代谢、排泄与药物动力学[(14)C] glasdegib (pf - 04449913)在健康志愿者口服。
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林杰,梁Vaz A, B, Y,杨X, Shaik MN
代谢、排泄与药物动力学[(14)C] glasdegib (pf - 04449913)在健康志愿者口服。
Xenobiotica。2017年12月,47 (12):1064 - 1076。doi: 10.1080 / 00498254.2016.1261307。Epub 2017年1月3。
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27866461 (在PubMed]
- 文摘
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1。代谢、排泄与药物动力学的glasdegib (pf - 04449913)进行调查后政府单剂量口服100毫克/ 100 muCi [(14) C] glasdegib六个健康男性志愿者(NCT02110342)。2。glasdegib的峰值浓度(890.3 ng / mL)和总辐射(1043 ngEq /毫升)发生在等离子体在post-dose 0.75小时。AUCinf 8469 ng。h /毫升和12230 ngEq。h /毫升分别glasdegib和总辐射。3所示。意味着复苏[(14)C] glasdegib-related放射性的排泄物是91%的服用剂量在尿液和粪便的42% (49%)。Glasdegib是主要的循环组件占了总数的69%在等离子体辐射。N-desmethyl代谢物和N-glucuronide代谢物的glasdegib代表循环放射性的8%和7%,分别。 Glasdegib was the major excreted component in urine and feces, accounting for 17% and 20% of administered dose in the 0-120 hour pooled samples, respectively. Other metabolites with abundance <3% of the total circulating radioactivity or dose in plasma or excreta were hydroxyl metabolites, a desaturation metabolite, N-oxidation and O-glucuronide metabolites. 4. Elimination of [(14)C]glasdegib-derived radioactivity was essentially complete, with similar contribution from urinary and fecal routes. Oxidative metabolism appears to play a significant role in the biotransformation of glasdegib.
