Pharmacokinetics and Safety of Fosaprepitant Dimeglumine in Healthy Chinese Volunteers: Bioequivalence Study.

Autor: Lu, Kang, Lin, Sisi, Wang, Yannan, Hao, Rui, Fang, Lu, Zhu, Jingjing, Zhao, Di, Yu, Jin, Tong, Shengjia, Wu, Yi, Si, Yongkai, Ye, Tiantian, Yang, Qigang, Wang, Ying
Předmět:
Zdroj: Clinical Pharmacology in Drug Development; Jul2021, Vol. 10 Issue 7, p748-755, 8p
Abstrakt: Fosaprepitant dimeglumine (FD) is a precursor of aprepitant. FD can be metabolized into aprepitant. This randomized, single‐center, open, 2‐cycle, single‐dose, crossover bioequivalence study compared the pharmacokinetics (PK) and safety of intravenously FD of test and reference products in healthy volunteers (HVs). HVs were assigned to the test group or reference group randomly and given FD intravenously. The plasma concentration of FD and aprepitant was measured using liquid chromatography‐tandem mass spectrometry. PK parameters were ascertained based on a noncompartmental model. Data for 29 HVs were obtained. The geometric mean and 90% confidence intervals of maximum plasma concentration (Cmax), area under the concentration‐time curve from time 0 to time of last measurable plasma concentration (AUC0‐t), and area from the last datum point to time infinity (AUC0‐∞) of test and reference groups were 101.69% (95.06%, 108.77%), 103.52% (99.15%, 108.09%), and 105.58% (99.51%, 112.01%), respectively. These 3 parameters were within the acceptance range of 80.0% to 125.00%, and the test product was bioequivalent to the reference product. The coefficient of variation (CV) of Cmax, AUC0‐t, and AUC0‐∞ was 15.14%, 9.67%, and 11.89%, respectively. Intravenously administered FD provided by 2 sponsors achieved bioequivalence. FD values from test and reference products were bioequivalent. All adverse events were mild and serious adverse events absent in HVs. This study indicated that FD may provide a safer alternative to aprepitant for chemotherapy‐induced nausea and vomiting. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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