Phase 0 clinical trial of single -dose imatinib mesylate in health Chinese male volunteers
10.13699/j.cnki.1001-6821.2015.15.014
- VernacularTitle:单次口服极低剂量甲磺酸伊马替尼在中国男性健康受试者的零期临床研究
- Author:
Jin WANG
1
;
Lu QI
;
Gang CHEN
;
Ze-Juan WANG
;
Jin-Tong LI
;
Tong ZHANG
;
Hui JIN
;
Xiao-Na LIU
;
Li FENG
;
Yu WANG
;
Chen LIU
;
Chun-Pu LEI
;
Ying LIU
;
Bao-Li ZHOU
;
Xing-He WANG
Author Information
1. 首都医科大学 附属北京世纪坛医院 药物 I期研究室
- Keywords:
imatinib mesylate;
microdose pharmacokinetic;
LC-MS/MS;
Phase 0
- From:
The Chinese Journal of Clinical Pharmacology
2015;(15):1512-1515
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluated the pharmacokinetics and safety of single microdose imatinib mesylate in Chinese health volunteers.Methods Eight subjects were randomly assigned to take orally a single microdose of 4 mg imatinib mesylate.The serum concentrations of ima-tinib were assayed with LC-MS/MS.Results The following pharmaco-kinetic parameters were calculated by WinNolin 6.3 software.Cmax (12.70 ±6.61 ) ng · mL-1, tmax ( 1.94 ±0.94 ) h, AUC0-24 h (90.10 ±37.70)ng· mL-1· h, t1/2 ( 10.40 ± 5.01 ) h, CL/F (47.20 ±33.40)L· h-1, V/F ( 541.00 ± 128.00 ) L, MRT (7.21 ±1.30)h.No adverse events and serious adverse events were detected.Conclusion Pharm-acokinetic parameters of phase 0 research of imatinib mesylate reflected the characteristics of the drug distribution and elimination in some extent.It was significant to protect subjects in phase 0 research by taking microdose imatinib mesylate.
