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.