CYP3A4型
药代动力学
药理学
伊马替尼
效力
化学
伏立康唑
药物相互作用
口服
新陈代谢
红霉素
细胞色素P450
髓系白血病
医学
体外
内科学
抗生素
生物化学
抗真菌
皮肤病科
作者
Jiangfei Chen,Suhang Guo,Xing Yu,Jinxiu Lei,Tao Xu,Suyan Zhu,Lu Chen,Ping Xu,Xuan Zhou,Lushan Yu
出处
期刊:PubMed
日期:2020-09-01
卷期号:75 (9): 424-429
被引量:2
摘要
Flumatinib, indicated for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia, is a structural analog of imatinib and has shown higher potency than imatinib as a BCR-ABL inhibitor. In this paper, the metabolic profile of flumatinib was studied. It was found that CYP3A4 and CYP2C8 were the main cytochrome P450 enzyme substyles catalyzing the metabolism of flumatinib, and CYP3A4 has a stronger metabolic ability for flumatinib than CYP2C8. Erythromycin, cyclosporine, and voriconazole can inhibit the metabolism of flumatinib in vitro. Accordingly, co-administration of erythromycin and cyclosporine with flumatinib increased the plasma concentration and the systemic exposure of flumatinib in rats, which indicated that lower doses should be considered in clinical practice.
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