Bioequivalence and Food Effect Assessment of Eltrombopag Olamine Tablets in Healthy Chinese Subjects: An Open, Randomized, Single‐Dose, and Two‐Period Crossover Study

Abstract

AbstractEltrombopag, a nonpeptide thrombopoietin receptor agonist, is primarily used for treating immune thrombocytopenic purpura. The aim of this study was to investigate the pharmacokinetic profile and food‐drug interaction of test and reference eltrombopag olamine tablets among healthy Chinese volunteers. An open, randomized, single‐dose, 2‐period crossover design was employed, involving fasting and fed conditions with a 10‐day washout period. Ninety‐six healthy volunteers received a single oral dose of 25 mg of the 2 eltrombopag formulations, with 48 participants in each group: fasting volunteers and those consuming a high‐fat, low‐calcium meal. Plasma eltrombopag concentrations were analyzed using liquid chromatography‐tandem mass spectrometry, and pharmacokinetic parameters were derived from the concentration‐time profiles. The geometric mean ratios, with 90% confidence intervals, for the maximum plasma concentration, area under the concentration‐time curve from time 0 to the last measurable concentration, and area under the concentration‐time curve from time 0 to infinity fell within the bioequivalence acceptance criteria (80%‐125%) under both fasting and fed conditions, indicating bioequivalence between the test and reference formulations. Administration of eltrombopag with a high‐fat, low‐calcium diet reduced the net systemic exposure by approximately 40%. Adverse events were recorded, and no serious adverse events were observed in either fasting or fed conditions. In conclusion, eltrombopag is well tolerated and exhibits a favorable safety profile in the Chinese population. The achievement of bioequivalence under fasting and fed conditions supports the demonstration of biosimilarity between the test and reference formulations.