A Phase 1 Study to Assess the Relative Bioavailability of Brigatinib Administered as an Oral Solution Versus an Immediate‐Release Tablet in Healthy Adults

Brigatinib is an ALK tyrosine kinase inhibitor approved for the treatment of adults with ALK + non‐small cell lung cancer. The commercial formulation of brigatinib is an immediate‐release (IR) tablet; however, an oral solution was developed for use in pediatric studies for patients unable to swallow solid oral dosage forms. This randomized, two‐period, two‐sequence crossover study assessed the relative bioavailability of the oral solution versus the IR tablet in healthy adults. Twelve participants received a single 90‐mg brigatinib dose as the oral solution or IR tablet on Day 1 of the first study period, followed by the alternate formulation on Day 1 of the second study period. Brigatinib pharmacokinetic parameters were similar following administration of the oral solution and IR tablet. The geometric least‐square mean ratios (oral solution vs IR tablet) for C max (0.92), AUC last (0.96), and AUC inf (0.96) were close to 1.00 with 90% confidence intervals within the bioequivalence range of 0.80–1.25 (C max , 0.87–0.98; AUC last , 0.88–1.04; AUC inf , 0.89–1.03). Treatment‐emergent adverse events were reported in three participants (25%), with the most frequent being cough (17%). These results indicate that the oral solution and IR tablet can be used interchangeably without dose adjustment in pediatric studies.