Effect of Food on the Single-dose Pharmacokinetics and Tolerability of Subutinib and its Active Metabolite in Chinese Healthy Volunteers

Abstract

The aim of this study is to investigate a food effect on the single-dose pharmacokinetics and tolerability of subutinib maleate capsules in healthy Chinese volunteers. The author evaluated the effect of being under a fasting or fed state at the time of drug intake on the single-dose of subutinib maleate capsules in a randomized, balanced, single-dose, 2-treatment (fasting and fed), 2-period design with a 3-week washout period. The end points were the maximum plasma drug concentration (C_max) and areas under the plasma-concentration curve (AUC) for 336 h exposure (AUC_0–336) and total exposure (AUC_0–∞). All volunteers completed the whole study without side effects being observed. For subutinib, C_max were 6.13 and 5.04 ng·mL⁻¹, and AUC_0–336 were 278.4 and 304.5 h·ng·mL⁻¹ in the fasting and the fed state, respectively. For active metabolite, C_max were 0.90 and 0.61 ng·mL⁻¹, and AUC_0–336 were 65.5 and 56.4 h·ng·mL⁻¹ in the fasting and the fed state, respectively. The authors showed that food intake was associated with a slight increase in AUC values but decrease in C_max of subutinib, and it was associated with a decrease both in AUC and C_max of active metabolite.

Key words

subutinib - active metabolite - food effect - tolerability - pharmacokinetics

^* These authors contributed equally to the completion of this study and the writing of this paper

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