AbstractPurposeThis randomized, open‐label, multiple‐dose, two‐period, crossover study compared the systemic bioavailability of mometasone furoate (MF) administered from a metered‐dose inhaler containing MF and formoterol fumarate (F) (MF/F‐MDI) versus MF administered from a single‐ingredient dry‐powder inhaler (MF‐DPI).MethodsHealthy, non‐smoking adults, 18–65 years with body mass index 18–29 kg/m2 (N = 12) received MF 800 µg/F 20 µg via MF/F‐MDI or MF 800 µg via MF‐DPI twice daily for 5 days separated by a 7‐day period. MF pharmacokinetics (AUC(0–12 hour), Cmax, and Tmax) were measured at Day 1 and 5 after each treatment. Safety and tolerability were assessed.ResultsSystemic exposure to MF based on AUC(0–12 hour) was ∼25% lower following MDI versus DPI administration. The Day 5 geometric mean ratio (MDI/DPI) estimates (90% confidence intervals [CI]) for AUC(0–12 hour) and Cmax were 0.747 (0.61, 0.91) and 0.606 (0.49, 0.75), respectively. The accumulation index (R) value for MF was higher following MDI (3.81‐fold) versus DPI administration (2.34‐fold) indicative of prolonged absorption. The most common adverse events were tremor, headache, and catheter site pain.ConclusionsSystemic exposure to MF was lower following multiple‐dose MF/F‐MDI administration versus MF‐DPI administration. The magnitude of this difference is not considered to be clinically important. MF/F‐MDI was safe and generally well tolerated.