Pharmacokinetic study on single-dose intravenous temozolomide in glioma patients and health Chinese male volunteers
10.13699/j.cnki.1001-6821.2017.23.026
- VernacularTitle:单次静脉输注注射用替莫唑胺在中国脑胶质瘤患者和健康受试者的药代动力学研究
- Author:
Jin WANG
1
;
Gang CHEN
;
Xiao-Yi KONG
;
Yan LI
;
Ze-Juan WANG
;
Ying LIU
;
Lu QI
;
Chen LIU
;
Xiao-Na LIU
;
Chun-Pu LEI
;
Li FENG
;
Yu WANG
;
Bao-Li ZHOU
;
Wen-Bin LI
;
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,北京100038
- Keywords:
intravenous temozolomide;
early clinical reseach;
LC-MS/MS;
health volunteer;
glioma patient
- From:
The Chinese Journal of Clinical Pharmacology
2017;33(23):2416-2419
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the pharmacokinetics and safety of single micro dose in travenous temozolomidein Chinese health male volunteers or standard treatment in glioma patients.Methods 14 healthy subjects of phase 0 research were assigned to take a single microdose of 2 mg · m-2 intravenous temozolomide.24 glioma patients of phase Ⅰ research were assigned to take 150 mg · m-2 intravenous temozolomide.These rumconcentrations of temozolomide were assayed with LC-MS/MS.Results Fourteen healthy subjects pharmacokinetic parameters wereCmax (0.14 ± 0.03) μg · mL-1,tmax (80.40 ± 12.60) min,t1/2 (114.00±6.00) min,AUC0-24h (25.80 ±4.72) μg · mL-1 · min,AUC0-x (26.20 ±4.79) μg · mL-1 · min.Twenty-one glioma patients were included in the pharmacokinetic analysis,pharmacokinetic parameters were Cmax (7.92 ± 1.50) μg · mL-1,tmax (87.90 ± 5.38) min,t1/2 (108.00 ± 5.25) min,AUC0-24h (1530.00 ±270.00) μg · mL-1 · min,AUC0-∞ (1550.00 ±273.00) μg · mL-1 · min.All the 14 healthy volunteers and 24 glioma patients were included in the safety analysis.No adverse events were detected in health volunteers.6 gliomapatients experienced 7 adverse events related to temozolomide.There were no serious adverse events in two early clinical reseach.Conclusion Pharmacokinetic parameters of phase 0 research of intravenous temozolomide reflected the characteristics of the drug distribution and elimination in some extent.It is significative to follow-up clinical trials.
