胃肠间质瘤患者中Imatinib血药浓度与治疗疗效的相关性

Correlation of Imatinib plasma concentration and efficacy found in GIST patients

目的检测中国晚期胃肠间质瘤(GIST)患者中伊马替尼(Imatinib)血药浓度,并分析血药浓度与治疗疗效的相关性。方法收集112例接受Imatinib治疗超过28 d的GIST患者的117份血浆样本,用HPLC-MS/MS法检测血浆中Imatinib浓度。分析Imatinib血药浓度与治疗疗效的相关性。结果高剂量组(600 mg/d)患者的血药浓度较低剂量组(400 mg/d)明显升高(P<0.001)。服药时间为1～2年患者的血药浓度(平均值1 268 ng/mL)较服药时间小于1年的患者(平均值1 845 ng/mL)明显降低(P<0.05)。随着血药浓度的增加有效率也随之增加,血药浓度低、中及高水平组的有效率分别为50%、67.5%及66.7%。结论 Imatinib血药浓度与服药剂量及服药时间明显相关;Imatinib治疗有效率随着血药浓度的增高呈增加趋势。

Objective To detect the plasma concentration of Imatinib in Chinese gastrointestinal stromal tumor（GIST） patients,and to analyze the relationship between Imatinib plasma concentration and efficacy.Methods We collected 117 plasma samples from 112 GIST patients treated with Imatinib over 28 days.Plasma concentration of Imatinib was detected using high performance liquid chromatography-mass spectrometry（HPLC-MS/MS）.The correlation between Imatinib plasma concentration and efficacy was statistically analyzed.Results The plasma concentration of Imatinib in high dose（600 mg/d） patients was significantly higher than that in low dose（400 mg/d） patients（P0.001）.Plasma concentrations in patients treated with Imatinib 1～2 years were higher than that in patients treated less than 1 year（P=0.028）.The efficacy increased along with the increase of plasma concentration of Imatinib,although it was not significant（P=0.546）： the efficacy in low plasma concentration,middle plasma concentration and high plasma concentration was 50%,67.5% and 66.7%,respectively.Conclusion There was significant correlation between Imatinib plasma concentration and drug dose or time of drug administration;the efficacy of Imatinib increased along with the increase of plasma concentration.