Assessment of Pharmacokinetics and Food Effect of AD‐109, a Novel Formulation of Rivaroxaban 18 mg

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ABSTRACT Rivaroxaban is an oral anticoagulant that requires food intake at high doses (15 and 20 mg) due to a pronounced food effect. AD‐109 is a novel formulation of rivaroxaban 18 mg, designed to enhance oral bioavailability and mitigate the food effect. This study aimed to evaluate the pharmacokinetics (PKs) of AD‐109 compared to the conventional formulation, Xarelto (Xarelto, rivaroxaban 20 mg) and the effect of food on the PK of AD‐109. Two open‐label, single‐dose, two‐period, two‐sequence crossover studies were conducted. In Study 1, participants received a single dose of AD‐109 and Xarelto under fed state, while in Study 2, participants received a single dose of AD‐109 under fed and fasted state. Serial blood samples were collected up to 34 h post‐dose and PK parameters were calculated by non‐compartmental method. In both studies, 33 out of 36 volunteers completed the study. The geometric mean ratios (GMRs) and their 90% confidence intervals (CIs) for the maximum plasma concentration ( C max ) and area under the curve until the last measurable concentration (AUC 0‐last ) of rivaroxaban for AD‐109 to Xarelto were 1.0466 (0.9961–1.0996) and 0.9450 (0.9094–0.9819), falling within the bioequivalence range of 0.8–1.25. The corresponding values of AD‐109 in the fed to fasted state were 1.0475 (0.9789–1.1209) and 0.9795 (0.9371–1.0238), suggesting the systemic exposure was not substantially influenced by food intake. AD‐109 (rivaroxaban 18 mg) demonstrated a PK profile comparable to that of Xarelto (rivaroxaban 20 mg) and effectively minimized the food effect on drug exposure.

Ce résumé expose les affirmations des auteurs. BNTIC ne l’interprète pas comme une validation indépendante des résultats.