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• W2048690056 abstract "Dasatinib is a tyrosine kinase inhibitor (including BCR‐ABL and the SRC family) that is effective in patients with chronic myeloid leukemia. Dasatinib has pH‐dependent solubility and is bioavailable as an oral formulation. The effect of gastric pH modifiers on dasatinib pharmacokinetics is evaluated in an open‐label, randomized, 3‐period, 3‐treatment crossover study. Twenty‐four healthy subjects receive treatment A (2 doses of dasatinib 50 mg separated by 12 hours), treatment B (famotidine 40 mg given 2 hours after dasatinib 50 mg and 10 hours before another dose of dasatinib 50 mg), and treatment C (30 mL of an antacid containing aluminum/magnesium hydroxides given 2 hours before dasatinib 50 mg and concomitantly with dasatinib 50 mg 12 hours after the previous dasatinib dose); a 7‐day washout separates each treatment period. When famotidine is administered 2 hours after dasatinib, dasatinib exposure is similar to dasatinib administered alone. However, dasatinib exposure is reduced by ∼60% when famotidine is administered 10 hours before dasatinib dosing. In contrast, dasatinib exposure is unchanged when antacid (Maalox) is administered 2 hours before dasatinib; but when the antacid is coadministered with dasatinib, dasatinib exposure is reduced by ∼55% to 58%. This indicates that H 2 ‐receptor antagonists should not be coadministered with dasatinib. Dasatinib may be administered with acid‐neutralizing antacids if the doses are temporally separated by at least 2 hours." @default.
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• W2048690056 date "2009-06-01" @default.
• W2048690056 modified "2023-10-18" @default.
• W2048690056 title "Phase I Study of the Effect of Gastric Acid pH Modulators on the Bioavailability of Oral Dasatinib in Healthy Subjects" @default.
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• W2048690056 doi "https://doi.org/10.1177/0091270009333854" @default.
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