胃肠道间质瘤患者伊马替尼血药浓度的监测及意义

Monitoring and Significance of Imatinib Plasma Concentration in Patients with Gastrointestinal Stromal Tumor

胃肠间质瘤(GIST)是消化道常见的间叶源性肿瘤,多发生于胃部,其免疫组化CD117及DOG-1常表达阳性,介导Kit基因突变是导致该病的主要机制。伊马替尼是一种酪氨酸酶抑制剂,可以很好的抑制c-Kit的活性,作为复发、不可切除或者晚期的GIGT患者一线用药甲磺酸伊马替尼,它已被证实是治疗中晚期GIST患者最有效的药物,可以显著改善预后。在常规的治疗过程中,伊马替尼的血药浓度在不同的GIST患者中存在很大差异,既有血药浓度不足导致疗效较差,也有血药浓度过高导致不良反应太大,血药浓度的监测对于提高患者的依从性及预后具有重要的意义。同时我们也可以通过马替尼血药浓度的检测去探究疾病的原因,然而对于甲磺酸伊马替尼血药浓度的监测主要集中在国外,国内相关研究甚少。本文从伊马替尼的药代动力学、伊马替尼血药浓度的现状及问题、监测的意义等方面进行综述,探讨伊马替尼血药浓度的监测对GIST患者的意义。

Gastrointestinal stromal tumor (GIST) is a common mesenchymal tumor of the digestive tract, which occurs in the stomach. Its immunohistochemical expression of CD117 and DOG-1 is positive, and the mutation of Kit gene is the main mechanism leading to the disease.Imatinib is a tyrosinase inhibitor that inhibits c-Kit activity as a first-line treatment for relapsed, unresectable or advanced GIGT patients with imatinib mesylate, which has been shown to be The most effective drug for the treatment of patients with advanced GIST can significantly improvethe prognosis. In the conventional treatment process, the blood concentration of imatinib is very different in different GIST patients. The lack of blood concentration leads to poor efficacy, and the excessive blood concentration leads to too much adverse reaction. The monitoring of drug concentration is of great significance for improving patient compliance and prognosis. At the same time, we can also explore the cause of the disease by detecting the blood concentration of Martini. However, the monitoring of the blood concentration of imatinib mesylate is mainly concentrated in foreign countries, and there are few domestic related studies. This article reviews the pharmacokinetics of imatinib, the status and problems of imatinib plasma concentration, and the significance of monitoring, in order to explore the monitoring and significant of imatinib blood concentration in patients with GIST.