A randomized, open-label study assessing the bioequivalence of two formulations of Fingolimod 0.5 mg in healthy subjects

Abstract

Fingolimod is an oral agent approved for the treatment of relapsing forms of multiple sclerosis (MS), which has demonstrated efficacy in Phase III trials in patients with relapsing-remitting MS (RRMS). The present study was designed to assess bioequivalence between a fingolimod Test capsule formulation (Teva Argentina, formerly IVAX Argentina S.A.) and a Reference capsule formulation (Novartis Pharma GmbH, Germany). In a single-center, randomized, single-dose, open-label, two-way crossover study under fed conditions, 16 healthy volunteers were randomized to receive a single oral dose of 0.5 mg of the Test and Reference formulations, with a 42-day washout period between administrations. The three pharmacokinetic (PK) parameters employed in the study to assess the bioequivalence between the Test and Reference formulations were maximum plasma concentration (Cmax), time to Cmax (Tmax), and area under the concentration–time curve from time zero to 72 h (AUC0–72). No significant differences between the Test and Reference formulations for any of the three PK parameters were observed. Based on 90% geometric confidence intervals (CIs) within 80% to 125% for both AUC0–72 and Cmax, the Test and Reference formulations were considered bioequivalent.