Asciminib (ABL001) is an orally administered allosteric inhibitor of the BCR-ABL 
tyrosine kinase. The current study evaluated the relative bioavailability of its 
2 tablet variants, AAA and NXA, compared with the capsule CSF and assessed the 
impact of food in healthy participants in a 2-arm, randomized, open-label, 4-way 
crossover design. The primary pharmacokinetic parameters analyzed were area 
under the plasma concentration-time curve (AUC) from time 0 to the time of last 
measurable concentration (AUClast ), AUC from time 0 to infinity (AUCinf ), and 
peak concentration (Cmax ). Forty-five healthy volunteers were enrolled, 22 in 
the AAA arm and 23 in the NXA arm. Under fasting conditions, the AUCinf , 
AUClast , and Cmax of the AAA tablet were similar to those of the capsule, but 
slightly higher (∼20%) for NXA and decreased with a high-fat meal (∼65%) and a 
low-fat meal (∼30%) for both tablet formulations. Overall, 20 participants (9 in 
the AAA arm; 11 in the NXA arm) experienced at least 1 adverse event, the most 
common in both arms being headache. The study showed that under fasting 
conditions, tablet AAA had bioavailability similar to that in the capsule CSF. 
The bioavailability of both tablet formulations decreased with food, with a more 
pronounced effect observed with a high-fat meal.