Institute of Hematology, Huazhong University of Science and Technology, Wuhan, China.
Acta Pharmacol Sin. 2010 Aug;31(8):999-1004. doi: 10.1038/aps.2010.79. Epub 2010 Jul 19.
To investigate the pharmacokinetics of imatinib in Chinese chronic myelogenous leukemia (CML) patients.
Fourty-six naïve Chinese CML patients treated with imatinib (400 and 600 mg daily, n=36 and 10, respectively) were recruited. The correlations of imatinib (400 mg) trough plasma concentrations (C(mins)) with the patients' characteristics and responses were analyzed.
The overall mean (+/-SD, CV%) steady-state C(mins) for imatinib at 400 mg (n=36) and 600 mg (n=10) daily was 1325.61 ng/mL (+/-583.53 ng/mL; 44%) and 1550.90 ng/mL (+/-462.63 ng/mL; 30%), respectively, and no statistically significant differences were found between them (P=0.267). At 400 mg daily, female patients had significantly higher C(mins) than the male patients (P=0.048), and molecular responses were not correlated with imatinib C(mins), but they were correlated with time elapsed before imatinib therapy.
The results suggest that Chinese CML patients have higher imatinib C(mins) than their Caucasian counterparts and that the optimal initial imatinib dose for them requires further investigation.
研究伊马替尼在中国慢性髓性白血病（CML）患者中的药代动力学。
招募了 46 名接受伊马替尼（400mg 和 600mg 每日，n=36 和 10）治疗的初治中国 CML 患者。分析了伊马替尼（400mg）谷浓度（C（min））与患者特征和反应的相关性。
每日 400mg（n=36）和 600mg（n=10）的伊马替尼的总体平均（+/-SD，CV%）稳态 C（min）分别为 1325.61ng/ml（+/-583.53ng/ml；44%）和 1550.90ng/ml（+/-462.63ng/ml；30%），两者之间无统计学差异（P=0.267）。每日 400mg 时，女性患者的 C（min）明显高于男性患者（P=0.048），分子反应与伊马替尼 C（min）无关，但与伊马替尼治疗前的时间有关。
结果表明，中国 CML 患者的伊马替尼 C（min）高于白种人，他们的最佳初始伊马替尼剂量需要进一步研究。
