Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2026
Bioequivalence of netupitant and palonosetron (NEPA) oral suspension and hard capsules in healthy individuals: results from an open-label, randomized, two-treatment, four-period, two-sequence replicative design trial.
СтатьяРандомизированное исследованиеКлиническое исследование I фазыНазвание и аннотация: Перевод в очереди
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Gasanin Edis, Bezzo Riccardo, Spinelli Tulla, Seitz Friedeborg
Аннотация
PURPOSE: NEPA, a fixed-antiemetic combination of netupitant and palonosetron, is available via two administration routes (oral and intravenous). A new oral suspension was developed to offer a more convenient option for patients. This study evaluated the bioequivalence between the oral capsule and the oral suspension.
METHODS: Open-label, randomized, single-center phase I trial conducted according to a two-treatment, four-period, two-sequence replicative design. Two treatments were investigated for bioequivalence: a 10-mL oral suspension (Test [T]) and the hard capsule (Reference [R]), both containing 300 mg netupitant/0.5 mg palonosetron. Healthy individuals were randomized (1:1) to receive two doses of both Test and Reference formulations, in either T-R-T-R or R-T-R-T sequence. The primary objective was to demonstrate AUC0-t bioequivalence of netupitant and palonosetron after a single dose of Test and Reference formulations.
RESULTS: In total, 72 participants were included. The geometric mean plasma concentration-time profiles of netupitant and palonosetron were similar for the Test and Reference formulations. The AUC0-t geometric means of both analytes were similar for the Test and Reference formulations. The 90% confidence interval of the Test/Reference ratios for AUC0-t of netupitant and palonosetron were within the acceptance range for bioequivalence of 80-125%. The AUC0-t variability was moderate for netupitant and low for palonosetron. Both formulations were well tolerated.
CONCLUSION: The NEPA oral suspension is pharmacokinetically bioequivalent to the capsule formulation in healthy individuals, with no new safety concerns. These findings support NEPA oral suspension as a potentially beneficial option for patients who prefer an oral suspension over a hard capsule and for those with swallowing difficulties. EUCT Number: 2023-504355-28-00 (25/08/2023).
METHODS: Open-label, randomized, single-center phase I trial conducted according to a two-treatment, four-period, two-sequence replicative design. Two treatments were investigated for bioequivalence: a 10-mL oral suspension (Test [T]) and the hard capsule (Reference [R]), both containing 300 mg netupitant/0.5 mg palonosetron. Healthy individuals were randomized (1:1) to receive two doses of both Test and Reference formulations, in either T-R-T-R or R-T-R-T sequence. The primary objective was to demonstrate AUC0-t bioequivalence of netupitant and palonosetron after a single dose of Test and Reference formulations.
RESULTS: In total, 72 participants were included. The geometric mean plasma concentration-time profiles of netupitant and palonosetron were similar for the Test and Reference formulations. The AUC0-t geometric means of both analytes were similar for the Test and Reference formulations. The 90% confidence interval of the Test/Reference ratios for AUC0-t of netupitant and palonosetron were within the acceptance range for bioequivalence of 80-125%. The AUC0-t variability was moderate for netupitant and low for palonosetron. Both formulations were well tolerated.
CONCLUSION: The NEPA oral suspension is pharmacokinetically bioequivalent to the capsule formulation in healthy individuals, with no new safety concerns. These findings support NEPA oral suspension as a potentially beneficial option for patients who prefer an oral suspension over a hard capsule and for those with swallowing difficulties. EUCT Number: 2023-504355-28-00 (25/08/2023).