均获得了治疗性暴露(分别为 185 和 166 mg·h/L),且耐受良好。有趣的是,在血液透析期间观察到培美曲塞的全身清除率增加了三倍(从 1.00 L/h 增加到 3.01 L/h),这与培美曲塞的人群清除率相近。
综上所述,我们表明,基于药代动力学的培美曲塞剂量调整可能是肾功能损害的肺癌患者的一种可行策略。