血管内皮生长因子受体酪氨酸激酶抑制剂[(14)C]-Tivozanib在健康男性参与者中的吸收、代谢和排泄:一项I期、开放标签、质量平衡研究
文章的细节
-
引用
复制到剪贴板 -
Cotreau MM, Hale CL, Jacobson L, Oelke CS, Strahs AL, Kochan RG, Sanga M, Slichenmyer W, Vargo DL
血管内皮生长因子受体酪氨酸激酶抑制剂[(14)C]-Tivozanib在健康男性参与者中的吸收、代谢和排泄:一项I期、开放标签、质量平衡研究
临床药学杂志，2012七月;1(3):102-9。doi: 10.1177 / 2160763 x12447303。
- PubMed ID
-
27121337 (PubMed视图］
- 摘要
-
目的:评价治疗肾细胞癌和实体性恶性肿瘤的新药替沃扎尼的吸收、代谢和排泄。方法:8名健康男性参与者接受单剂量1.5 mg (160 muCi)口服[(14)C]-tivozanib。全血、血清、尿液和粪便在给药28天后进行了药代动力学、放射分析和代谢物的评估。在整个研究过程中记录不良事件。结果:[(14)C]-替伏扎尼浓度在10.9 +/- 5.84 h时达到峰值。[(14) C]-替沃扎尼的平均血清半衰期为89.3 +/- 23.5小时。[(14) C]-tivozanib的最大浓度和曲线下面积分别为12.1 +/- 5.67 ng/mL和1084 +/- 417.0 ng.h/mL。总放射性平均回收率为91.0% +/- 11.0%;79.3% +/- 8.82%的放射性在粪便中以不变的替沃扎尼和代谢物的形式被回收。在尿液中，11.8% +/- 4.59%仅为代谢物。 No unchanged tivozanib was found in the urine. CONCLUSION: Tivozanib had a long half-life with no major circulating metabolite, was well tolerated as a single dose, and was primarily eliminated via feces with no unchanged tivozanib found in urine. These pharmacokinetic data of [(14) C]-tivozanib are consistent with previous studies of unlabeled tivozanib.
引用本文的药物库数据
- 药物