Xiaodong Wang
TESARO Inc., USA
Title: An open-label, randomized, pivotal bioequivalence study of oral rolapitant in healthy subjects
Biography
Biography: Xiaodong Wang
Abstract
Rolapitant (VARUBI®/VARUBY®), a selective and long-acting neurokinin-1 receptor antagonist, is approved in oral formulation for the prevention of delayed chemotherapy-induced nausea and vomiting in adults in the US and EU. This pivotal open-label, randomized, single-dose, multicenter, parallel-group study assessed the bioequivalence of a single oral dose of 180 mg rolapitant administered as tablets (2 × 90 mg tablets, commercial formulation) or capsules (4 × 45 mg capsules, formulation used in clinical development) in healthy subjects. Blood samples for pharmacokinetic analysis were collected pre-dose and at multiple time points up to 912 h post-dose. The pharmacokinetic analysis of the capsule group (n = 42) and tablet group (n = 42) were similar. The rolapitant tablet was considered bioequivalent to the rolapitant capsule if the 90% confidence intervals for the ratios of the geometric means for rolapitant, observed maximum plasma concentration (Cmax), and area under the curve (AUC0–∞) were within the 0.80–1.25 range. The geometric mean ratios of Cmax and AUC0–∞ were 0.99 (0.89–1.11) and 1.05 (0.92–1.19), respectively, establishing bioequivalence of the rolapitant tablet and capsule, and suggesting that data obtained during clinical development is translatable to the commercial formulation. Both formulations were well tolerated, with a similar incidence of treatment-emergent adverse events in the two groups.