An open-label, phase 1, randomized, three treatments, three-period, crossover, relative bioavailability study of CC-292, a potent and orally available inhibitor of bruton tyrosine kinase.

For all three formulations, following administration of CC-292 at a dose level of 250 mg under fasted conditions, CC-292 was rapidly absorbed with maximum plasma concentrations (Cmax) occurring at a median of 1.5-1.75 h (Tmax). P22-CAP formulation showed a similar range of Tmax compared to P01-CAP and P22-TAB showed a wider range of Tmax compared to P01-CAP. Comparable or higher Cmax and AUC0-∞ were noted for P22-TAB and P22-CAP formulations as compared to P01-CAP formulation. The relative bioavailability (Frel) of the CC-292 P22-TAB compared to the P01-CAP reference formulation was 1.02, and the relative bioavailability (Frel) of the CC-292 P22-CAP compared to the P01-CAP reference formulation was 1.23. In conclusion, CC-292 was well tolerated when administered as single 250-mg oral doses of P22-TAB, P22-CAP or P01-CAP in the fasted state in this group of healthy subjects. Given that CC-292 has shown favourable safety profiles in the current clinical settings, the new formulations (P22-TAB and P22-CAP) are similar as the reference formulation (P01-CAP).